Aryl nitrogen-containing bicyclic compounds and methods of use
First Claim
Patent Images
1. A compound of Formula I:
- or stereoisomer, tautomer, solvate, pharmaceutically acceptable salt, derivative or prodrug thereof, wherein A1 is CR5 or N;
one of A2 and A3, independently, is CR5 or N;
B is a direct bond, (CR5R6), C(O), NR6, O, S, S(O) or SO2;
R1 is halo, haloalkyl, NO2, CN, R7, NR7R7, NR7R8, OR7;
SR7, OR8, SR8, C(O)R7, OC(O)R7, COOR7, C(O)R8, OC(O)R8, COOR8, C(O)NR7R7, C(S)NR7R7, NR7C(O)R7, NR7C(S)R7, NR7C(O)NR7R7, NR7C(S)NR7R7, NR7(COOR7), OC(O)NR7R7, C(O)NR7R8, C(S)NR7R8, NR7C(O)R8, NR7C(S)R8, NR7C(O)NR7R8, NR7C(S)NR7R8, NR7(COOR8), OC(O)NR7R8, S(O)2R7, S(O)2NR7R7, NR7S(O)2NR7R7, NR7S(O)2R7, S(O)2R8, S(O)2NR7R8, NR7S(O)2NR7R8 or NR7S(O)2R8;
R2 is H, halo, haloalkyl, NO2, CN, OR7, SR7, NR7R7, C(O)R7, COOR7, C(O)NR7R7, C(O)NR7R8, NR7C(O)NR7R7, NR7C(O)NR7R8, OC(O)NR7R8, S(O)2R7, S(O)2NR7R7, S(O)2NR7R8, NR7S(O)2R7, NR7S(O)2R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R3 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, wherein said ring system is substituted independently with one or more substituents of R10, R11, R16, NR10R10, NR10R11, OR10, SR10, OR11, SR11, C(O)R10, C(S)R10, C(NCN)R10, C(O)R11, C(S)R11, C(NCN)R11, C(O)C(O)R10, OC(O)R10, COOR10, C(O)SR10, C(O)C(O)R11, OC(O)R11, COOR11, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, OC(O)NR10R11, NR10C(O)R10, NR10C(O)R11, NR10C(S)R10, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), NR10C(O)C(O)R10, NR10C(O)C(O)R11, NR10C(O)C(O)NR10R11, S(O)2R10, S(O)2R11, S(O)2NR10R11, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)2R11;
R4 is H, halo, haloalkyl, NO2, NR7R7, NR7R8, CN, OR7, SR7, C(O)R7, OC(O)R7, COOR7, C(O)NR7R7, C(O)NR7R8, NR7C(O)R7, NR10C(O)R8, NR8C(O)NR7R8, NR7(COOR7), OC(O)NR7R8, S(O)2R7, S(O)2NR7R8, NR7S(O)2NR7R8, NR7S(O)2R7, NR7S(O)2R7, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R5 is H, halo, haloalkyl, NO2, CN, SR7, OR7, C(O)R7, COOR7, OC(O)R7, NR7R7, NR7R8, C(O)NR7R7, C(O)NR7R8, NR7C(O)R7, NR7C(O)NR7R8, S(O)NR7R8, S(O)2NR7R8, NR7S(O)2NR7R8, NR7S(O)2NR7R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R6 is H, CN or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R7 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of NR8R9, NR9R9, OR8, SR8, OR9, SR9, C(O)R8, OC(O)R8, COOR8, C(O)R9, OC(O)R9, COOR9, C(O)NR8R9, C(O)NR9R9, NR9C(O)R8, NR9C(O)R9, NR9C(O)NR8R9, NR9C(O)NR9R9, NR9(COOR8), NR9(COOR9), OC(O)NR8R9, OC(O)NR9R9, S(O)2R8, S(O)2NR8R9, S(O)2R9, S(O)2NR9R9, NR9S(O)2NR8R9, NR9S(O)2NR9R9, NR9S(O)2R8, NR9S(O)2R9, R8 or R9;
R8 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-3 substituents of R9, oxo, NR9R9, OR9;
SR9, C(O)R9 or a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and optionally substituted independently with 1-3 substituents of R9;
alternatively, R7 and R8 taken together form a saturated or partially or fully unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-3 substituents of R9;
R9 is H, halo, haloalkyl, CN, OH, NO2, NH2, acetyl, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl or a saturated or partially or fully unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, wherein each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl and ring of said ring system is optionally substituted independently with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, OH, oxo, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamine, dimethylamine, ethylamine, diethylamine, propylamine, isopropylamine, dipropylamine, diisopropylamine, benzyl or phenyl;
R10 is H, halo, haloalkyl, CN, NO2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-11-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R11, R12 or R16, NR11R12, NR12R12, OR11, SR11, OR12, SR12, C(O)R11, OC(O)R11, COOR11, C(O)R12, OC(O)R12, COOR12, C(O)NR11R12, NR12C(O)R11, C(O)NR12R12, NR12C(O)R12, NR12C(O)NR11R12, NR12C(O)NR12R12, NR12(COOR11), NR12(COOR12), OC(O)NR11R12, OC(O)NR12R12, S(O)2R11, S(O)2R12, S(O)2NR11R12, S(O)2NR12R12, NR12S(O)2NR11R12, NR12S(O)2NR12R12, NR12S(O)2R11, NR12S(O)2R12, NR12S(O)2R11 or NR12S(O)2R12;
R11 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-5 substituents of R12, R13, R14 or R16;
alternatively, R10 and R11 taken together form a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-5 substituents of R12, R13, R14 or R16;
R12 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkyl, each of which is optionally substituted independently with 1-5 substituents of R13, R14, R15 or R16;
R13 is NR14R15, NR15R15, OR14;
SR14, OR15;
SR15, C(O)R14, OC(O)R14, COOR17, C(O)R15, OC(O)R15, COOR15, C(O)NR14R15, C(O)NR15R15, NR14C(O)R14, NR15C(O)R14, NR14C(O)R15, NR15C(O)R15, NR15C(O)NR14R15, NR15C(O)NR15R15, NR15(COOR14), NR15(COOR15), OC(O)NR14R15, OC(O)NR15R15, S(O)2R14, S(O)2R15, S(O)2NR14R15, S(O)2NR15R15, NR14S(O)2NR14R15, NR15S(O)2NR15R15, NR14S(O)2R14 or NR15S(O)2R15;
R14 is a partially or fully saturated or unsaturated 5-8 membered or a saturated or partially or fully unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-5 substituents of R15 or R16;
R15 is H or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkoxyl, each of which is optionally substituted independently with 1-5 substituents of R16; and
R16 is H, halo, haloalkyl, CN, OH, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, oxo, acetyl, benzyl, phenyl, cyclopropyl, cyclobutyl or a partially or fully saturated or unsaturated 5-8 membered monocyclic or 6-12 membered bicyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic or 1-6 heteroatoms if bicyclic, said heteroatoms selected from O, N, or S, and optionally substituted independently with 1-5 substituents of halo, haloalkyl, CN, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, benzyl or phenyl;
provided that (1) when R1 is NR7R8, R8 is not a substituted or unsubstituted phenyl or a 9- or 10-membered bicyclic heterocycle containing 1 or 2 nitrogen atoms;
(2) when R2 is NR7R7, each R7, independently, is H;
(3) when R3 is substituted aryl or substituted heteroaryl, the substituents are not halo, N-alkyl, N-dialkyl, N-diaryl, N-diheteroaryl, OH, O-alkyl, O-aryl, O-heteroaryl, SH, S-alkyl, S-aryl or S-heteroaryl;
(4) when A2 is N and A3 is CH, then R4 is not halo, hydroxyl, NH2, or a mono- or di-alkyl, alkylamino, alkenyl, alkynyl, or aryl substituted amine;
or (5) when each of A1, A2 and A3 is, independently, CR5, then no more than two of R2, R4 and R5 is NR7R8 or C1-2-alkyl-R8.
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Abstract
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I
wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
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Citations
61 Claims
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1. A compound of Formula I:
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or stereoisomer, tautomer, solvate, pharmaceutically acceptable salt, derivative or prodrug thereof, wherein A1 is CR5 or N;
one of A2 and A3, independently, is CR5 or N;
B is a direct bond, (CR5R6), C(O), NR6, O, S, S(O) or SO2;
R1 is halo, haloalkyl, NO2, CN, R7, NR7R7, NR7R8, OR7;
SR7, OR8, SR8, C(O)R7, OC(O)R7, COOR7, C(O)R8, OC(O)R8, COOR8, C(O)NR7R7, C(S)NR7R7, NR7C(O)R7, NR7C(S)R7, NR7C(O)NR7R7, NR7C(S)NR7R7, NR7(COOR7), OC(O)NR7R7, C(O)NR7R8, C(S)NR7R8, NR7C(O)R8, NR7C(S)R8, NR7C(O)NR7R8, NR7C(S)NR7R8, NR7(COOR8), OC(O)NR7R8, S(O)2R7, S(O)2NR7R7, NR7S(O)2NR7R7, NR7S(O)2R7, S(O)2R8, S(O)2NR7R8, NR7S(O)2NR7R8 or NR7S(O)2R8;
R2 is H, halo, haloalkyl, NO2, CN, OR7, SR7, NR7R7, C(O)R7, COOR7, C(O)NR7R7, C(O)NR7R8, NR7C(O)NR7R7, NR7C(O)NR7R8, OC(O)NR7R8, S(O)2R7, S(O)2NR7R7, S(O)2NR7R8, NR7S(O)2R7, NR7S(O)2R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R3 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, wherein said ring system is substituted independently with one or more substituents of R10, R11, R16, NR10R10, NR10R11, OR10, SR10, OR11, SR11, C(O)R10, C(S)R10, C(NCN)R10, C(O)R11, C(S)R11, C(NCN)R11, C(O)C(O)R10, OC(O)R10, COOR10, C(O)SR10, C(O)C(O)R11, OC(O)R11, COOR11, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, OC(O)NR10R11, NR10C(O)R10, NR10C(O)R11, NR10C(S)R10, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), NR10C(O)C(O)R10, NR10C(O)C(O)R11, NR10C(O)C(O)NR10R11, S(O)2R10, S(O)2R11, S(O)2NR10R11, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)2R11;
R4 is H, halo, haloalkyl, NO2, NR7R7, NR7R8, CN, OR7, SR7, C(O)R7, OC(O)R7, COOR7, C(O)NR7R7, C(O)NR7R8, NR7C(O)R7, NR10C(O)R8, NR8C(O)NR7R8, NR7(COOR7), OC(O)NR7R8, S(O)2R7, S(O)2NR7R8, NR7S(O)2NR7R8, NR7S(O)2R7, NR7S(O)2R7, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R5 is H, halo, haloalkyl, NO2, CN, SR7, OR7, C(O)R7, COOR7, OC(O)R7, NR7R7, NR7R8, C(O)NR7R7, C(O)NR7R8, NR7C(O)R7, NR7C(O)NR7R8, S(O)NR7R8, S(O)2NR7R8, NR7S(O)2NR7R8, NR7S(O)2NR7R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R6 is H, CN or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R7 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of NR8R9, NR9R9, OR8, SR8, OR9, SR9, C(O)R8, OC(O)R8, COOR8, C(O)R9, OC(O)R9, COOR9, C(O)NR8R9, C(O)NR9R9, NR9C(O)R8, NR9C(O)R9, NR9C(O)NR8R9, NR9C(O)NR9R9, NR9(COOR8), NR9(COOR9), OC(O)NR8R9, OC(O)NR9R9, S(O)2R8, S(O)2NR8R9, S(O)2R9, S(O)2NR9R9, NR9S(O)2NR8R9, NR9S(O)2NR9R9, NR9S(O)2R8, NR9S(O)2R9, R8 or R9;
R8 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-3 substituents of R9, oxo, NR9R9, OR9;
SR9, C(O)R9 or a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and optionally substituted independently with 1-3 substituents of R9;
alternatively, R7 and R8 taken together form a saturated or partially or fully unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-3 substituents of R9;
R9 is H, halo, haloalkyl, CN, OH, NO2, NH2, acetyl, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl or a saturated or partially or fully unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, wherein each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl and ring of said ring system is optionally substituted independently with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, OH, oxo, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamine, dimethylamine, ethylamine, diethylamine, propylamine, isopropylamine, dipropylamine, diisopropylamine, benzyl or phenyl;
R10 is H, halo, haloalkyl, CN, NO2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-11-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R11, R12 or R16, NR11R12, NR12R12, OR11, SR11, OR12, SR12, C(O)R11, OC(O)R11, COOR11, C(O)R12, OC(O)R12, COOR12, C(O)NR11R12, NR12C(O)R11, C(O)NR12R12, NR12C(O)R12, NR12C(O)NR11R12, NR12C(O)NR12R12, NR12(COOR11), NR12(COOR12), OC(O)NR11R12, OC(O)NR12R12, S(O)2R11, S(O)2R12, S(O)2NR11R12, S(O)2NR12R12, NR12S(O)2NR11R12, NR12S(O)2NR12R12, NR12S(O)2R11, NR12S(O)2R12, NR12S(O)2R11 or NR12S(O)2R12;
R11 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-5 substituents of R12, R13, R14 or R16;
alternatively, R10 and R11 taken together form a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-5 substituents of R12, R13, R14 or R16;
R12 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkyl, each of which is optionally substituted independently with 1-5 substituents of R13, R14, R15 or R16;
R13 is NR14R15, NR15R15, OR14;
SR14, OR15;
SR15, C(O)R14, OC(O)R14, COOR17, C(O)R15, OC(O)R15, COOR15, C(O)NR14R15, C(O)NR15R15, NR14C(O)R14, NR15C(O)R14, NR14C(O)R15, NR15C(O)R15, NR15C(O)NR14R15, NR15C(O)NR15R15, NR15(COOR14), NR15(COOR15), OC(O)NR14R15, OC(O)NR15R15, S(O)2R14, S(O)2R15, S(O)2NR14R15, S(O)2NR15R15, NR14S(O)2NR14R15, NR15S(O)2NR15R15, NR14S(O)2R14 or NR15S(O)2R15;
R14 is a partially or fully saturated or unsaturated 5-8 membered or a saturated or partially or fully unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-5 substituents of R15 or R16;
R15 is H or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkoxyl, each of which is optionally substituted independently with 1-5 substituents of R16; and
R16 is H, halo, haloalkyl, CN, OH, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, oxo, acetyl, benzyl, phenyl, cyclopropyl, cyclobutyl or a partially or fully saturated or unsaturated 5-8 membered monocyclic or 6-12 membered bicyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic or 1-6 heteroatoms if bicyclic, said heteroatoms selected from O, N, or S, and optionally substituted independently with 1-5 substituents of halo, haloalkyl, CN, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, benzyl or phenyl;
provided that (1) when R1 is NR7R8, R8 is not a substituted or unsubstituted phenyl or a 9- or 10-membered bicyclic heterocycle containing 1 or 2 nitrogen atoms;
(2) when R2 is NR7R7, each R7, independently, is H;
(3) when R3 is substituted aryl or substituted heteroaryl, the substituents are not halo, N-alkyl, N-dialkyl, N-diaryl, N-diheteroaryl, OH, O-alkyl, O-aryl, O-heteroaryl, SH, S-alkyl, S-aryl or S-heteroaryl;
(4) when A2 is N and A3 is CH, then R4 is not halo, hydroxyl, NH2, or a mono- or di-alkyl, alkylamino, alkenyl, alkynyl, or aryl substituted amine;
or(5) when each of A1, A2 and A3 is, independently, CR5, then no more than two of R2, R4 and R5 is NR7R8 or C1-2-alkyl-R8. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 18, 19, 21, 22, 24, 26, 29, 33, 35, 37, 39, 41, 43, 45, 51, 53)
R3 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, dihydrobenzofuranyl, benzothiophenyl or benzimidazolyl, each of which is optionally substituted with 1-3 substitutions of R16.
-
-
7. The compound of claim 1 wherein R3 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, dihydrobenzofuranyl, benzothiophenyl or benzimidazolyl, each of which is optionally substituted with and 1-2 subsitutions of R10 and 1 substitution of R11.
-
8. The compound of claim 1 wherein B is a direct bond.
-
9. The compound of claim 1 wherein
A1 is N; -
A2 is CR5 or N;
A3 is CR5;
R2 is H; and
R3 is an optionally substituted phenyl, naphthyl, pyridyl, pyrimidyl, pyrazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, dihydrobenzofuranyl, benzothiophenyl or benzimidazolyl.
-
-
10. The compound of claim 1 wherein
R1 is NR7R7 or NR7R8; - and
R3 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, dihydrobenzofuranyl, benzothiophenyl or benzimidazolyl, each of which is optionally substituted with 1-3 substitutions of R16.
- and
-
18. The compound of claim 1, and pharmaceutically acceptable salts thereof, selected from:
-
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(3-chloro-2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-fluorobenzamide;
5-(2-amino-6-quinazolinyl)-N-(3-(1-methyl-4-piperidinyl)-5-(trifluoromethyl)phenyl)-3-thiophenecarboxamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-methyl-3-((4-methyl-1-piperazinyl)methyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-(1,1-dimethylethyl)-3-((N,N-dimethylglycyl)amino)phenyl)-4-methylbenzamide;
3-(((3-(2-amino-6-quinazolinyl)-4-methylphenyl)carbonyl)amino)-2,6-difluoro-N-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-fluoro-4-(1-pyrrolidinyl)-3-(1-pyrrolidinylcarbonyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-methyl-3-((4-morpholinylacetyl)amino)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-methyl-3-((4-morpholinylacetyl)amino)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-((N,N-diethylglycyl)amino)-2-methylphenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(1-(N,N-diethylglycyl)-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(3,3-dimethyl-1-(4-morpholinylacetyl)-2,3-dihydro-1H-indol-6-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-((trifluoromethyl)oxy)phenyl)benzamide;
phenylmethyl 3-(2-amino-6-quinazolinyl)-4-methylbenzoate;
3-(2-amino-6-quinazolinyl)-N-(6-chloro-3-pyridinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(4-(cyclopropylethynyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(4-bromo-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(phenylethynyl)-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-chloro-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-((2,2,2-trifluoroethyl)oxy)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-((3-(1-piperidinyl)propyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-((3-(1-piperidinyl)propyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-((3-(dimethylamino)propyl)oxy)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(4-((2-(diethylamino)ethyl)oxy)-2-(methyloxy)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(5-((2-(diethylamino)ethyl)oxy)-2-(methyloxy)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2,4-bis(methyloxy)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(5-((diethylamino)sulfonyl)-2-(methyloxy)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2,3-dichlorophenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2,6-bis(methyloxy)-3-pyridinyl)-4-methylbenzamide;
N-(2-(acetylamino)-5-(trifluoromethyl)phenyl)-3-(2-amino-6-quinazolinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-5-((3-(4-methyl-1-piperazinyl)propyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2,2-difluoro-1,3-benzodioxol-4-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2,2,3,3-tetrafluoro-2,3-dihydro-1,4-benzodioxin-5-yl)benzamide;
3-(7-isoquinolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(1-hydroxy-7-isoquinolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(7-isoquinolinyl)-N-(2-(1-piperidinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(1-piperidinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-(methylamino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
4-(2-amino-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3R)-3-(dimethylamino)-1-pyrrolidinyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(1-piperidinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2,5-bis(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2,5-bis(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(4-morpholinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(1-pyrrolidinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(dimethylamino)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
N-(3-(2-amino-6-quinazolinyl)-5-(trifluoromethyl)phenyl)-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-5-(trifluoromethyl)phenyl)-3-(1-methylethyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-((3R)-1-methyl-3-piperidinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-(1-methylethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(2-(dimethylamino)-1,1-dimethylethyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(2-(dimethylamino)-1,1-dimethylethyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyl((3S)-1-methyl-3-pyrrolidinyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
N-(2-(2-(dimethylamino)-1,1-dimethylethyl)-5-(trifluoromethyl)phenyl)-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(methyl((3R)-1-methyl-3-pyrrolidinyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-(methylamino)-6-quinazolinyl)-N-(2-((4-methyl-1-piperazinyl)methyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-((4-methyl-1-piperazinyl)methyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(2,4-diaminopyrido[2,3-d]pyrimidin-6-yl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-2-fluoro-N-(2-(1-piperidinyl)-5-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-fluorobenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(2-(dimethylamino)ethyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
5-(2-amino-6-quinazolinyl)-2-fluoro-N-(2-(methyl((3R)-1-methyl-3-pyrrolidinyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-((2-(1-pyrrolidinyl)ethyl)oxy)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(1-methylethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-2-fluoro-N-(2-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3S)-3-(dimethylamino)-1-piperidinyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3R)-3-(dimethylamino)-1-pyrrolidinyl)-5-(trifluoromethyl)phenyl)-2-fluorobenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(4-(dimethylamino)-1-piperidinyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-((trifluoromethyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(1,1-dimethylethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(1,1-dimethylethyl)phenyl)-2-fluorobenzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-ethynylphenyl)-2-fluorobenzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-fluorobenzamide;
5-(2-amino-6-quinazolinyl)-N-(2-(dimethylamino)-5-(trifluoromethyl)phenyl)-2-fluorobenzamide;
N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-fluoro-5-(2-(methylamino)-6-quinazolinyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(pentafluoroethyl)phenyl)-2-fluorobenzamide;
6-(2,6-dimethylphenyl)-2-quinazolinamine;
3-(2-amino-6-quinazolinyl)-N-(2-(dimethylamino)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-(1,1-dimethylethyl)phenyl)benzamide;
6-(2,6-bis(methyloxy)phenyl)-2-quinazolinamine;
N-(3-(1,1-dimethylethyl)phenyl)-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3,5-bis(methyloxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-3-isoxazolyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-((1,1,2,2-tetrafluoroethyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-1H-pyrazol-3-yl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-chlorophenyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(5-bromo-2-((3-(dimethylamino)propyl)(methyl)amino)phenyl)-2-fluorobenzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)oxy)-5-(trifluoromethyl)phenyl)-2-fluorobenzamide;
5-(2-amino-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)-2-thiophenecarboxamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-(1-methyl-4-piperidinyl)-5-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-thiophenecarboxamide;
5-(2-amino-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)-3-thiophenecarboxamide;
5-(2-amino-6-quinazolinyl)-N-(2-(2-(dimethylamino)ethyl)-5-(trifluoromethyl)phenyl)-2-fluorobenzamide;
N-(4-(2-amino-6-quinazolinyl)-3-methylphenyl)-N′
-(3-fluoro-5-(trifluoromethyl)phenyl)urea;
5-(2-amino-6-quinazolinyl)-N-(5-chloro-2-((3-(dimethylamino)propyl)(methyl)amino)phenyl)-2-fluorobenzamide;
4-methyl-3-(2-(4-methyl-1-piperazinyl)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(4-(2-amino-6-quinazolinyl)-3-methylphenyl)-N′
-(5-chloro-2-(methyloxy)phenyl)urea;
4-(2-amino-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)-2-pyridinecarboxamide;
3-(2-amino-6-quinazolinyl)-N-(2-(((3-(dimethylamino)propyl)(methyl)amino)sulfonyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
4-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-pyridinecarboxamide;
4-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-thiophenecarboxamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-3-thiophenecarboxamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-(methyloxy)benzamide;
5-(2-amino-6-quinazolinyl)-2-chloro-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-chloro-2-((3-(dimethylamino)propyl)(methyl)amino)phenyl)-4-methylbenzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2,3-dihydro-1-benzofuran-7-carboxamide;
5-(2-amino-6-quinazolinyl)-2-bromo-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-((trifluoromethyl)oxy)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-2,3-bis(methyloxy)-N-(3-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-2-(methyloxy)-N-(3-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(5-cyclopropyl-2-((3-(dimethylamino)propyl)(methyl)amino)phenyl)-2-fluorobenzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2,3-bis(methyloxy)benzamide;
5-(2-amino-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)-2,3-dihydro-1-benzofuran-7-carboxamide;
5-(2-amino-6-quinazolinyl)-3-bromo-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-(methyloxy)benzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-(methyloxy)benzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-1-methyl-2-oxo-1,2-dihydro-3-pyridinecarboxamide;
5-(2-amino-6-quinazolinyl)-2-fluoro-N-(3-((4-methyl-1-piperazinyl)methyl)-5-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-2,3-bis(methyloxy)-N-(3-((4-methyl-1-piperazinyl)methyl)-5-(trifluoromethyl)phenyl)benzamide;
1-(4-(2-amino-6-quinazolinyl)-3-methylphenyl)-3-(3-(trifluoromethyl)phenyl)-2-imidazolidinone;
5-(2-amino-6-quinazolinyl)-2-(methyloxy)-N-(3-((4-methyl-1-piperazinyl)methyl)-5-(trifluoromethyl)phenyl)benzamide;
N-(4-(2-amino-6-quinazolinyl)phenyl)-N′
-(3-fluoro-5-(trifluoromethyl)phenyl)urea;
N-(4-(2-amino-6-quinazolinyl)phenyl)-N′
-(3-fluorophenyl)urea;
5-(2-amino-6-quinazolinyl)-2-((2-(dimethylamino)ethyl)oxy)-N-(3-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-2-(methyloxy)-N-(3-((trifluoromethyl)oxy)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-2,3,4-tris(methyloxy)-N-(3-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2,3,4-tris(methyloxy)benzamide;
5-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-(ethyloxy)benzamide;
3-(2-amino-6-quinazolinyl)-2,6-bis(methyloxy)-N-(3-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-2-(dimethylamino)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
N-(4-(2-amino-6-quinazolinyl)-3-methylphenyl)-3-(trifluoromethyl)benzamide;
N-(4-(2-amino-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
N-(4-(4-amino-6-quinazolinyl)phenyl)-N′
-(3-fluorophenyl)urea;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2,6-bis(methyloxy)benzamide;
5-(2-amino-6-quinazolinyl)-2-fluoro-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3-(1-methylethyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)cyclopropanecarboxamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)-2,3-dichlorobenzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)-4-(1,1-dimethylethyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)-3-fluoro-5-(trifluoromethyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)-3,5-bis(methyloxy)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)-3-(1-methylethyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)-2-fluoro-5-(trifluoromethyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)-2-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)-2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-fluorophenyl)-2-((3R)-3-(dimethylamino)-1-pyrrolidinyl)-5-(trifluoromethyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(1,1-dioxido-4-thiomorpholinyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-phenylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(phenyloxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2,4-bis(methyloxy)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-cyclohexyl-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(1-piperidinyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-chloro-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-cyclopentyl-4-methylbenzamide;
N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-4-methylphenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(1-methyl-4-piperidinyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(4-methyl-1-piperazinyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-methyl-6-(methyloxy)-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-chloro-4-((2-(1-piperidinyl)ethyl)oxy)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-fluoro-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(5-quinolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(8-quinolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5,6-bis(methyloxy)-1,3-cyclohexadien-1-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(5-chloro-6-(methyloxy)-1,3-cyclohexadien-1-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-4,5-dimethylphenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(6-((3-(dimethylamino)propyl)(methyl)amino)-2-methyl-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-4-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(methyloxy)-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
N-(4-chloro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-chloro-2-methyl-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
N-(4-chloro-2-methyl-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(2-fluoro-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-N′
-(3-(trifluoromethyl)phenyl)urea;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(4-methyl-1-piperazinyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(phenylmethyl)benzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-3-(2-amino-6-quinazolinyl)-4-methylbenzamide;
N-(1-acetyl-2,3-dihydro-1H-indol-6-yl)-3-(2-amino-6-quinazolinyl)-4-methylbenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-N′
-phenylurea;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-N′
-(4-(phenyloxy)phenyl)urea;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-N′
-(3,5-bis(methyloxy)phenyl)urea;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-pyridinylmethyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-pyridinylmethyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-((1R)-1-phenylethyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-((3-(trifluoromethyl)phenyl)methyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3,5-bis(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2,3-dihydro-1H-inden-4-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methylsulfanyl)-3-(trifluoromethyl)phenyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-N′
-(phenylmethyl)urea;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-N′
-(3-(trifluoromethyl)phenyl)thiourea;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-N′
-phenylthiourea;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(pentafluoroethyl)phenyl)benzamide;
3-(trifluoromethyl)phenyl 3-(2-amino-6-quinazolinyl)-4-methylphenylcarbamate;
N-(6-(2-methyl-5-((phenylcarbonyl)amino)phenyl)-2-quinazolinyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3-(trifluoromethyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-((1S)-1-phenylethyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-((1R)-2-(dimethylamino)-1-phenylethyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-((1R)-2-(4-methyl-1-piperazinyl)-1-phenylethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-4-(1,1-dimethylethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2,3-dichlorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3,5-bis(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2-fluoro-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-4-((trifluoromethyl)oxy)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3,5-dichlorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3-fluoro-5-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-4-(methyloxy)-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2,3-dichlorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2-methyl-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2-naphthalenecarboxamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-1-naphthalenecarboxamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2,2-difluoro-1,3-benzodioxole-4-carboxamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-2-naphthalenecarboxamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3-(1,1-dimethylethyl)-1-methyl-1H-pyrazole-5-carboxamide;
4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
2,3-dichloro-N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)benzamide;
N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-N′
-(3-(trifluoromethyl)phenyl)urea;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3-chloro-2-fluorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3-fluoro-2-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-1-benzofuran-2-carboxamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-1,3-dimethyl-1H-thieno[2,3-c]pyrazole-5-carboxamide;
N-(3-(2-amino-6-quinazolinyl)-4-(trifluoromethyl)phenyl)-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-(trifluoromethyl)phenyl)-N′
-(3-(trifluoromethyl)phenyl)urea;
2,3-dichloro-N-(4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)phenyl)benzamide;
N-(2,3-dihydro-1H-inden-4-yl)-4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3-(trifluoromethyl)benzenesulfonamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-((1S)-1-(1,3-thiazol-2-yl)ethyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2,3-dimethyl-4-(methyloxy)phenyl)-4-methylbenzamide;
N-(1-acetyl-2,3-dihydro-1H-indol-7-yl)-3-(2-amino-6-quinazolinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(1-methyl-1H-indol-4-yl)benzamide;
N,N′
-bis(3-(2-amino-6-quinazolinyl)-4-methylphenyl)urea;
N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(methyloxy)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2,1,3-benzoxadiazol-4-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(2-cyanoethyl)-2,4,5,6-tetrahydrocyclopenta[c]pyrazol-3-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(4-((3-(diethylamino)propyl)oxy)-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-((1-methyl-4-piperidinyl)oxy)-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-fluoro-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
N-(4-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-cyano-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
3-(2-(cyclopropylamino)-6-quinazolinyl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)benzamide;
N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((4-((3-(1-piperidinyl)propyl)oxy)phenyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-((3-(2-oxo-1-pyrrolidinyl)propyl)amino)-6-quinazolinyl)benzamide;
3-(2-(((1-ethyl-4-piperidinyl)methyl)amino)-6-quinazolinyl)-4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
3-(2-(cyclopropylamino)-6-quinazolinyl)-4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
6-(2,6-dimethylphenyl)-N-(2-(4-morpholinyl)ethyl)-2-quinazolinamine;
6-(2,6-dimethylphenyl)-N-(4-(4-methyl-1-piperazinyl)phenyl)-2-quinazolinamine;
6-(2,6-dimethylphenyl)-N-(4-((3-(1-piperidinyl)propyl)oxy)phenyl)-2-quinazolinamine;
5-(2-amino-6-quinazolinyl)-2-fluoro-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
2-fluoro-4-methyl-5-(2-(methylamino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
5-(2-(cyclopropylamino)-6-quinazolinyl)-2-fluoro-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-(cyclopropylamino)-6-quinazolinyl)-4-methyl-N-(4-((1-methyl-4-piperidinyl)oxy)-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(4,4-dimethyl-2-oxo-1,2,3,4-tetrahydro-7-quinolinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(4,4-dimethyl-1,2,3,4-tetrahydro-7-quinolinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(4,4-dimethyl-1,2,3,4-tetrahydro-7-isoquinolinyl)-4-methylbenzamide;
5-(2-amino-6-quinazolinyl)-2-fluoro-N-(4-(trifluoromethyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(4,4-dimethyl-2-oxo-1,2,3,4-tetrahydro-7-quinolinyl)-2-fluorobenzamide;
5-(2-amino-6-quinazolinyl)-N-(4-cyclohexylphenyl)-2-fluorobenzamide;
5-(2-amino-6-quinazolinyl)-2-fluoro-N-(4-(4-morpholinyl)phenyl)benzamide;
5-(2-amino-6-quinazolinyl)-N-(4-(1,1-dimethylethyl)phenyl)-2-fluorobenzamide;
3-(2-amino-6-quinazolinyl)-5-chloro-N-(4-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-chloro-N-cyclopropylbenzamide;
3-(2-amino-6-quinazolinyl)-5-chloro-N-(1-methylethyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-(4-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-(4-chloro-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-(3-methyl-4-(1-methylethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-(4-((trifluoromethyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-(3-chloro-4-methylphenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-cyclopropylbenzamide;
N-(3-(2-amino-6-quinazolinyl)phenyl)-5-(dimethylamino)-1-naphthalenesulfonamide;
N-(5-(2-amino-6-quinazolinyl)-2-methylphenyl)-3-(trifluoromethyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-methylphenyl)-4-(1,1-dimethylethyl)benzamide;
N-(5-(2-amino-6-quinazolinyl)-2-methylphenyl)-5-methyl-3-isoxazolecarboxamide;
N-(5-(2-amino-6-quinazolinyl)-2-methylphenyl)-3,4-difluorobenzamide;
N-(5-(2-amino-6-quinazolinyl)-2-methylphenyl)cyclopropanecarboxamide;
N-(3-(2-amino-6-quinazolinyl)-5-chlorophenyl)-3-(trifluoromethyl)benzamide;
N′
-(3-(2-amino-6-quinazolinyl)-5-chlorophenyl)-N,N-dimethylurea;
N-(3-(2-amino-6-quinazolinyl)-5-chlorophenyl)-4-(1,1-dimethylethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-5-chlorophenyl)-4-(dimethylamino)benzamide;
N-(3-(2-amino-6-quinazolinyl)-5-chlorophenyl)-3-((trifluoromethyl)oxy)benzamide;
N-(3-(2-amino-6-quinazolinyl)-5-chloro-4-methylphenyl)-4-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-5-chloro-4-methylphenyl)-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-5-chloro-4-methylphenyl)-3-chlorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-5-chloro-4-methylphenyl)-4-chlorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-5-chloro-4-methylphenyl)-4-(methyloxy)-3-(trifluoromethyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-cyclopropyl-4-(methyloxy)benzamide;
3-(2-amino-6-quinazolinyl)-2-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(1-methylethyl)benzamide;
ethyl 7-(2-methyl-5-(((3-(trifluoromethyl)phenyl)amino)carbonyl)phenyl)-3-isoquinolinecarboxylate;
3-(2-amino-6-quinazolinyl)-N-(2-(dimethylamino)ethyl)-4-methylbenzamide;
7-(2-methyl-5-(((3-(trifluoromethyl)phenyl)amino)carbonyl)phenyl)-3-isoquinolinecarboxylic acid;
N-(2-(dimethylamino)ethyl)-7-(2-methyl-5-(((3-(trifluoromethyl)phenyl)amino)carbonyl)phenyl)-3-isoquinolinecarboxamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(1-methylpropyl)benzamide;
ethyl 7-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-3-isoquinolinecarboxylate;
7-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-3-isoquinolinecarboxylic acid;
N-cyclobutyl-4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
7-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-N-(2-(dimethylamino)ethyl)-3-isoquinolinecarboxamide;
3-(2-aminopyrido[2,3-d]pyrimidin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-phenylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-ethynylphenyl)-4-methylbenzamide;
N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-((((2S)-1-methyl-2-pyrrolidinyl)methyl)oxy)-5-(trifluoromethyl)phenyl)benzamide;
N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-3-(2-(((ethylamino)carbonyl)amino)-6-quinazolinyl)-4-methylbenzamide;
3-(2-(((ethylamino)carbonyl)amino)-6-quinazolinyl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-((1-methylethyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-(ethyloxy)phenyl)-4-methylbenzamide;
3-(2-(dimethylamino)-6-quinazolinyl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-(dimethylamino)-6-quinazolinyl)-4-methyl-N-(4-(trifluoromethyl)phenyl)benzamide;
2-fluoro-5-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-fluoro-5-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-2-(methyloxy)phenyl)-4-methylbenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2,5-bis(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2-fluoro-4-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-1-methyl-1H-indole-2-carboxamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2,4-bis(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2,3-difluorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3,5-bis(1,1-dimethylethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3,5-bis(methyloxy)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3,4-dimethylbenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2-chloro-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2,3-dimethylbenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-4-chloro-2-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-(methyloxy)phenyl)-1-methyl-1H-indole-2-carboxamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2-chloro-3-methylbenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2-chloro-3-fluorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-(methyloxy)phenyl)-2-fluoro-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3-chloro-2,4-difluorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2,3-difluoro-4-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-2,3-difluoro-4-methylbenzamide;
N-(3-(2-amino-6-quinazolinyl)phenyl)-2-fluoro-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)phenyl)-2,3-dichlorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-fluorophenyl)-2-fluoro-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-fluorophenyl)-2,3-dichlorobenzamide;
N-(3-(2-amino-6-quinazolinyl)-4-chlorophenyl)-2-fluoro-3-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-chlorophenyl)-2,3-dichlorobenzamide;
3-(2-amino-6-quinazolinyl)-4-fluoro-N-(2-fluoro-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-fluoro-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-2-(methyloxy)phenyl)-4-fluorobenzamide;
3-(2-amino-6-quinazolinyl)-4-chloro-N-(5-(1,1-dimethylethyl)-2-(methyloxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-chloro-N-(2-fluoro-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-chloro-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-chloro-N-(3-((trifluoromethyl)oxy)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(4-(phenyloxy)phenyl)benzamide;
3-(4-(((1E)-(dimethylamino)methylidene)amino)-6-quinazolinyl)-4-methyl-N-(4-(phenyloxy)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-phenylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(3-bromophenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(4-(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(4-(4-morpholinyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(2-((4-methyl-1-piperazinyl)methyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(2-(4-morpholinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-N-(2-(dimethylamino)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(2-(1-pyrrolidinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-N-(2-fluoro-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-5-(trifluoromethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-cyclopentyl-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(2,3-dimethylphenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(2,5-bis(methyloxy)phenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(cyclopropylmethyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(3-((1-methylethyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3,4-dimethyl-5-isoxazolyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(3-(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-3-isoxazolyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(3,4-bis(methyloxy)-5-((3-(4-methyl-1-piperazinyl)propyl)oxy)phenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(3-((trifluoromethyl)oxy)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-N-(4,5-dimethyl-3-isoxazolyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(phenylmethyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(2-methyl-5-(1-methylethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(3-((phenylmethyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-pyridinylmethyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-pyridinylmethyl)benzamide;
3-(4-amino-6-quinazolinyl)-N-(1,1′
-biphenyl-3-yl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-2-(methyloxy)phenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-3-isoxazolyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(3-methyl-5-isoxazolyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(3-((1,1,2,2-tetrafluoroethyl)oxy)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-N-(5-cyclohexyl-2-(methyloxy)phenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-N-(3,5-bis(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-methyl-5-isoxazolyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-((2S)-tetrahydro-2-furanylmethyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3,5-bis(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-chloro-5-(trifluoromethyl)-3-pyridinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(1,3-thiazol-2-yl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-bromo-2-pyridinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(6-(4-morpholinyl)-3-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-quinolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(6-quinolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-chloro-4-pyridinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-naphthalenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4,5-dihydro-1,3-thiazol-2-yl)-4-methylbenzamide;
S-(4,5-dihydro-1,3-thiazol-2-yl)3-(2-amino-6-quinazolinyl)-4-methylbenzenecarbothioate;
3-(2-amino-6-quinazolinyl)-N-(5-ethyl-1,3,4-thiadiazol-2-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-methyl-2-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-ethyl-2-pyridinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-methyl-1,3-thiazol-2-yl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-chloro-1,3-benzoxazol-2-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(3-pyridinyl)ethyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(5-methyl-3-isothiazolyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(trifluoromethyl)-2-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3,5-dichloro-2-pyridinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-3-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4,5-dimethyl-1,3-thiazol-2-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-methyl-1,3-benzothiazol-2-yl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(6-(ethyloxy)-1,3-benzothiazol-2-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(5-nitro-1,3-thiazol-2-yl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(6-fluoro-1,3-benzothiazol-2-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(4-(1,1-dimethylethyl)-1,3-thiazol-2-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(5-iodo-2-pyridinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(1-methyl-1H-benzimidazol-2-yl)benzamide;
N-(2-acetyl-3-thienyl)-3-(2-amino-6-quinazolinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(5-bromo-1,3-thiazol-2-yl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-((6-(trifluoromethyl)-3-pyridinyl)methyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-((phenylmethyl)oxy)-2-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-fluoro-4-(1-pyrrolidinyl)-3-(1-pyrrolidinylcarbonyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(6-(trifluoromethyl)-2-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(5-(trifluoromethyl)-2-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-hydroxy-2-pyridinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2,4-difluorophenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-((3-(1-piperidinyl)propyl)oxy)-2-pyridinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-cyanophenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(3-((2-(diethylamino)ethyl)oxy)-2-pyridinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(methyloxy)-1,1′
-biphenyl-3-yl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-methyl-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-chloro-2-(methyloxy)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)oxy)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-5-((phenylamino)carbonyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methylsulfanyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-fluoro-5-methylphenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2,5-bis(methyloxy)phenyl)-4-methylbenzamide;
5-(2-amino-6-quinazolinyl)-2-chloro-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-fluoro-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-(4-(1,1-dimethylethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3,5-bis(methyloxy)phenyl)-5-bromobenzamide;
3-(2-amino-6-quinazolinyl)-5-bromo-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-5-chloro-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-chloro-N-(2-(1-pyrrolidinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-chloro-N-(2-(1-piperidinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-chloro-N-(2-(4-morpholinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(3-(1-methylethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-N-(3-(1-methylethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(2-(methyl((3S)-1-methyl-3-pyrrolidinyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
3-(4-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(4-amino-6-quinazolinyl)-4-methyl-N-(2-(1-piperidinyl)-5-(trifluoromethyl)phenyl)benzamide;
N-(3-(4-amino-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
N-(3-(4-amino-6-quinazolinyl)phenyl)benzamide;
N-(3-(4-amino-6-quinazolinyl)phenyl)-3-(methyloxy)benzamide;
N-(3-(4-amino-6-quinazolinyl)phenyl)-4-(trifluoromethyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-5-(trifluoromethyl)phenyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(2-(methyloxy)-5-(trifluoromethyl)phenyl)-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-3-(2-((2-(dimethylamino)ethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
1,1-dimethylethyl 2-(((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)methyl)-1-piperidinecarboxylate;
N-cyclopropyl-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-(4-methyl-1-piperazinyl)-6-quinazolinyl)benzamide;
1,1-dimethylethyl 4-(2-((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)ethyl)-1-piperazinecarboxylate;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(2,3-dihydro-1H-inden-4-yl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-3-(trifluoromethyl)benzamide;
N-(4-chloro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(3-methyl-4-(1-methylethyl)phenyl)benzamide;
N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-3,5-bis(trifluoromethyl)benzamide;
2,3-dichloro-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)benzamide;
2-fluoro-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-3-(trifluoromethyl)benzamide;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
2-fluoro-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-5-(trifluoromethyl)benzamide;
4-(1,1-dimethylethyl)-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(4-(trifluoromethyl)phenyl)benzamide;
N-(4-(1,1-dimethylethyl)phenyl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
N-(3-(1,1-dimethylethyl)phenyl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-2,4-bis(trifluoromethyl)benzamide;
N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-2,3-dihydro-1-benzofuran-7-carboxamide;
3-chloro-2-fluoro-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)benzamide;
3-fluoro-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-2-(trifluoromethyl)benzamide;
2-chloro-3-fluoro-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)benzamide;
2-chloro-3-methyl-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)benzamide;
2,3-difluoro-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-4-(trifluoromethyl)benzamide;
2,3-difluoro-4-methyl-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(3-((trifluoromethyl)oxy)phenyl)benzamide;
2-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzamide;
2-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
N-(2,3-dichlorophenyl)-2-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
2-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(4-(methyloxy)-3-(trifluoromethyl)phenyl)benzamide;
2-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(3-((trifluoromethyl)oxy)phenyl)benzamide;
N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-4-(trifluoromethyl)benzamide;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(4-(methyloxy)-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(2-pyridinylmethyl)benzamide;
N-(2-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-3-(trifluoromethyl)benzamide;
2,2-difluoro-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-1,3-benzodioxole-4-carboxamide;
N-(5-(1,1-dimethylethyl)-2-(methyloxy)phenyl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-((((2-(4-morpholinyl)ethyl)amino)carbonyl)amino)-3-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-((((2-(diethylamino)ethyl)amino)carbonyl)amino)-3-(trifluoromethyl)phenyl)-4-methylbenzamide;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(4-((((2-(4-morpholinyl)ethyl)amino)carbonyl)amino)-3-(trifluoromethyl)phenyl)benzamide;
N-(4-((((2-(diethylamino)ethyl)amino)carbonyl)amino)-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-(((2-(4-morpholinyl)ethyl)amino)carbonyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-N-(3-(((2-(4-morpholinyl)ethyl)amino)carbonyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-(((2-(diethylamino)ethyl)amino)carbonyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
N-(3-(((2-(diethylamino)ethyl)amino)carbonyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
N-(5-((diethylamino)sulfonyl)-2-(methyloxy)phenyl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)-3,4,5-tris(methyloxy)benzamide;
N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-3,4,5-tris(methyloxy)benzamide;
3-fluoro-N-(4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-5-(trifluoromethyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-((4-methyl-1-piperazinyl)carbonyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-((4-methyl-1-piperazinyl)methyl)-5-(trifluoromethyl)phenyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-2-methylphenyl)-3-(trifluoromethyl)benzamide;
N-(5-(1,1-dimethylethyl)-2-((4-morpholinylacetyl)amino)phenyl)-4-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-2-((4-morpholinylacetyl)amino)phenyl)-4-methylbenzamide;
N-(3-(2-amino-6-quinazolinyl)-2-methylphenyl)-3-fluoro-5-(trifluoromethyl)benzamide;
3-fluoro-N-(2-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-5-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-2-methylphenyl)-3,5-bis(trifluoromethyl)benzamide;
N-(2-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-3,5-bis(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-2-methylphenyl)-2-fluoro-5-(trifluoromethyl)benzamide;
2-fluoro-N-(2-methyl-3-(2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)-5-(trifluoromethyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-2,4,6-trimethylphenyl)-3-(trifluoromethyl)benzamide;
4-((3-(2-amino-6-quinazolinyl)-4-methylphenyl)carbonyl)-6-(1,1-dimethylethyl)-3,4-dihydro-2(1H)-quinoxalinone;
N-(4-(2-amino-6-quinazolinyl)phenyl)-N′
-phenylurea;
N-(4-(4-amino-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
N-(4-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
4-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(4-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
4-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(4-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
4-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
N-cyclopropyl-4-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)benzamide;
4-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)-N-phenylbenzamide;
N-(4-chlorophenyl)-4-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)benzamide;
N-(4-(2-(methylamino)-6-quinazolinyl)phenyl)-2-(phenylamino)benzamide;
N-(4-(4-amino-6-quinazolinyl)phenyl)-2-(phenylamino)benzamide;
6-methyl-5-(2-(methylamino)-6-quinazolinyl)-1(2H)-isoquinolinone;
2′
,7′
-dimethyl-2-(methylamino)-6,8′
-biquinazolin-4′
(3′
H)-one;
2-fluoro-4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-((1-methylethyl)oxy)phenyl)benzamide;
3-fluoro-4-methyl-2-(2-(methylamino)-6-quinazolinyl)-N-(3-((1-methylethyl)oxy)phenyl)benzamide;
2-fluoro-4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-((1-methylethyl)oxy)phenyl)benzenecarbothioamide;
2-fluoro-4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(4-(methyloxy)-3-(trifluoromethyl)phenyl)benzamide;
2-amino-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzoic acid;
2-amino-4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-((1-methylethyl)oxy)phenyl)benzamide;
2-amino-4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-(1-methylethyl)phenyl)benzamide;
2-amino-N-(4-(1,1-dimethylethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-Methyl-3-(quinazolin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzamide hydrochloride;
3-(2-amino-6-quinazolinyl)-N-(3-((3-(dimethylamino)propyl)oxy)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
6-(5-isothiocyanato-2-methylphenyl)-N-methyl-2-quinazolinamine;
6-(2-phenylimidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-(4-(methyloxy)phenyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-(3-(methyloxy)phenyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-(2-(methyloxy)phenyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-(1,3-benzodioxol-5-yl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-(3-thienyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-ethyl-1-benzofuran-5-yl)-2-quinazolinamine;
6-(2-(1,1-dimethylethyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
3-(2-amino-6-quinazolinyl)-N-(3-(3-(dimethylamino)propyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
N-(4-(diethylnitroryl)-1-methylbutyl)-6-(4-methyl-3-pyridinyl)-2-quinazolinamine;
methyl 4-methyl-3-(6-quinazolinyl)benzoate;
4-methyl-3-(6-quinazolinyl)benzoic acid;
N-cyclopropyl-4-methyl-3-(2-((((2R)-1-(2,2,2-trifluoroethyl)-2-pyrrolidinyl)methyl)amino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(3-((N,N-diethylglycyl)amino)-4-(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(4-(1,1-dimethylethyl)-3-((1-pyrrolidinylacetyl)amino)phenyl)-4-methylbenzamide;
N-(1-(N,N-diethylglycyl)-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-(cyclopropylamino)-6-quinazolinyl)-N-(1-(N,N-diethylglycyl)-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methylbenzamide;
N-(3-((N,N-diethylglycyl)amino)-4-(1-piperidinyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(4-chloro-3-(((1-methyl-4-piperidinyl)methyl)oxy)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(3-fluoro-4-((3-(1-piperidinyl)propyl)oxy)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(3-((N,N-diethylglycyl)amino)-4-methylphenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(3-((N,N-diethylglycyl)amino)-4-fluorophenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(2-((diethylamino)methyl)-4,5-bis(methyloxy)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(2-((diethylamino)methyl)-4,5-bis(methyloxy)phenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(3-fluoro-4-(((1-methyl-3-piperidinyl)methyl)oxy)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-(((methylsulfonyl)amino)methyl)phenyl)benzamide;
4-methyl-N-(3-(((methylsulfonyl)amino)methyl)phenyl)-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(4-fluoro-3-(((methyloxy)acetyl)amino)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-N-(4-fluoro-3-(((methyloxy)acetyl)amino)phenyl)-4-methylbenzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-((4-methyl-1-piperazinyl)methyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-((((2S)-1-methyl-2-pyrrolidinyl)methyl)oxy)-4-(pentafluoroethyl)phenyl)benzamide;
N-(4-chloro-3-((((2S)-1-methyl-2-pyrrolidinyl)methyl)oxy)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
ethyl 3,3-dimethyl-6-(((4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)carbonyl)amino)-2,3-dihydro-1H-indole-1-carboxylate;
N-(3-((diethylamino)methyl)-4-(methyloxy)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
ethyl 6-(((3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methylphenyl)carbonyl)amino)-3,3-dimethyl-2,3-dihydro-1H-indole-1-carboxylate;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-(2-oxo-1-pyrrolidinyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(1-piperidinyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(1-methyl-4-piperidinyl)benzamide;
N-(2-((2,2-dimethylpropanoyl)amino)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(methyl(1-methyl-4-piperidinyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-(2-methyl-1-pyrrolidinyl)-2-pyridinyl)benzamide;
N-(2,2-difluoro-1,3-benzodioxol-4-yl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2,2-difluoro-1,3-benzodioxol-4-yl)-4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
N-(2,2-difluoro-1,3-benzodioxol-4-yl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2-((3-(dimethylamino)propyl)oxy)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-((3-(methyloxy)propyl)amino)-6-quinazolinyl)-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-(phenylamino)-6-quinazolinyl)benzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methyl-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-3-(2-(((1-ethyl-4-piperidinyl)methyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-3-(2-(cyclopropylamino)-6-quinazolinyl)-4-methylbenzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methyl-3-(2-((3-(2-oxo-1-pyrrolidinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-(methyl(3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
2-fluoro-N-(2-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-5-(trifluoromethyl)benzamide;
4-methyl-3-(2-((1E)-3-(methyloxy)-1-propenyl)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-((1E)-3-(methyloxy)-1-propenyl)-6-quinazolinyl)-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
6-(2,6-dichlorophenyl)-N-(3-(4-morpholinyl)propyl)-2-quinazolinamine;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-(cyclopropylamino)-6-quinazolinyl)-4-methylbenzamide;
4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methylbenzamide;
3-(2-((3-fluoro-4-((4-(1H-imidazol-1-yl)butyl)oxy)phenyl)amino)-6-quinazolinyl)-4-methylbenzamide;
4-methyl-3-(2-((4-((3-(1-piperidinyl)propyl)oxy)phenyl)amino)-6-quinazolinyl)benzamide;
6-(2,6-dimethylphenyl)-N-(3-morpholinopropyl)quinazolin-2-amine;
N-(2-fluoro-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2-fluoro-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2-fluoro-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2-fluoro-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-((2-(1-(phenylmethyl)-4-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
1,1-dimethylethyl 4-(2-((6-(2-methyl-5-(((2-methyl-3-(trifluoromethyl)phenyl)amino)carbonyl)phenyl)-2-quinazolinyl)amino)ethyl)-1-piperazinecarboxylate;
3-(2-((((2R)-1-ethyl-2-pyrrolidinyl)methyl)amino)-6-quinazolinyl)-4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
3-(2-(1,3-benzoxazol-2-ylamino)-6-quinazolinyl)-4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-((2-(1-piperazinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(4-chloro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(3-methyl-4-(1-methylethyl)phenyl)-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(4-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(4-chloro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
N-(4-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(3-methyl-4-(1-methylethyl)phenyl)-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
N-(4-chloro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(4-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(3-methyl-4-(1-methylethyl)phenyl)-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(1-acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-((4-((3-(1-piperidinyl)propyl)oxy)phenyl)amino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-((3-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
N-(2-fluoro-3-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2,3-dihydro-1H-inden-4-yl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-N-(2,3-dihydro-1H-inden-4-yl)-4-methylbenzamide;
N-(2,3-dihydro-1H-inden-4-yl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(2,3-dihydro-1H-inden-4-yl)-4-methyl-3-(2-((4-((3-(1-piperidinyl)propyl)oxy)phenyl)amino)-6-quinazolinyl)benzamide;
3-(2-(((1S)-4-(diethylamino)-1-methylbutyl)amino)-6-quinazolinyl)-4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
6-(5-amino-2-methylphenyl)-N-(4-(4-methyl-1-piperazinyl)phenyl)-2-quinazolinamine;
2-methyl-N-(4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
4-(1,1-dimethylethyl)-N-(4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)benzamide;
N-(4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)acetamide;
N-(4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)-3,5-bis(methyloxy)benzamide;
2-fluoro-N-(4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
2,2-difluoro-N-(4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)-1,3-benzodioxole-5-carboxamide;
N-(4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)-1-naphthalenecarboxamide;
3-(1,1-dimethylethyl)-1-methyl-N-(4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)-1H-pyrazole-4-carboxamide;
6-(5-(1H-benzimidazol-2-ylamino)-2-methylphenyl)-N-(4-(4-methyl-1-piperazinyl)phenyl)-2-quinazolinamine;
N-(4-(4-methyl-1-piperazinyl)phenyl)-6-(2-methyl-5-((5-(trifluoromethyl)-1H-benzimidazol-2-yl)amino)phenyl)-2-quinazolinamine;
N-(2-(2-(dimethylamino)ethyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-ethyl-N′
-(4-methyl-3-(2-((4-(4-methyl-1-piperazinyl)phenyl)amino)-6-quinazolinyl)phenyl)urea;
3-(2-((3-hydroxypropyl)amino)-6-quinazolinyl)-4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-N-(2-methyl-3-(trifluoromethyl)phenyl)-3-(2-(3-pyridinylamino)-6-quinazolinyl)benzamide;
N-methyl-6-(2-methyl-5-((5-(trifluoromethyl)-1H-benzimidazol-2-yl)amino)phenyl)-2-quinazolinamine;
6-(5-(1H-benzimidazol-2-ylamino)-2-methylphenyl)-N-methyl-2-quinazolinamine;
6-(5-((1-(2-(dimethylamino)ethyl)-1H-benzimidazol-2-yl)amino)-2-methylphenyl)-N-methyl-2-quinazolinamine;
6-(5-((1-(3-(dimethylamino)propyl)-1H-benzimidazol-2-yl)amino)-2-methylphenyl)-N-methyl-2-quinazolinamine;
6-(5-((7-chloro-5-(trifluoromethyl)-1H-benzimidazol-2-yl)amino)-2-methylphenyl)-N-methyl-2-quinazolinamine;
6-(5-(1H-imidazo[4,5-b]pyridin-2-ylamino)-2-methylphenyl)-N-methyl-2-quinazolinamine;
N-methyl-6-(2-methyl-5-((1-methyl-5-(trifluoromethyl)-1H-benzimidazol-2-yl)amino)phenyl)-2-quinazolinamine;
6-(5-((5,6-difluoro-1H-benzimidazol-2-yl)amino)-2-methylphenyl)-N-methyl-2-quinazolinamine;
N-methyl-6-(2-methyl-5-((6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl)amino)phenyl)-2-quinazolinamine;
N-methyl-6-(6-methyl-5-phthalazinyl)-2-quinazolinamine;
6-methyl-5-(2-(methylamino)-6-quinazolinyl)-1-phthalazinol;
N-(4-chloro-3-(2-(methylamino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
N-(4-chloro-3-(2-(methylamino)-6-quinazolinyl)phenyl)-2-fluoro-5-(trifluoromethyl)benzamide;
N-(4-chloro-3-(2-(methylamino)-6-quinazolinyl)phenyl)-2-methyl-3-(trifluoromethyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2,6-dimethylphenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(ethyloxy)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-5-(trifluoromethyl)phenyl)benzamide d—
3_;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-methyl-5-nitrophenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2,5-dimethylphenyl)-4-methylbenzamide;
N-(5-(aminocarbonyl)-2-methylphenyl)-3-(2-amino-6-quinazolinyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-5-nitrophenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-cyclohexyl-2-(methyloxy)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-methyl-5-(methyloxy)phenyl)benzamide;
4-(2-amino-6-quinazolinyl)-N-(2-fluoro-5-(trifluoromethyl)phenyl)-3-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-5-((2-pyridinylamino)carbonyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-5-((3-pyridinylamino)carbonyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(methyloxy)-5-((4-pyridinylamino)carbonyl)phenyl)benzamide;
4-(2-amino-6-quinazolinyl)-3-methyl-N-(3-((4-methyl-1-piperazinyl)methyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-((2-(1-pyrrolidinyl)ethyl)oxy)-5-(trifluoromethyl)phenyl)benzamide;
N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-2-((2-(1-pyrrolidinyl)ethyl)amino)-5-(trifluoromethyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-chloro-4-(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-chloro-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-bromo-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(4-(1-methylethyl)-2-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-(1,1-dimethylethyl)imidazo[1,2-a]pyridin-6-yl)-4-methylbenzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(4-((1-methyl-4-piperidinyl)oxy)phenyl)benzamide;
3-(2-(cyclopropylamino)-6-quinazolinyl)-4-methyl-N-(4-((1-methyl-4-piperidinyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(3-methyl-4-((1-methyl-4-piperidinyl)oxy)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-methyl-4-((1-methyl-4-piperidinyl)oxy)phenyl)benzamide;
3-(2-(cyclopropylamino)-6-quinazolinyl)-4-methyl-N-(3-methyl-4-((1-methyl-4-piperidinyl)oxy)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-((1-cyclopropylethyl)oxy)phenyl)-4-methylbenzamide;
N-(4-((1-cyclopropylethyl)oxy)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(4-((1-cyclopropylethyl)oxy)-3-methylphenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(4-((1-cyclopropylethyl)oxy)-3-methylphenyl)-4-methylbenzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(4-(1-methylethyl)phenyl)benzamide;
3-(2-(cyclopropylamino)-6-quinazolinyl)-4-methyl-N-(4-(1-methylethyl)phenyl)benzamide;
4-methyl-N-(4-(1-methylethyl)phenyl)-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-((1-methyl-4-piperidinyl)oxy)-5-(trifluoromethyl)phenyl)benzamide;
N-(4-((cyclopropylmethyl)oxy)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(4-((cyclopropylmethyl)oxy)phenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(3-(acetylamino)-4-fluorophenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2-(((1R)-1-cyclopropylethyl)oxy)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(3-(acetylamino)-4-(((1S)-1-cyclopropylethyl)oxy)phenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2-(((1R)-1-cyclopropylethyl)oxy)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-methyl-N-(4-(1-methylethyl)phenyl)-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2-(1,1-dimethylethyl)imidazo[1,2-a]pyridin-6-yl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2-(1,1-dimethylethyl)imidazo[1,2-a]pyridin-6-yl)-4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-N-(2-(1,1-dimethylethyl)imidazo[1,2-a]pyridin-6-yl)-4-methylbenzamide;
N-(2-(1,1-dimethylethyl)imidazo[1,2-a]pyridin-6-yl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-methyl-N-(2-(1-methylethyl)-1H-benzimidazol-6-yl)-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(2-(1-methylethyl)-1H-benzimidazol-6-yl)benzamide;
4-methyl-N-(2-(1-methylethyl)-1H-benzimidazol-6-yl)-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(1-methylethyl)-1H-benzimidazol-6-yl)benzamide;
N-(2-((2-(diethylamino)ethyl)oxy)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(1-acetyl-2,3-dihydro-1H-indol-5-yl)-4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
N-(1-acetyl-2,3-dihydro-1H-indol-5-yl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-((2-(4-morpholinyl)ethyl)oxy)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)-N-(2-((2-(4-morpholinyl)ethyl)oxy)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-N-(2-((2-(4-morpholinyl)ethyl)oxy)-5-(trifluoromethyl)phenyl)-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-methyl-6-(2-methyl-5-(5-(trifluoromethyl)-1,3-benzoxazol-2-yl)phenyl)-2-quinazolinamine;
N-(2-(1-ethylpyrrolidin-3-yloxy)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)quinazolin-6-yl)benzamide;
N-(2-(((3S)-1-ethyl-3-piperidinyl)oxy)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-methyl-N-(2-((1-methyl-4-piperidinyl)oxy)-5-(trifluoromethyl)phenyl)-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(2-((1-methyl-4-piperidinyl)oxy)-5-(trifluoromethyl)phenyl)-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-2-((1-methyl-4-piperidinyl)oxy)-5-(trifluoromethyl)benzamide;
2-(((3R)-1-ethyl-3-piperidinyl)oxy)-N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-5-(trifluoromethyl)benzamide;
2-((cyclopentylmethyl)oxy)-N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-5-(trifluoromethyl)benzamide;
2-((cyclopropylmethyl)oxy)-N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-5-(trifluoromethyl)benzamide;
2-((cyclobutylmethyl)oxy)-N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-5-(trifluoromethyl)benzamide;
N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-2-((2-(4-morpholinyl)ethyl)oxy)-5-(trifluoromethyl)benzamide;
2-((2-(diethylamino)ethyl)oxy)-N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-5-(trifluoromethyl)benzamide;
2-(((1S)-1-cyclopentylethyl)oxy)-N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-5-(trifluoromethyl)benzamide;
N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-2-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)benzamide;
5-methyl-N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-2-(methyloxy)benzamide;
N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-2-((1-methyl-4-piperidinyl)amino)-5-(trifluoromethyl)benzamide;
5-fluoro-N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-2-(methyloxy)benzamide;
6-(1,6-dimethyl-1H-indazol-7-yl)-N-methyl-2-quinazolinamine;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(6-(trifluoromethyl)-1,3-benzothiazol-2-yl)benzamide;
4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)-N-(6-(trifluoromethyl)-1,3-benzothiazol-2-yl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(6-((trifluoromethyl)oxy)-1,3-benzothiazol-2-yl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(5-(trifluoromethyl)-1,3-benzothiazol-2-yl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-2-((1-pyrrolidinylacetyl)amino)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-2-((2-(1-piperidinyl)ethyl)oxy)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(5-(1,1-dimethylethyl)-2-((1-piperidinylacetyl)amino)phenyl)-4-methylbenzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((N,N-diethylglycyl)amino)-5-(1,1-dimethylethyl)phenyl)-4-methylbenzamide;
3-(trifluoromethyl)-N-(2,4,6-trimethyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)phenyl)benzamide;
6-(2,6-dichlorophenyl)-2-quinazolinamine;
N˜
1˜
-(6-(2,6-dimethylphenyl)-2-quinazolinyl)-N-4-,N-4-dimethyl-1,4-butanediamine;
6-(2-chloro-6-methylphenyl)-2-quinazolinamine;
N˜
1˜
-(6-(2,6-dichlorophenyl)-2-quinazolinyl)-N-3-,N-3-diethyl-1,3-propanediamine;
N˜
1˜
-(6-(2,6-dimethylphenyl)-2-quinazolinyl)-N-3-,N-3-diethyl-1,3-propanediamine;
6-(2,6-dichlorophenyl)-N-(2-(1-piperidinyl)ethyl)-2-quinazolinamine;
4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
3-(2-((3-(dimethylamino)propyl)(methyl)amino)-6-quinazolinyl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methyl(2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)-N-(3-(trifluoromethyl)phenyl)benzamide;
N-(2-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
N˜
1˜
-(6-(2-chloro-6-methylphenyl)-2-quinazolinyl)-N-3-,N-3-diethyl-1,3-propanediamine;
N˜
1˜
-(6-(2-chloro-6-methylphenyl)-2-quinazolinyl)-N-2-,N-2-diethyl-1,2-ethanediamine;
6-(2-chloro-6-methylphenyl)-N-(3-(1-pyrrolidinyl)propyl)-2-quinazolinamine;
N˜
1˜
,N˜
1-diethyl-N-3-(6-(2-ethyl-6-methylphenyl)-2-quinazolinyl)-1,3-propanediamine;
N˜
1˜
-(6-(5-amino-2-methylphenyl)-2-quinazolinyl)-N-3-,N-3-diethyl-1,3-propanediamine;
N-(3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-2-methylphenyl)-3,5-bis(trifluoromethyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)pyrido[2,3-d]pyrimidin-6-yl)-4-methyl-N-(4-(trifluoromethyl)phenyl)benzamide;
3-fluoro-N-(2-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-5-(trifluoromethyl)benzamide;
N-(3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methylphenyl)-2-fluoro-5-(trifluoromethyl)benzamide;
N-(3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methylphenyl)-3-fluoro-5-(trifluoromethyl)benzamide;
N-(2-((N,N-diethylglycyl)amino)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((N,N-diethylglycyl)amino)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(3-((trifluoromethyl)oxy)phenyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(3-((trifluoromethyl)oxy)phenyl)benzamide;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)acetamide;
N-(4-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)acetamide;
N-(3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methylphenyl)acetamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(5-methyl-2-((4-morpholinylacetyl)amino)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(5-methyl-2-((4-morpholinylacetyl)amino)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(5-methyl-2-((1-pyrrolidinylacetyl)amino)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(5-methyl-2-((1-pyrrolidinylacetyl)amino)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(5-methyl-2-((1-piperidinylacetyl)amino)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(5-methyl-2-((1-piperidinylacetyl)amino)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((N,N-diethylglycyl)amino)-5-methylphenyl)-4-methylbenzamide;
N-(2-((N,N-diethylglycyl)amino)-5-methylphenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(2-methyl-3-(2-((3-(1-piperidinyl)propyl)amino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
N-(3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-2-methylphenyl)-3-(trifluoromethyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(1-pyrrolidinylcarbonyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(1-pyrrolidinylcarbonyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)-N-(2-(1-pyrrolidinylcarbonyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-(1-pyrrolidinylmethyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(1-pyrrolidinylmethyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)-N-(2-(1-pyrrolidinylmethyl)-5-(trifluoromethyl)phenyl)benzamide;
N-(2-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-3-((1,1,2,2-tetrafluoroethyl)oxy)benzamide;
N-(2-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)phenyl)-3-((1,1,2,2-tetrafluoroethyl)oxy)benzamide;
N-(2-(3,3-dimethyl-2-oxo-1-azetidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(2-(3,3-dimethyl-2-oxo-1-azetidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-methyl-6-(2-methyl-5-(6-(trifluoromethyl)-1H-benzimidazol-2-yl)phenyl)-2-quinazolinamine;
N-(2-methyl-3-(2-(methylamino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
N-(2-(acetylamino)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2-(acetylamino)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((3-(1-piperidinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2-(acetylamino)-5-(trifluoromethyl)phenyl)-3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-(4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)phenyl)-3-(trifluoromethyl)benzamide;
methyl 4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzoate;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(((methyloxy)acetyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
methyl 4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzoate;
4-methyl-N-(2-(((methyloxy)acetyl)amino)-5-(trifluoromethyl)phenyl)-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
6-(5-(4-chloro-6-(trifluoromethyl)-1H-benzimidazol-2-yl)-2-methylphenyl)-N-methyl-2-quinazolinamine;
6-(5-(4,6-bis(trifluoromethyl)-1H-benzimidazol-2-yl)-2-methylphenyl)-N-methyl-2-quinazolinamine;
N-(2-(3,3-dimethyl-2-oxo-1-azetidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-N-(2-(3,3-dimethyl-2-oxo-1-azetidinyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
N-(2-(3,3-dimethyl-2-oxo-1-azetidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((3-(1-piperidinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2-(acetylamino)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-((((2-(4-morpholinyl)ethyl)amino)carbonyl)amino)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(4-(2-oxo-1-azetidinyl)-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(4-(2-oxo-1-pyrrolidinyl)-3-(trifluoromethyl)phenyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(4-(2-oxo-1-azetidinyl)-3-(trifluoromethyl)phenyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(4-(2-oxo-1-pyrrolidinyl)-3-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(2-oxo-1-pyrrolidinyl)-5-(trifluoromethyl)phenyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(2-(2-oxo-1-pyrrolidinyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(2-oxo-1-azetidinyl)-5-(trifluoromethyl)phenyl)benzamide;
N-(2-(3-(1,1-dimethylethyl)-2-oxo-1-imidazolidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(5-(trifluoromethyl)-2-(3,4,4-trimethyl-2,5-dioxo-1-imidazolidinyl)phenyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(5-(trifluoromethyl)-2-(3,4,4-trimethyl-2,5-dioxo-1-imidazolidinyl)phenyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-N-(2-(3-(1,1-dimethylethyl)-2-oxo-1-imidazolidinyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(2-(2-oxo-1-azetidinyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-N-(2-(2-oxo-1-azetidinyl)-5-(trifluoromethyl)phenyl)-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2-(3-(1,1-dimethylethyl)-2-oxo-1-imidazolidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)-N-(5-(trifluoromethyl)-2-(3,4,4-trimethyl-2,5-dioxo-1-imidazolidinyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(3-methyl-2-oxo-1-imidazolidinyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-N-(2-(3-methyl-2-oxo-1-imidazolidinyl)-5-(trifluoromethyl)phenyl)-3-(2-((1-methyl-4-piperidinyl)amino)-6-quinazolinyl)benzamide;
4-methyl-N-(2-(3-methyl-2-oxo-1-imidazolidinyl)-5-(trifluoromethyl)phenyl)-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
3-(2-((3-(diethylamino)propyl)amino)-6-quinazolinyl)-4-methyl-N-(2-(3-methyl-2-oxo-1-imidazolidinyl)-5-(trifluoromethyl)phenyl)benzamide;
N-(2-((4-(2-(dimethylamino)ethyl)phenyl)oxy)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
6-(5-(1H-benzimidazol-2-yl)-2-methylphenyl)-N-methyl-2-quinazolinamine;
6-(5-(1H-benzimidazol-2-yl)-2-methylphenyl)-N-(3-(4-morpholinyl)propyl)-2-quinazolinamine;
6-(2-methyl-5-(6-(trifluoromethyl)-1H-benzimidazol-2-yl)phenyl)-N-(3-(4-morpholinyl)propyl)-2-quinazolinamine;
N,N-diethyl-N′
-(6-(2-methyl-5-(6-(trifluoromethyl)-1H-benzimidazol-2-yl)phenyl)-2-quinazolinyl)-1,3-propanediamine;
6-(2-methyl-5-(6-(trifluoromethyl)-1H-benzimidazol-2-yl)phenyl)-N-(2-(1-pyrrolidinyl)ethyl)-2-quinazolinamine;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)-N-(2-(3-oxo-1-piperazinyl)-5-(trifluoromethyl)phenyl)benzamide;
N-(2-((3-(dimethylamino)phenyl)oxy)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)-N-(2-(3-oxo-1-piperazinyl)-5-(trifluoromethyl)phenyl)benzamide;
4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzoic acid;
N-(2-(1-azetidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-(methylamino)-6-quinazolinyl)benzamide;
N-(2-(1-azetidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-(2-(1-azetidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-(2-(1-azetidinyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(2-((2-(1-piperidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-(2-amino-6-quinazolinyl)-N-cyclopropyl-1H-indole-6-carboxamide;
5-(2-amino-6-quinazolinyl)-N-cyclopropyl-2-fluoro-4-methylbenzamide;
N-cyclopropyl-2-fluoro-4-methyl-5-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-2-((2-(4-morpholinyl)ethyl)amino)-5-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-(2-amino-6-quinazolinyl)-N-cyclopropyl-5-methyl-2-pyridinecarboxamide;
N-cyclopropyl-5-methyl-4-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)-2-pyridinecarboxamide;
N-cyclopropyl-5-methyl-4-(2-((3-((2R)-2-methyl-1-piperidinyl)propyl)amino)-6-quinazolinyl)-2-pyridinecarboxamide;
N-cyclopropyl-2-fluoro-4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
1,1-dimethylethyl 2-((6-(2-((cyclopropylamino)carbonyl)-5-methyl-4-pyridinyl)-2-quinazolinyl)amino)-2-methylpropylcarbamate;
4-(2-((2-amino-1,1-dimethylethyl)amino)-6-quinazolinyl)-N-cyclopropyl-5-methyl-2-pyridinecarboxamide;
N-cyclopropyl-4-(2-((2-(dimethylamino)-1,1-dimethylethyl)amino)-6-quinazolinyl)-5-methyl-2-pyridinecarboxamide;
N-cyclopropyl-3-(2-((2-((2,2-dimethylpropanoyl)amino)-1,1-dimethylethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-3-(2-((2-((2,2-dimethylpropanoyl)amino)-2-methylpropyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-4-(2-((1,1-dimethyl-2-((1-methylethyl)amino)ethyl)amino)-6-quinazolinyl)-5-methyl-2-pyridinecarboxamide;
N-cyclopropyl-3-(2-((2-(dimethylamino)-1,1-dimethylethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
1,1-dimethylethyl 2-((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)-2-methylpropyl(1-methylethyl)carbamate;
N-cyclopropyl-3-(2-((1,1-dimethyl-2-((1-methylethyl)amino)ethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-3-(2-((3-(dimethylamino)propyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-((3-(2-methyl-1-piperidinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((1-methyl-2-(methyloxy)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((3-((1-methylethyl)oxy)propyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-3-(2-((4-(diethylamino)-1-methylbutyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-((3-(1-pyrrolidinyl)propyl)amino)-6-quinazolinyl)benzamide;
3-(2-((2-amino-2-methylpropyl)amino)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
N-(6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-2-yl)-1,4-cyclohexanediamine;
N-cyclopropyl-4-methyl-3-(2-((tetrahydro-2-furanylmethyl)amino)pyrido[2,3-d]pyrimidin-6-yl)benzamide;
4-((6-(4-methyl-3-pyridinyl)-2-quinazolinyl)amino)cyclohexanol;
trans-4-((6-(2-methyl-3-pyridinyl)-2-quinazolinyl)amino)cyclohexanol;
trans-N-(6-(4-methyl-3-pyridinyl)-2-quinazolinyl)-1,4-cyclohexanediamine;
N-(trans-4-((6-(4-methyl-3-pyridinyl)-2-quinazolinyl)amino)cyclohexyl)acetamide;
N-(2-(1,1-dioxido-4-thiomorpholinyl)ethyl)-6-(4-methyl-3-pyridinyl)-2-quinazolinamine;
4-((6-(3-methyl-2-pyridinyl)-2-quinazolinyl)amino)cyclohexanol;
N˜
1˜
,N˜
1˜
-dimethyl-N-4-(6-(4-methyl-3-pyridinyl)-2-quinazolinyl)-1,4-cyclohexanediamine;
N˜
1˜
-(1-methylethyl)-N-4-(6-(4-methyl-3-pyridinyl)-2-quinazolinyl)-1,4-cyclohexanediamine;
6-(2-fluorophenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(4-fluorophenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(2-chlorophenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(2,3-difluorophenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(2,4-difluorophenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(2,5-difluorophenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(2,3-dimethylphenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(3,5-difluorophenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
N-(2-(2-pyridinyl)ethyl)-6-(2-(trifluoromethyl)phenyl)-2-quinazolinamine;
4-((6-(2,5-dimethylphenyl)-2-quinazolinyl)amino)cyclohexanol;
N-cyclopropyl-4-methyl-3-(2-((2-(2-pyridinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)-N-(1,3-thiazol-2-yl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((3-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-3-(2-((1,1-dimethyl-2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
3-(2-(((1S)-2-(3-(aminomethyl)phenyl)-1-methylethyl)amino)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-methyl-6-quinazolinyl)benzamide;
1,1-dimethylethyl(3-((2S)-2-((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)propyl)phenyl)methylcarbamate;
N-cyclopropyl-3-(2-(((1S)-2-(3-((dimethylamino)methyl)phenyl)-1-methylethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-((2-methyl-2-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
1,1-dimethylethyl((3-((2S)-2-((6-(5-((ethylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)propyl)phenyl)methyl)carbamate;
3-(2-(((1S)-2-(3-(aminomethyl)phenyl)-1-methylethyl)amino)-6-quinazolinyl)-N-ethyl-4-methylbenzamide;
3-(2-((2-(dimethylamino)ethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-3-(2-(((1S)-1-((dimethylamino)carbonyl)-2-methylpropyl)amino)-6-quinazolinyl)-4-methylbenzamide;
3-(2-((3-(dimethylamino)-2,2-dimethylpropyl)amino)-6-quinazolinyl)-4-methylbenzamide;
3-(2-((3-(dimethylamino)-2,2-dimethylpropyl)amino)-6-quinazolinyl)-N-ethyl-4-methylbenzamide;
4-methyl-3-(2-((2-methyl-2-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N,4-dimethyl-3-(2-((2-methyl-2-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-ethyl-4-methyl-3-(2-((2-methyl-2-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-3-(2-((2-(3,5-dimethyl-4-morpholinyl)ethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
4-methyl-3-(2-((2-methyl-2-(4-morpholinyl)propyl)amino)-6-quinazolinyl)benzoic acid;
N-cyclopropyl-4-methyl-3-(2-((2-((3S)-3-methyl-4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((2-(phenylamino)ethyl)amino)-6-quinazolinyl)benzamide;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-O-methyl-L-threonine;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-D-tryptophan;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-D-phenylalanine;
N-cyclopropyl-3-(2-(((1S)-1-(4-fluorophenyl)ethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)(tetrahydro-2H-pyran-4-yl)acetic acid;
N-cyclopropyl-4-methyl-3-(2-((2-(2-pyridinylamino)ethyl)amino)-6-quinazolinyl)benzamide;
3-(4-bromo-7-isoquinolinyl)-4-methylbenzamide;
3-(4-(2-chloro-4-fluorophenyl)-7-isoquinolinyl)-4-methylbenzamide;
4-methyl-3-(4-(4-morpholinyl)-7-isoquinolinyl)benzamide;
4-methyl-3-(4-(2-methyl-3-pyridinyl)-7-isoquinolinyl)benzamide;
3-(4-(4-(aminosulfonyl)-2-methylphenyl)-7-isoquinolinyl)-N-cyclopropyl-4-methylbenzamide;
6-(2-methylphenyl)-N-(3-(4-morpholinyl)propyl)-2-quinazolinamine;
N-(3-(1H-imidazol-1-yl)propyl)-6-(2-methylphenyl)-2-quinazolinamine;
6-(2-methylphenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
N-(6-(2-methylphenyl)-2-quinazolinyl)-1,4-cyclohexanediamine;
6-(2-methylphenyl)-N-(3-(2-methyl-1-piperidinyl)propyl)-2-quinazolinamine;
N-((1S)-2-(3-((1S)-1-aminoethyl)phenyl)-1-methylethyl)-6-(2-methylphenyl)-2-quinazolinamine;
N˜
1˜
,N˜
1˜
-diethyl-N-3-(6-(2-methylphenyl)-2-quinazolinyl)-1,3-propanediamine;
4-((6-(2-methylphenyl)-2-quinazolinyl)amino)cyclohexanol;
N-((1S)-2-(3-(1-amino-1-methylethyl)phenyl)-1-methylethyl)-6-(2-methylphenyl)-2-quinazolinamine;
N-((1S)-2-(3-(1-amino-1-methylethyl)phenyl)-1-methylethyl)-6-(4-methyl-3-thienyl)-2-quinazolinamine;
4-((6-(2-aminophenyl)-2-quinazolinyl)amino)cyclohexanol;
6-(2-methylphenyl)-N-(1-(phenylmethyl)-3-pyrrolidinyl)-2-quinazolinamine;
6-(2-methylphenyl)-N-(1-(phenylmethyl)-4-piperidinyl)-2-quinazolinamine;
1,1-dimethylethyl 2-(2-((6-(2-methylphenyl)-2-quinazolinyl)amino)ethyl)-1-piperidinecarboxylate;
6-(2-methylphenyl)-N-(2-(2-piperidinyl)ethyl)-2-quinazolinamine;
N-((1S)-2-(3-(1-amino-1-methylethyl)phenyl)-1-methylethyl)-6-(4-methyl-3-pyridinyl)-2-quinazolinamine;
6-(3-methyl-2-pyridinyl)-2-quinazolinamine;
N-((1S)-2-(3-(1-amino-1-methylethyl)phenyl)-1-methylethyl)-6-(3-methyl-2-pyridinyl)-2-quinazolinamine;
N-((1S)-2-(3-((1S)-1-aminoethyl)phenyl)-1-methylethyl)-6-(2-chloro-3-pyridinyl)-2-quinazolinamine;
N-((1S)-2-(3-((1S)-1-aminoethyl)phenyl)-1-methylethyl)-6-(4-methyl-3-pyridinyl)-2-quinazolinamine;
N˜
1˜
,N˜
1˜
-diethyl-N-4-(6-(4-methyl-3-pyridinyl)-2-quinazolinyl)-1,4-pentanediamine;
N-(2-(3-chlorophenyl)ethyl)-6-(4-methyl-3-pyridinyl)-2-quinazolinamine;
(5S)-5-((6-(4-methyl-3-pyridinyl)-2-quinazolinyl)amino)-2-piperidinone;
((1R)-4-(diethylamino)-1-methylbutyl)(6-(4-methyl-3-pyridinyl)-2-quinazolinyl)amine;
((1S)-4-(diethylamino)-1-methylbutyl)(6-(4-methyl-3-pyridinyl)-2-quinazolinyl)amine;
N,N,2,2-tetramethyl-N′
-(6-(4-methyl-3-pyridinyl)-2-quinazolinyl)-1,3-propanediamine;
6-(4-methyl-3-pyridinyl)-N-(4-(1-pyrrolidinyl)butyl)-2-quinazolinamine;
N-((1S)-1-(4-fluorophenyl)ethyl)-6-(4-methyl-3-pyridinyl)-2-quinazolinamine;
4-chloro-N-cyclopropyl-3-(2-((2-(dimethylamino)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-3-(2-((2-(dimethylamino)ethyl)amino)-6-quinazolinyl)-4-(trifluoromethyl)benzamide;
ethyl 5-(2-((2-(dimethylamino)ethyl)amino)-6-quinazolinyl)-4-methyl-2-thiophenecarboxylate;
6-(2-methylphenyl)-2-quinazolinamine;
6-(2-methylphenyl)-N-(2-(3-pyridinyl)ethyl)-2-quinazolinamine;
N-((1S)-2-(3-(aminomethyl)phenyl)-1-methylethyl)-6-(2-methylphenyl)-2-quinazolinamine;
N-(2,4-dimethylphenyl)-6-(2-methylphenyl)-2-quinazolinamine;
6-(2-methylphenyl)-N-(2-(4-morpholinyl)ethyl)-2-quinazolinamine;
6-(2-((dimethylamino)methyl)phenyl)-N-(2-(4-morpholinyl)ethyl)-2-quinazolinamine;
6-(2-((dimethylamino)methyl)phenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(4-fluoro-2-methylphenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(3-chloro-2-methylphenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(2,6-dimethylphenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
(3-(2-((2-(2-pyridinyl)ethyl)amino)-6-quinazolinyl)phenyl)methanol;
(2-(2-((2-(2-pyridinyl)ethyl)amino)-6-quinazolinyl)phenyl)methanol;
6-(3-(aminomethyl)phenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
N-methyl-3-(2-((2-(2-pyridinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-3-(2-((2-(2-pyridinyl)ethyl)amino)-6-quinazolinyl)benzamide;
6-phenyl-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
6-(2-(methyloxy)phenyl)-N-(2-(2-pyridinyl)ethyl)-2-quinazolinamine;
4-((6-(2,6-dimethylphenyl)-2-quinazolinyl)amino)cyclohexanol;
N-(3-(2-amino-6-quinazolinyl)-4-methylphenyl)cyclopropanecarboxamide;
N-(4-methyl-3-(2-((2-(4-moxpholinyl)ethyl)amino)-6-quinazolinyl)phenyl)cyclopropanecarboxamide;
N-(3-methyl-4-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)phenyl)cyclopropanecarboxamide;
N-cyclopropyl-3-(2-(3-(dimethylamino)-1-propynyl)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-3-(2-(3-(dimethylamino)propyl)-6-quinazolinyl)-4-methylbenzamide;
1,1-dimethylethyl 1-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-3-pyrrolidinylcarbamate;
3-(2-((3S)-3-amino-1-pyrrolidinyl)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-(((3R)-6-oxo-3-piperidinyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-3-(2-((2-((1,1-dimethylethyl)amino)ethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
3-(2-(cyclohexylamino)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-(((3S)-6-oxo-3-piperidinyl)amino)-6-quinazolinyl)benzamide;
N-ethyl-4-methyl-3-(2-(((3S)-6-oxo-3-piperidinyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-3-(2-((2-(1,1-dioxido-4-thiomorpholinyl)ethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-((2-(2-oxo-1-pyrrolidinyl)ethyl)amino)-6-quinazolinyl)benzamide;
3-(2-(4-amino-1-piperidinyl)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
3-(2-(4-(acetylamino)-1-piperidinyl)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
1,1-dimethylethyl(1-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-4-piperidinyl)carbamate;
1,1-dimethylethyl 4-((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)-1-piperidinecarboxylate;
N-cyclopropyl-4-methyl-3-(2-(4-piperidinylamino)-6-quinazolinyl)benzamide;
3-(2-((1-acetyl-4-piperidinyl)amino)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(4-(2-methylphenyl)-7-isoquinolinyl)benzamide;
4-methyl-3-(4-(2-methylphenyl)-7-isoquinolinyl)benzamide;
methyl 4-methyl-3-(4-((3S)-3-methyl-4-morpholinyl)-7-isoquinolinyl)benzoate;
N-cyclopropyl-4-methyl-3-(2-((2-(1-piperazinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((3S)-3-piperidinylamino)-6-quinazolinyl)benzamide;
1,1-dimethylethyl 2-((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)-2-methylpropylcarbamate;
1,1-dimethylethyl(2S)-2-(((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)methyl)-1-pyrrolidinecarboxylate;
N-cyclopropyl-4-methyl-3-(2-((2-(4-methyl-1-piperazinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-(((2S)-2-pyrrolidinylmethyl)amino)-6-quinazolinyl)benzamide;
1,1-dimethylethyl(2R)-2-(((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)methyl)-1-pyrrolidinecarboxylate;
N-cyclopropyl-4-methyl-3-(2-(((2R)-2-pyrrolidinylmethyl)amino)-6-quinazolinyl)benzamide;
3-(2-((2-amino-1,1-dimethylethyl)amino)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-(((3R)-1-methyl-3-pyrrolidinyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((3R)-3-pyrrolidinylamino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((((2S)-1-methyl-2-pyrrolidinyl)methyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((((2R)-1-(1-methylethyl)-2-pyrrolidinyl)methyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-4-methyl-3-(2-((((2S)-1-(2-(methyloxy)ethyl)-2-pyrrolidinyl)methyl)amino)-6-quinazolinyl)benzamide;
3-(2-((2-aminoethyl)amino)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-((2-((1-methylethyl)amino)ethyl)amino)-6-quinazolinyl)benzamide N-cyclopropyl-3-(2-(((1R,2R)-2-(dimethylamino)cyclohexyl)amino)-6-quinazolinyl)-4-methylbenzamide N-cyclopropyl-3-(2-(((1S,2S)-2-(dimethylamino)cyclohexyl)amino)-6-quinazolinyl)-4-methylbenzamide N-cyclopropyl-4-methyl-3-(2-(((1R,2R)-2-((1-methylethyl)amino)cyclohexyl)amino)-6-quinazolinyl)benzamide methyl 2-((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)ethylcarbamate N-cyclopropyl-4-methyl-3-(2-(((1S,2S)-2-((1-methylethyl)amino)cyclohexyl)amino)-6-quinazolinyl)benzamide;
1-((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)cyclopentanecarboxylic acid;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-3-(2-thienyl)alanine;
1-((6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)amino)cyclopropanecarboxylic acid;
methyl N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-beta-alaninate;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-2-methylalanine;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-L-valine;
N,4-dimethyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)-N-(2,2,2-trifluoroethyl)benzamide;
4-methyl-N-(2-methylpropyl)-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopentyl-4-methyl-3-(2-((2-(4-morpholinyl)ethyl)amino)-6-quinazolinyl)benzamide;
N-cyclopropyl-3-(2-((3-(dimethylamino)-2,2-dimethylpropyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-3-(2-(((1S,2R)-2-(dimethylamino)cyclohexyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-3-(2-((2-(diethylamino)ethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-((2-(methyloxy)ethyl)amino)-6-quinazolinyl)benzamide;
3-(2-(((1S,2S)-2-aminocyclohexyl)amino)-6-quinazolinyl)-N-cyclopropyl-4-methylbenzamide;
N-cyclopropyl-3-(2-(((1R,2R)-2-(dimethylamino)cyclohexyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-3-(2-((2-furanylmethyl)amino)-6-quinazolinyl)-4-methylbenzamide;
N-cyclopropyl-4-methyl-3-(2-((tetrahydro-2-furanylmethyl)amino)-6-quinazolinyl)benzamide;
N-5-(6-(4-methyl-3-pyridinyl)-2-quinazolinyl)-2,5-pyridinediamine;
((1R)-4-(diethylamino)-1-methylbutyl)(6-(6-fluoro-2-methyl-3-pyridinyl)-2-quinazolinyl)amine;
5-(2-((4-(diethylamino)-1-methylbutyl)amino)-6-quinazolinyl)-6-methyl-2(1H)-pyridinone;
3-(2-(((1R)-4-(diethylamino)-1-methylbutyl)amino)-6-quinazolinyl)-4-methyl-2(1H)-pyridinone;
((1R)-4-(diethylamino)-1-methylbutyl)(6-(2-fluoro-5-methyl-4-pyridinyl)-2-quinazolinyl)amine;
4-(2-(((1R)-4-(diethylamino)-1-methylbutyl)amino)-6-quinazolinyl)-5-methyl-2(1H)-pyridinone;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-D-valine;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-D-leucine;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)glycine;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-L-alanine;
N-(6-(5-((cyclopropylamino)carbonyl)-2-methylphenyl)-2-quinazolinyl)-D-alanine;
5-(2-amino-6-quinazolinyl)-N-(2-(methyl((3R)-1-methyl-3-pyrrolidinyl)amino)-5-(trifluoromethyl)phenyl)-2-(methyloxy)benzamide;
3-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-((phenylmethyl)amino)benzamide;
4-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-5-methyl-2-pyridinecarboxamide;
4-(2-amino-6-quinazolinyl)-N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-1-(methyloxy)-2-naphthalenecarboxamide;
4-(2-amino-6-quinazolinyl)-1-(methyloxy)-N-(3-(trifluoromethyl)phenyl)-2-naphthalenecarboxamide;
4-(2-amino-6-quinazolinyl)-N-(2-(methyl((3R)-1-methyl-3-pyrrolidinyl)amino)-5-(trifluoromethyl)phenyl)-1-(methyloxy)-2-naphthalenecarboxamide;
4-(2-amino-6-quinazolinyl)-N-(2-(((3R)-3-(dimethylamino)-1-pyrrolidinyl)methyl)-5-(trifluoromethyl)phenyl)-1-(methyloxy)-2-naphthalenecarboxamide;
5-(2-amino-6-quinazolinyl)-N-(2-(3,3-dimethyl-2-oxo-1-azetidinyl)-5-(trifluoromethyl)phenyl)-2-(methyloxy)benzamide; and
5-(2-amino-6-quinazolinyl)-N-(2-((3S)-3-(dimethylamino)-1-piperidinyl)-5-(trifluoromethyl)phenyl)-2-fluorobenzamide;
6-(2-phenylimidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine 6-(2-(4-(methyloxy)phenyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-(3-(methyloxy)phenyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-(2-(methyloxy)phenyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-(1,3-benzodioxol-5-yl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-(3-thienyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine;
6-(2-ethyl-1-benzofuran-5-yl)-2-quinazolinamine; and
6-(2-(1,1-dimethylethyl)imidazo[1,2-a]pyridin-6-yl)-2-quinazolinamine.
-
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19. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound according to claim 1.
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21. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound according to claim 18.
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22. A method of modulating in a subject a protein kinase enzyme selected from the group consisting of KDR, Lck, p38, tie2 and a combination thereof, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
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24. A method of treating a disorder related to at least one of Tie-2, Lck, KDR and P38 in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
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26. A method of treating a proliferation-related disorder in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
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29. A method of treating cancer in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
-
33. A method of treating cancer in a subject, the method comprising administering to the subject an effective dosage amount of the pharmaceutical composition of claim 19.
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35. A method of treating angiogenesis in a subject, the method comprising administering to the subject an effective dosage amount of a compound according toclaim 1.
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37. A method of reducing blood flow in a tumor in a subject, said method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
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39. A method of reducing tumor size in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
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41. A method of treating inflammation in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
-
43. A method of inhibiting T cell activation and proliferation in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
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45. A method of treating arthritis, rheumatoid arthritis, psoriatic arthritis, or osteoarthritis in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
-
51. A method of decreasing the level of one or more of TNF-α
- , IL-1β
, IL-6 and IL-8 in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
- , IL-1β
-
53. A method of treating rheumatoid spondylitis, gouty arthritis, adult respiratory distress syndrome (ARDS), anaphylaxis, muscle degeneration, cachexia, Reiter'"'"'s syndrome, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer'"'"'s disease, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, and myalgias due to infection, or which subject is infected by HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses (including HSV-1, HSV-2), or herpes zoster in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 1.
-
11. A compound of Formula I:
-
or stereoisomer, tautomer, solvate, pharmaceutically acceptable salt, derivative or prodrug thereof, wherein A1 is CR5 or N;
one of A2 and A3, independently, is CR5 or N;
B is a direct bond, (CR5R6), C(O), NR6, O, S, S(O) or SO2;
R1 is H, halo, haloalkyl, NO2, CN, R7, NR7R7, NR7R8, OR7;
SR7, OR8, SR8, C(O)R7, OC(O)R7, COOR7, C(O)R8, OC(O)R8, COOR8, C(O)NR7R7, C(S)NR7R7, NR7C(O)R7, NR7C(S)R7, NR7C(O)NR7R7, NR7C(S)NR7R7, NR7(COOR7), OC(O)NR7R7, C(O)NR7R8, C(S)NR7R8, NR7C(O)R8, NR7C(S)R8, NR7C(O)NR7R8, NR7C(S)NR7R8, NR7(COOR8), OC(O)NR7R8, S(O)2R7, S(O)2NR7R7, NR7S(O)2NR7R7, NR7S(O)2R7, S(O)2R8, S(O)2NR7R8, NR7S(O)2NR7R8 or NR7S(O)2R8;
R2 is H, halo, haloalkyl, NO2, CN, OR7, SR7, NR7R7, NR7R8, C(O)R7, COOR7, C(O)NR7R7, C(O)NR7R8, NR7C(O)NR7R7, NR7C(O)NR7R8, OC(O)NR7R8, S(O)2R7, S(O)2NR7R7, S(O)2NR7R8, NR7S(O)2R7, NR7S(O)2R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R3 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, wherein said ring system is substituted independently with one or more substituents of R10, R11, R16, NR10R10, NR10R11, OR10, SR10, OR11, SR11, C(O)R10, C(S)R10, C(NCN)R10, C(O)R11, C(S)R11, C(NCN)R11, C(O)C(O)R10, OC(O)R10, COOR10, C(O)SR10, C(O)C(O)R11, OC(O)R11, COOR11, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, OC(O)NR10R11, NR10C(O)R10, NR10C(O)R11, NR10C(S)R10, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), NR10C(O)C(O)R10, NR10C(O)C(O)R11, NR10C(O)C(O)NR10R11, S(O)2R10, S(O)2R11, S(O)2NR10R10, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O), R10 or NR10S(O)2R11, provided that at least one substituent on R3 is C(O)R10, OC(O)R10, COOR10, C(O)R11, OC(O)R11, COOR11, C(O)SR10, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, NR10C(O)R10, NR10C(S)R10, NR10C(O)R11, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), OC(O)NR10R11, S(O)2R11, S(O)2NR10R10, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)2R11;
R4 is H, halo, haloalkyl, NO2, CN, NR7R7, NR7R8, OR7;
SR7, C(O)R7, OC(O)R7, COOR7, C(O)NR7R7, C(O)NR7R8, NR7C(O)R7, NR7C(O)R8, NR8C(O)NR7R8, NR7(COOR7), OC(O)NR7R8, S(O)2R7, S(O)2NR7R8, NR7S(O)2NR7R8, NR7S(O)2R7, NR7S(O)2R7, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R5 is H, halo, haloalkyl, NO2, CN, SR7, OR7, C(O)R7, COOR7, OC(O)R7, NR7R7, NR7R8, C(O)NR7R7, C(O)NR7R8, NR7C(O)R7, NR7C(O)NR7R8, S(O)NR7R8, S(O)2NR7R8, NR7S(O)NR7R8, NR7S(O)2NR7R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R6 is H, CN or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R8 or R9;
R7 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of NR8R9, NR9R9, OR8, SR8, OR9, SR9, C(O)R8, OC(O)R8, COOR8, C(O)R9, OC(O)R9, COOR9, C(O)NR8R9, C(O)NR9R9, NR9C(O)R8, NR9C(O)R9, NR9C(O)NR8R9, NR9C(O)NR9R9, NR9(COOR8), NR9(COOR9), OC(O)NR8R9, OC(O)NR9R9, S(O)2R8, S(O)2NR8R9, S(O)2R9, S(O)2NR9R9, NR9S(O)2NR8R9, NR9S(O)2NR9R9, NR9S(O)2R8, NR9S(O)2R9, R8 or R9;
R8 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-3 substituents of R9, oxo, NR9R9, OR9;
SR9, C(O)R9 or a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and optionally substituted independently with 1-3 substituents of R9;
alternatively, R7 and R8 taken together form a saturated or partially or fully unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-3 substituents of R9;
R9 is H, halo, haloalkyl, CN, OH, NO2, NH2, acetyl, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl or a saturated or partially or fully unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, wherein each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl and ring of said ring system is optionally substituted independently with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, OH, oxo, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamine, dimethylamine, ethylamine, diethylamine, propylamine, isopropylamine, dipropylamine, diisopropylamine, benzyl or phenyl;
R10 is H, halo, haloalkyl, CN, NO2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R11, R12 or R16, NR11R12, NR12R12, OR11, SR11, OR12, SR12, C(O)R11, OC(O)R11, COOR11, C(O)R12, OC(O)R12, COOR12, C(O)NR11R12, NR12C(O)R11, C(O)NR12R12, NR11C(O)R12, NR12C(O)NR11R12, NR12C(O)NR12R12, NR12(COOR11), NR12(COOR12), OC(O)NR11R12, OC(O)NR12R12, S(O)2R11, S(O)2R12, S(O)2NR11R12, S(O)2NR12R12, NR12S(O)2NR11R12, NR12S(O)2NR12R12, NR12S(O)2R11, NR12S(O)2R12, NR12S(O)2R11 or NR12S(O)2R12;
R11 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-5 substituents of R12, R13, R14 or R16;
alternatively, R10 and R11 taken together form a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-5 substituents of R12, R13, R14 or R16;
R12 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkyl, each of which is optionally substituted independently with 1-5 substituents of R13, R14, R15 or R16;
R13 is NR14R15, NR15R15, OR14;
SR14, OR15;
SR15, C(O)R14OC(O)R14, COOR14, C(O)R15, OC(O)R15, COOR15, C(O)NR14R15, C(O)NR15R15, NR14C(O)R14, NR15C(O)R14, NR14C(O)R15, NR15C(O)R15, NR15C(O)NR14R15, NR15C(O)NR15R15, NR15(COOR14), NR15(COOR15), OC(O)NR14R15, OC(O)NR15R15, S(O)2R14, S(O)2R15, S(O)2NR14R15, S(O)2NR15R15, NR14S(O)2NR14R15, NR15S(O)2NR15R15, NR14S(O)2R14 or NR15S(O)2R15;
R14 is a partially or fully saturated or unsaturated 5-8 membered or a saturated or partially or fully unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-5 substituents of R15 or R16;
R15 is H or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkoxyl, each of which is optionally substituted independently with 1-5 substituents of R16; and
R16 is H, halo, haloalkyl, CN, OH, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, oxo, acetyl, benzyl, phenyl, cyclopropyl, cyclobutyl or a partially or fully saturated or unsaturated 5-8 membered monocyclic or 6-12 membered bicyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic or 1-6 heteroatoms if bicyclic, said heteroatoms selected from O, N, or S, and optionally substituted independently with 1-5 substituents of halo, haloalkyl, CN, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, benzyl or phenyl;
provided that (1) when R1 is NR7R8, R8 is not a substituted or unsubstituted phenyl or a 9- or 10-membered bicyclic heterocycle containing 1 or 2 nitrogen atoms;
(2) when R2 is NR7R8, R7 and R8 are H;
(3) when A2 is N and A3 is CH, then R4 is not halo, hydroxyl or a mono- or di-alkyl, alkylamino, alkenyl, alkynyl, or aryl substituted amine;
or(4) when each of A1, A2 and A3 is, independently, CR5, then no more than two of R2, R4 and R5 is NR7R8 or C1-2-alkyl-R8. - View Dependent Claims (12, 13, 14, 15, 16, 17, 20, 23, 25, 27, 28, 30, 31, 32, 34, 36, 38, 40, 42, 44, 46, 47, 48, 49, 50, 52, 54, 55, 56, 57, 58, 59, 60, 61)
B is a direct bond;
R2 is H; and
R3 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, dihydrobenzofuranyl, benzothiophenyl or benzimidazolyl, each of which is substituted independently with 1-3 substituents of R10, R11, R15, NR10R10, NR10R11, OR10, SR10, OR11, SR11, C(O)R10, C(S)R10, C(NCN)R10, C(O)R11, C(S)R11, C(NCN)R11, C(O)C(O)R10, OC(O)R10, COOR10, C(O)SR10, C(O)C(O)R11, OC(O)R11, COOR11, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, OC(O)NR10R11, NR10C(O)R10, NR10C(O)R11, NR10C(S)R10, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), NR10C(O)C(O)R10, NR10C(O)C(O)R11, NR10C(O)C(O)NR10R11, S(O)2R10, S(O)2R11, S(O)2NR10R10, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)2R11, provided that at least one substituent on R3 is C(O)R10, OC(O)R10, COOR10, C(O)R11, OC(O)R11, COOR11, C(O)SR10, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, NR10C(O)R10, NR10C(S)R10, NR10C(O)R11, NR10C(S)R11, NR10C(O)NR10R11, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), OC(O)NR10R11, S(O)2R11, S(O)2NR10R10, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)S2R11.
-
-
13. The compound of formula I of claim 11
wherein A1 is N; -
A2 is CR5 or N;
A3 is CR5;
B is a direct bond, (CR5R6), C(O), NR6, O or S;
R1 is halo, haloalkyl, NO2, CN, R7, NR7R7, NR7R8, OR7;
SR7, OR8;
SR8, C(O)R7, OC(O)R7, COOR7, C(O)R8, OC(O)R8, COOR8, C(O)NR7R7, C(S)NR7R7, NR7C(O)R7, NR7C(S)R7, NR7C(O)NR7R7, NR7C(S)NR7R7, NR7(COOR7), OC(O)NR7R7, C(O)NR7R8C(S)NR7R8, NR7C(O)R8, NR7C(S)R8, NR7C(O)NR7R8, NR7C(S)NR7R8, NR7(COOR8), OC(O)NR7R8, S(O)2R7, S(O)2NR7R7, NR7S(O)2NR7R7, NR7S(O)2R7, S(O)2R8, S(O)2NR7R8, NR7S(O)2NR7R8 or NR7S(O)2R8;
R2 is H, halo, haloalkyl, NO2, CN, OR7, SR7, C(O)R7, COOR7, C(O)NR7R7, C(O)NR7R8, NR7C(O)NR7R8, S(O)2R7, S(O)2NR7R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl;
R3 is phenyl, naphthyl, pyridyl, piperazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, dihydrobenzofuranyl, benzothiophenyl or benzimidazolyl, each of which is substituted independently with 1-3 substituents of R10, R11, R15, NR10R10, NR10R11, OR10, SR10, OR11, SR11, C(O)R10, C(S)R10, C(NCN)R10, C(O)R11, C(S)R11, C(NCN)R11, C(O)C(O)R10, OC(O)R10, COOR10, C(O)SR10, C(O)C(O)R11, OC(O)R11, COOR11, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, OC(O)NR10R10R11, NR10C(O)R10, NR10C(O)R11, NR10C(S)R10, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10) NR10(COOR11), NR10C(O)C(O)R10, NR10C(O)C(O)R11, NR10C(O)C(O)NR10R11, S(O)2R10, S(O)2R11, S(O)2NR10R10, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)2R11, provided that at least one substituent on R3 is C(O)R10, OC(O)R10, COOR10, C(O)R11, OC(O)R11, COOR11, C(O)SR10, C(O)SR11, C(O)NR10R10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, NR10C(O)R10, NR10C(S)R10, NR10C(O)R11, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), OC(O)NR10R11, S(O)2R11, S(O)2NR10R10, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)2R11;
R4 is H, halo, haloalkyl, NO2, CN, NR7R8, OR7;
SR7, C(O)R7C(O)NR7R7, C(O)NR7R8, NR7C(O)R7, NR7C(O)R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl;
R5 is H, halo, haloalkyl, CN, SR7, OR7, NR7R7, NR7R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl;
R6 is H, CN or C1-10-alkyl;
R7 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of NR8R9, NR9R9, OR8, SR8, OR9, SR9, C(O)R8, OC(O)R8, COOR8, C(O)R9, OC(O)R9, COOR9, C(O)NR8R9, C(O)NR9R9, NR9C(O)R8, NR9C(O)R9, NR9C(O)NR8R9, NR9C(O)NR9R9, NR9(COOR8), NR9(COOR9), OC(O)NR8R9, OC(O)NR9R9, S(O)2R8, S(O)2NR8R9, S(O)2R9, S(O)2NR9R9, NR9S(O)2NR8R9, NR9S(O)2NR9R9, NR9S(O)2R8, NR9S(O)2R9, R8 or R9;
R8 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-3 substituents of R9, oxo, NR9R9, OR9;
SR9, C(O)R9 or a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and optionally substituted independently with 1-3 substituents of R9;
alternatively, R7 and R8 taken together form a saturated or partially or fully unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-3 substituents of R9;
R9 is H, halo, haloalkyl, CN, OH, NO2, NH2, acetyl, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl or a saturated or partially or fully unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, wherein each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl and ring of said ring system is optionally substituted independently with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, OH, oxo, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamine, dimethylamine, ethylamine, diethylamine, propylamine, isopropylamine, dipropylamine, diisopropylamine, benzyl or phenyl;
R10 is H, halo, haloalkyl, CN, NO2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R11, R12 or R16, NR11R12, NR12R12, OR11, SR11, OR12, SR12, C(O)R11, OC(O)R11, COOR11, C(O)R12, OC(O)R12, COOR12, C(O)NR11R12, NR12C(O)R11, C(O)NR12R12, NR12C(O)R12, NR12C(O)NR11R12, NR12C(O)NR12R12, NR12(COOR11), NR12(COOR12), OC(O)NR11R12, OC(O)NR12R12, S(O)2R11, S(O)2R12, S(O)2NR11R12, S(O)2NR12R12, NR12S(O)2NR11R12, NR12S(O)2NR12R12, NR12S(O)2R11, NR12S(O)2R12, NR12S(O)2R11 or NR12S(O)2R12;
R11 is a partially or fully saturated or unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-5 substituents of R12, R13, R14 or R16;
alternatively, R10 and R11 taken together form a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-5 substituents of R12, R13, R14 or R16;
R12 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkyl, each of which is optionally substituted independently with 1-5 substituents of R13, R14, R15 or R16;
R13 is NR14R15, NR15R15, OR14;
SR14, OR15;
SR15, C(O)R14, OC(O)R14, COOR14, C(O)R15, OC(O)R15, COOR15, C(O)NR14R15, C(O)NR14R15, NR14C(O)R14, NR15C(O)R14, NR14C(O)R15, NR15C(O)R15, NR15C(O)NR14R15, NR15C(O)NR15R15, NR15(COOR14), NR15(COOR15), OC(O)NR14R15, OC(O)NR15R15, S(O)2R14, S(O)2R15, S(O)2NR14R15, S(O)2NR15R15, NR14S(O)2NR14R15, NR15S(O)2NR15R15, NR14S(O)2R14 or NR15S(O)2R15;
R14 is a partially or fully saturated or unsaturated 5-8 membered or a saturated or partially or fully unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S, and wherein each ring of said ring system is optionally substituted independently with 1-5 substituents of R15 or R16;
R15 is H or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkoxyl, each of which is optionally substituted independently with 1-5 substituents of R16; and
R16 is H, halo, haloalkyl, CN, OH, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, oxo, acetyl, benzyl, phenyl, cyclopropyl, cyclobutyl or a partially or fully saturated or unsaturated 5-8 membered monocyclic or 6-12 membered bicyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic or 1-6 heteroatoms if bicyclic, said heteroatoms selected from O, N, or S, and optionally substituted independently with 1-5 substituents of halo, haloalkyl, CN, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, benzyl or phenyl.
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14. The compound of formula I of claim 11
wherein A1 is N; -
A2 is CR5 or N;
A3 is CR5;
B is a direct bond, C(O), NR6, O or S;
R1 is NO2, CN, R7, NR7R7, NR7R8, OR7;
SR7, OR8;
SR8, C(O)R7, OC(O)R7, COOR7, C(O)R8, OC(O)R8, COOR8, C(O)NR7R7, C(S)NR7R7, NR7C(O)R7, NR7C(S)R7, NR7C(O)NR7R7, NR7C(S)NR7R7, NR7(COOR), OC(O)NR7R7, C(O)NR7R8, C(S)NR7R8, NR7C(O)R8, NR7C(S)R8, NR7C(O)NR7R8, NR7C(S)NR7R8, NR7(COOR8), OC(O)NR7R8, S(O)2R7, S(O)2NR7R7, NR7S(O)2NR7R7, NR7S(O)2R7, S(O)2R8, S(O)2NR7R8, NR7S(O)2NR7R8 or NR7S(O)2R8;
R2 is H, halo, haloalkyl, NO2, CN, OR7, SR7, C(O)R7, COOR7, C(O)NR7R7, C(O)NR7R8, NR7C(O)NR7R8, S(O)2R7, S(O)2NR7R8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl;
R3 is wherein A4 is CR3b or N;
each of A5, A6, A7 and A8 is, independently, CR3a or N;
each of A9 and A10 is, independently, CR3b or N;
each of X1 and X2 is, independently, CR3a or N;
each of X3 and X4 is, independently, CR3b or N;
Y is CR3bR3c, NR3c, O or S; and
Z is CH or N;
R3a is C(O)R10, OC(O)R10, COOR10, C(O)R11, OC(O)R11, COOR11, C(O)SR10, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, NR10C(O)R10, NR10C(S)R10, NR10C(O)R11, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), OC(O)NR10R11, S(O)2R11, S(O)2NR10R11, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)2R11;
R3b is H, halo, haloalkyl, CN, NO2, NH2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl; and
R3c is H, CN or C1-10-alkyl;
R4 is H, halo, haloalkyl, NO2, CN, NR7R8, OR7;
SR7, C(O)R7, C(O)NR7R7, C(O)NR7R7, NR7C(O)R7, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl;
R5 is H, halo, haloalkyl, CN, NO2, NH2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl;
R6 is H, CN or C1-10-alkyl;
R7 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of NR8R9, NR9R9, OR8, SR8, OR9, SR9, C(O)R8, OC(O)R8, COOR8, C(O)R9, OC(O)R9, COOR9, C(O)NR8R9, C(O)NR9R9, NR9C(O)R8, NR9C(O)R9, NR9C(O)NR8R9, NR9C(O)NR9R9, NR9(COOR8), NR9(COOR9), OC(O)NR8R9, OC(O)NR9R9, S(O)2R8, S(O)2NR8R9, S(O)2R9, S(O)2NR9R9, NR9S(O)2NR8R9, NR9S(O)2NR9R9, NR9S(O)2R8, NR9S(O)2R9, R8 or R9;
R8 is a ring system selected from phenyl, naphthyl, pyridyl, piperazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, tetrahydrofuranyl, pyrrolidinyl, oxazolinyl, isoxazolinyl, thiazolinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, pyranyl, dioxozinyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, wherein the ring system is optionally substituted independently with 1-3 substituents of R9, oxo, NR9R9, OR9;
SR9, C(O)R9, phenyl, pyridyl, piperidyl, piperazinyl or morpholinyl;
alternatively, R7 and R8 taken together form a saturated or partially or fully unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-3 substituents of R9;
R9 is H, halo, haloalkyl, CN, OH, NO2, NH2, acetyl, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl or a ring system selected from phenyl, naphthyl, pyridyl, piperazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, tetrahydrofuranyl, pyrrolidinyl, oxazolinyl, isoxazolinyl, thiazolinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, pyranyl, dioxozinyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl and ring system optionally substituted independently with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, OH, oxo, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, propylamine, isopropylamine, dipropylamine, diisopropylamine, benzyl or phenyl;
R10 is H, halo, haloalkyl, CN, NO2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R11, R12 or R16, NR11R12, NR12R12, OR11, SR11, OR12, SR12, C(O)R11, OC(O)R11, COOR11, C(O)R12, OC(O)R12, COOR12, C(O)NR11R12, NR12C(O)R11, C(O)NR12R12, NR12C(O)R12, NR12C(O)NR11R12, NR12C(O)NR12R12, NR12(COOR11), NR12(COOR12), OC(O)NR11R12, OC(O)NR12R12, S(O)2R11, S(O)2R12, S(O)2NR11R12, S(O)2NR12R12, NR12S(O)2NR11R12, NR12S(O)2NR12R12, NR12S(O)2R11, NR12S(O)2R12, NR12S(O)2R11 or NR12S(O)2R12;
R11 is a ring system selected from phenyl, naphthyl, 5,6,7,8-tetrahydronaphthyl, dihydro-indenyl, pyridyl, pyrimidinyl, triazinyl, quinolinyl, tetrahydroquinolinyl, oxo-tetrahydroquinolinyl, isoquinolinyl, oxo-tetrahydroisoquinolinyl, tetrahydroisoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, tetrahydrofuranyl, pyrrolyl, pyrazolyl, thieno-pyrazolyl, tetrahydropentapyrazolyl, imidazolyl, triazolyl, tetrazolyl, thiazolyl, thiadiazolyl, benzothiazolyl, oxazolyl, oxadiazolyl, benzoxazolyl, benzoxadiazolyl, isoxazolyl, isothiazolyl, indolyl, azaindolyl, 2,3-dihydroindolyl, isoindolyl, indazolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, imidazo-pyridinyl, purinyl, benzotriazolyl, oxazolinyl, isoxazolinyl, thiazolinyl, pyrrolidinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, pyranyl, dioxozinyl, 2,3-dihydro-1,4-benzoxazinyl, 1,3-benzodioxolyl, cyclopropyl, cyclobutyl, azetidinyl, cyclopentyl, cyclohexyl and cycloheptyl, said ring system optionally substituted independently with 1-3 substituents of R12, R13, R14 or R16;
alternatively, R10 and R11 taken together form a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-3 substituents of R12, R13, R14 or R16;
R12 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkyl, each of which is optionally substituted independently with 1-3 substituents of R13, R14, R15 or R16;
R13 is NR14R15, NR15R15, OR14;
SR14, OR15;
SR15, C(O)R14, OC(O)R14, COOR14C(O)R15, OC(O)R15, CR15, C(O)NR14R15, C(O)NR15R15, NR14C(O)R14, NR15C(O)R14, NR14C(O)R15, NR15C(O) R15, NR15C(O)NR14R15, NR15C(O)NR15R15, NR15(COOR14), NR15(COOR15), OC(O)NR14R15, OC(O)NR15R15, S(O)2R4, S(O)2R15, S(O)2NR14R15, S(O)2NR15R15, NR14S(O)2NR14R15, NR15S(O)2NR15R15, NR14S(O)2R14 or NR15S(O)2R15;
R14 is phenyl, pyridyl, pyrimidinyl, thiophenyl, furyl, tetrahydrofuryl, pyrrolyl, pyrazolyl, thieno-pyrazolyl, imidazolyl, triazolyl, thiazolyl, thiadiazolyl, benzothiazolyl, oxazolyl, oxadiazolyl, benzoxazolyl, benzoxadiazolyl, isoxazolyl, isothiazolyl, indolyl, azaindolyl, isoindolyl, indazolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, pyrrolidinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, 2,3-dihydro-1,4-benzoxazinyl, 1,3-benzodioxolyl, cyclopropyl, cyclobutyl, azetidinyl, cyclopentyl and cyclohexyl, each of which is optionally substituted independently with 1-3 substituents of R15 or R16;
R15 is H or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkoxyl, each of which is optionally substituted independently with 1-3 substituents of R16; and
R16 is H, halo, haloalkyl, CN, OH, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, oxo, acetyl, benzyl, phenyl, cyclopropyl, cyclobutyl or a partially or fully saturated or unsaturated 5-8 membered monocyclic or 6-12 membered bicyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic or 1-6 heteroatoms if bicyclic, said heteroatoms selected from O, N, or S, and optionally substituted independently with 1-5 substituents of halo, haloalkyl, CN, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, benzyl or phenyl.
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15. The compound of claim 11 having a formula II
wherein A2 is CR5 or N; -
R2 is H, halo, haloalkyl, NO2, CN, OR7b, SR7b, C(O)R7b, COOR7b, C(O)NR7aR7b, C(O)NR7bR8, S(O)2R7b, S(O)2NR7bR8, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl;
R3 is wherein Y is NR6, S or O;
R3a is C(O)R10, OC(O)R10, COOR10, C(O)R10, OC(O)R11, COOR11, C(O)SR10, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, NR10C(O)R10, NR10C(S)R11, NR10C(O)R11, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), OC(O)NR10R11, S(O)2R11, S(O)2NR10R10, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)2R11;
R3b is independently, at each occurrence, H, halo, haloalkyl, CN, NO2, NH2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C1-10-alkoxyl;
R3c is H, halo, haloalkyl, CN, NO2, NH2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C1-10-alkoxyl;
R3d is H, halo, haloalkyl, CN, NO2, NH2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C1-10-alkoxyl; and
alternatively, R3c and R3d taken together form a 5 or 6 membered ring formed of carbon atoms and optionally including 1-3 heteroatoms selected from N, O and S, and optionally substituted with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, oxo, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C1-10-alkoxyl;
R4 is H, halo, haloalkyl, NO2, CN, NR7R8, OR8;
SR7, C(O)R7, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl;
R5 is H, halo, haloalkyl, CN, NO2, NH2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C1-10-alkoxyl;
R6 is H, CN or C1-10-alkyl;
R7a is H, C(O)R8, COOR8, C(O)R9, COOR9, C(O)NR8R9, C(O)NR9R9, S(O)2R8, S(O)2NR8R9, S(O)2R9, S(O)2NR9R9, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of NR8R9, NR9R9, OR8, SR8, OR9, SR9, C(O)R8, OC(O)R8, COOR8, C(O)R9, OC(O)R9, COOR9, C(O)NR8R9, C(O)NR9R9, NR9C(O)R8, NR9C(O)R9, NR9C(O)NR8R9, NR9C(O)NR9R9, NR9(COOR8), NR9(COOR9), OC(O)NR8R9, OC(O)NR9R9, S(O)2R8, S(O)2NR8R9, S(O)2R9, S(O)2NR9R9, NR9S(O)2NR8R9, NR9S(O)2NR9R9, NR9S(O)2R8, NR9S(O)2R9, R8 or R9;
R7b is H, CN, haloalkyl or C1-10-alkyl;
alternatively, R7a and R7b taken together form a saturated or partially or fully unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-3 substituents of R9;
R8 is a ring system selected from phenyl, naphthyl, pyridyl, piperazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, tetrahydrofuranyl, pyrrolidinyl, oxazolinyl, isoxazolinyl, thiazolinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, pyranyl, dioxozinyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, wherein the ring system is optionally substituted independently with 1-3 substituents of R9, oxo, NR9R9, OR9;
SR9, C(O)R9, phenyl, pyridyl, piperidyl, piperazinyl or morpholinyl;
R9 is H, halo, haloalkyl, CN, OH, NO2, NH2, acetyl, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl or a ring system selected from phenyl, naphthyl, pyridyl, piperazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, tetrahydrofuranyl, pyrrolidinyl, oxazolinyl, isoxazolinyl, thiazolinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, pyranyl, dioxozinyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl and ring system optionally substituted independently with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, OH, oxo, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, propylamine, isopropylamine, dipropylamine, diisopropylamine, benzyl or phenyl;
R10 is H, halo, haloalkyl, CN, NO2, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl or C4-10-cycloalkenyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of R11, R12 or R16, NR11R12, NR12R12, OR11, SR11, OR12, SR12, C(O)R11, OC(O)R11, COOR11, C(O)R12, OC(O)R12, COOR12, C(O)NR11R12, NR12C(O)R11, C(O)NR12R12, NR12C(O)R12, NR12C(O)NR11R12, NR12C(O)NR12R12, NR12(COOR11), NR12(COOR12), OC(O)NR11R12, OC(O)NR12R12, S(O)2R11, S(O)2R12, S(O)2NR11R12, S(O)2NR12R12, NR12S(O)2NR11R12, NR12S(O)2NR12R12, NR12S(O)2R11, NR12S(O)2R12, NR12S(O)2R11 or NR12S(O)2R12;
R11 is a ring system selected from phenyl, naphthyl, 5,6,7,8-tetrahydronaphthyl, dihydro-indenyl, pyridyl, pyrimidinyl, triazinyl, quinolinyl, tetrahydroquinolinyl, oxo-tetrahydroquinolinyl, isoquinolinyl, oxo-tetrahydroisoquinolinyl, tetrahydroisoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, tetrahydrofuranyl, pyrrolyl, pyrazolyl, thieno-pyrazolyl, tetrahydropentapyrazolyl, imidazolyl, triazolyl, tetrazolyl, thiazolyl, thiadiazolyl, benzothiazolyl, oxazolyl, oxadiazolyl, benzoxazolyl, benzoxadiazolyl, isoxazolyl, isothiazolyl, indolyl, azaindolyl, 2,3-dihydroindolyl, isoindolyl, indazolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, imidazo-pyridinyl, purinyl, benzotriazolyl, oxazolinyl, isoxazolinyl, thiazolinyl, pyrrolidinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, pyranyl, dioxozinyl, 2,3-dihydro-1,4-benzoxazinyl, 1,3-benzodioxolyl, cyclopropyl, cyclobutyl, azetidinyl, cyclopentyl, cyclohexyl and cycloheptyl, said ring system optionally substituted independently with 1-3 substituents of R12, R13, R14 or R16;
alternatively, R10 and R11 taken together form a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-3 substituents of R12, R13, R14 or R16;
R12 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkyl, each of which is optionally substituted independently with 1-3 substituents of R13, R14, R15 or R16;
R13 is NR14R15, NR15R15, OR14;
SR14, OR15;
SR15, C(O)R14OC(O)R14, COOR14, C(O)R15, OC(O)R15, COOR15, C(O)NR14R15, C(O)NR15R15, NR14C(O)R14, NR15C(O)R14, NR14C(O)R15, NR15C(O)R15, NR15C(O)NR14R15, NR15C(O)NR15R15, NR15(COOR14) NR15(COOR15), OC(O)NR14R15, OC(O)NR15R15, S(O)2R14, S(O)2R15, S(O)2NR14R15, S(O)2NR15R15, NR14S(O)2NR14R15, NR15S(O)2NR15R15R15, NR14S(O)2R14 or NR15S(O)2R15;
R14 is phenyl, pyridyl, pyrimidinyl, thiophenyl, furyl, tetrahydrofuryl, pyrrolyl, pyrazolyl, thieno-pyrazolyl, imidazolyl, triazolyl, thiazolyl, thiadiazolyl, benzothiazolyl, oxazolyl, oxadiazolyl, benzoxazolyl, benzoxadiazolyl, isoxazolyl, isothiazolyl, indolyl, azaindolyl, isoindolyl, indazolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, pyrrolidinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, 2,3-dihydro-1,4-benzoxazinyl, 1,3-benzodioxolyl, cyclopropyl, cyclobutyl, azetidinyl, cyclopentyl and cyclohexyl, each of which is optionally substituted independently with 1-3 substituents of R15 or R16;
R15 is H or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkoxyl, each of which is optionally substituted independently with 1-5 substituents of R16; and
R16 is H, halo, haloalkyl, CN, OH, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, oxo, acetyl, benzyl, phenyl, cyclopropyl, cyclobutyl or a partially or fully saturated or unsaturated 5-8 membered monocyclic or 6-12 membered bicyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic or 1-6 heteroatoms if bicyclic, said heteroatoms selected from O, N, or S, and optionally substituted independently with 1-5 substituents of halo, haloalkyl, CN, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, benzyl or phenyl.
-
-
16. The compound of claim 15 wherein
R2 is H, NO2, CN, OR7b, SR7b, C1-10-alkyl or C3-10-cycloalkyl; -
R3 is wherein R3a is C(O)R10, COOR10, C(O)R11, COOR11, C(O)SR10, C(O)SR11, C(O)NR10R10, C(S)NR10R10, C(O)NR10R11, C(S)NR10R11, NR10C(O)R10, NR10C(S)R10, NR10C(O)R11, NR10C(S)R11, NR10C(O)NR10R10, NR10C(O)NR10R11, NR10C(S)NR10R10, NR10C(S)NR10R11, NR10(COOR10), NR10(COOR11), S(O)2R11, S(O)2NR10R10, S(O)2NR10R11, NR10S(O)2NR10R11, NR10S(O)2R10 or NR10S(O)2R11;
R3b is H, F, Cl, Br, I, CF3, CF2CF3, OCF3, OCF2CF3, CN, NO2, NH2, methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, acetylenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, OH, methoxyl, ethoxyl, propoxyl, SH, thiomethyl or thioethyl;
R3c is H, F, Cl, Br, I, CF3, CF2CF3, OCF3, OCF2CF3, CN, NO2, NH2, methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, acetylenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, OH, methoxyl, ethoxyl, propoxyl, SH, thiomethyl or thioethyl;
R3d is H, F, Cl, Br, I, CF3, CF2CF3, OCF3, OCF2CF3, CN, NO2, NH2, methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, acetylenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, OH, methoxyl, ethoxyl, propoxyl, SH, thiomethyl or thioethyl;
R4 is H, F, Cl, Br, I, CF3, CF2CF3, OCF3, CN, methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, OH, methoxyl, ethoxyl, propoxyl;
R5 is H, F, Cl, Br, I, CF3, CF2CF3, OCF3, CN, methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, OH, methoxyl, ethoxyl, propoxyl;
R6 is H, CN, methyl, ethyl, propyl, isopropyl or n-butyl;
R7a is H, C(O)R8, COOR8, C(O)R9, COOR9, C(O)NR8R9, C(O)NR9R9, S(O)2R8, S(O)2NR8R9, S(O)2R9, S(O)2NR9R9, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl and C3-10-cycloalkyl optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with one or more substituents of NR8R9, NR9R9, OR8, SR8, OR9, SR9, C(O)R8, C(O)R9, C(O)NR8R9, C(O)NR9R9, NR9C(O)R8, NR9C(O)R9, NR9C(O)NR8R9, NR9C(O)NR9R9, NR9(COOR8), NR9(COOR9), S(O)2R8, S(O)2NR8R9, S(O)2R9, S(O)2NR9R9, NR9S(O)2NR8R9, NR9S(O)2NR9R9, NR9S(O)2R8, NR9S(O)2R9, R8 or R9;
R7b is H;
R8 is a ring system selected from phenyl, naphthyl, pyridyl, piperazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, tetrahydrofuranyl, pyrrolidinyl, oxazolinyl, isoxazolinyl, thiazolinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, pyranyl, dioxozinyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, wherein the ring system is optionally substituted independently with 1-3 substituents of R9, oxo, NR9R9, OR9;
SR9, C(O)R9, phenyl, pyridyl, piperidyl, piperazinyl or morpholinyl;
R9 is H, halo, haloalkyl, CN, OH, NO2, NH2, acetyl, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl or a ring system selected from phenyl, naphthyl, pyridyl, piperazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, pyrrolyl, imidazolyl, triazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, indolyl, isoindolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, tetrahydrofuranyl, pyrrolidinyl, oxazolinyl, isoxazolinyl, thiazolinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, pyranyl and dioxozinyl, each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl and ring system optionally substituted independently with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, OH, oxo, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, propylamine, isopropylamine, dipropylamine, diisopropylamine, benzyl or phenyl;
R10 is H, methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, acetylenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, OH, methoxyl, ethoxyl, propoxyl, SH, thiomethyl or thioethyl;
each of which is optionally substituted with one or more substituents of R11, R12 or R16;
R11 is a ring system selected from phenyl, naphthyl, 5,6,7,8-tetrahydronaphthyl, dihydro-indenyl, pyridyl, pyrimidinyl, triazinyl, quinolinyl, tetrahydroquinolinyl, oxo-tetrahydroquinolinyl, isoquinolinyl, oxo-tetrahydroisoquinolinyl, tetrahydroisoquinolinyl, quinazolinyl, isoquinazolinyl, thiophenyl, furyl, tetrahydrofuranyl, pyrrolyl, pyrazolyl, thieno-pyrazolyl, tetrahydropentapyrazolyl, imidazolyl, triazolyl, tetrazolyl, thiazolyl, thiadiazolyl, benzothiazolyl, oxazolyl, oxadiazolyl, benzoxazolyl, benzoxadiazolyl, isoxazolyl, isothiazolyl, indolyl, azaindolyl, 2,3-dihydroindolyl, isoindolyl, indazolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, imidazo-pyridinyl, purinyl, benzotriazolyl, oxazolinyl, isoxazolinyl, thiazolinyl, pyrrolidinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, pyranyl, dioxozinyl, 2,3-dihydro-1,4-benzoxazinyl, 1,3-benzodioxolyl, cyclopropyl, cyclobutyl, azetidinyl, cyclopentyl, cyclohexyl and cycloheptyl, said ring system optionally substituted independently with 1-3 substituents of R12, R13, R14 or R16;
alternatively, R10 and R11 taken together form a partially or fully saturated or unsaturated 5-6 membered ring of carbon atoms optionally including 1-3 heteroatoms selected from O, N, or S, and the ring optionally substituted independently with 1-3 substituents of R12, R13, R14 or R16;
R12 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C11—
O—
dialkylamino-, C1-10-alkoxyl or C1-10-thioalkyl, each of which is optionally substituted independently with 1-3 substituents of R13, R14, R15 or R16;
R13 is NR14R15, NR15R15, OR14;
SR14, OR15;
SR15, C(O)R14, OC(O)R14, COOR14, C(O)R15, OC(O)R15, COOR15, C(O)NR14R15, C(O)NR15R15, NR14C(O)R14, NR15C(O)R14, NR14C(O)R15, NR15C(O)R15, NR15C(O)NR14R15, NR15C(O)NR15R15, NR15(COOR14), NR15(COOR15), OC(O)NR14R15, OC(O)NR15R15, S(O)2R14, S(O)2R15, S(O)2NR14R15, S(O)2NR15R15, NR14S(O)2NR14R15, NR15S(O)2NR15R15, NR14S(O)2R14 or NR15S(O)2R15;
R14 is phenyl, pyridyl, pyrimidinyl, thiophenyl, furyl, tetrahydrofuryl, pyrrolyl, pyrazolyl, thieno-pyrazolyl, imidazolyl, triazolyl, thiazolyl, thiadiazolyl, benzothiazolyl, oxazolyl, oxadiazolyl, benzoxazolyl, benzoxadiazolyl, isoxazolyl, isothiazolyl, indolyl, azaindolyl, isoindolyl, indazolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, pyrrolidinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, 2,3-dihydro-1,4-benzoxazinyl, 1,3-benzodioxolyl, cyclopropyl, cyclobutyl, azetidinyl, cyclopentyl and cyclohexyl, each of which is optionally substituted independently with 1-3 substituents of R15 or R16;
R15 is H or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkoxyl, each of which is optionally substituted independently with 1-3 substituents of R16; and
R16 is H, halo, haloalkyl, CN, OH, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, oxo, acetyl, benzyl, phenyl, cyclopropyl, cyclobutyl or a partially or fully saturated or unsaturated 5-8 membered monocyclic or 6-12 membered bicyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic or 1-6 heteroatoms if bicyclic, said heteroatoms selected from O, N, or S, and optionally substituted independently with 1-5 substituents of halo, haloalkyl, CN, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, benzyl or phenyl.
-
-
17. The compound of claim 16 wherein
R11 is phenyl, naphthyl, pyridyl, quinolinyl, tetrahydroquinolinyl, oxo-tetrahydroquinolinyl, isoquinolinyl, oxo-tetrahydroisoquinolinyl, tetrahydroisoquinolinyl, thiophenyl, tetrahydrofuranyl, thieno-pyrazolyl, tetrahydropentapyrazolyl, imidazolyl, thiazolyl, thiadiazolyl, benzothiazolyl, oxazolyl, oxadiazolyl, benzoxazolyl, benzoxadiazolyl, isoxazolyl, isothiazolyl, indolyl, 2,3-dihydroindolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, 2,3-dihydro-1,4-benzoxazinyl, 1,3-benzodioxolyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, said ring system optionally substituted independently with 1-3 substituents of R12, R13, R14 or R16; -
R12 is H, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino- or C1-10-alkoxyl, each of which is optionally substituted independently with 1-3 substituents of R13, R14 R15 or R16;
R13 is NR14R15, NR15R15, OR15;
SR14, OR15;
SR15, C(O)R14OC(O)R14, COOR14, C(O)R15, OC(O)R15, COOR15, C(O)NR14R15, C(O)NR15R15, NR14C(O)R14, NR15C(O)R14, NR14C(O)R15, NR15C(O)R15, NR15C(O)NR14R15, NR15C(O)NR15R15, NR15(COOR14), NR15(COOR15), OC(O)NR14R15, OC(O)NR14R15, S(O)2R14, S(O)2R15, S(O)2NR14R15, S(O)2NR15R15, NR14S(O)2NR14R15, NR15S(O)2NR15R15, NR14S(O)2R14 or NR15S(O)2R15;
R14 is phenyl, pyridyl, pyrimidinyl, thiophenyl, furyl, tetrahydrofuryl, pyrrolyl, pyrazolyl, thieno-pyrazolyl, imidazolyl, triazolyl, thiazolyl, thiadiazolyl, benzothiazolyl, oxazolyl, oxadiazolyl, benzoxazolyl, benzoxadiazolyl, isoxazolyl, isothiazolyl, indolyl, azaindolyl, isoindolyl, indazolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, pyrrolidinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, 2,3-dihydro-1,4-benzoxazinyl, 1,3-benzodioxolyl, cyclopropyl, cyclobutyl, azetidinyl, cyclopentyl and cyclohexyl, each of which is optionally substituted independently with 1-3 substituents of R15 or R16;
R15 is H or C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl or C1-10-thioalkoxyl, each of which is optionally substituted independently with 1-3 substituents of R16; and
R16 is H, halo, haloalkyl, CN, OH, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, oxo, acetyl, benzyl or a ring system selected from phenyl, pyridyl, thiophenyl, furyl, tetrahydrofuryl, pyrrolyl, pyrazolyl, thieno-pyrazolyl, imidazolyl, triazolyl, thiazolyl, thiadiazolyl, benzothiazolyl, oxazolyl, oxadiazolyl, benzoxazolyl, benzoxadiazolyl, isoxazolyl, isothiazolyl, indolyl, azaindolyl, isoindolyl, indazolyl, benzofuranyl, benzothiophenyl, benzimidazolyl, pyrrolidinyl, pyrazolinyl, morpholinyl, piperidinyl, piperazinyl, cyclopropyl, cyclobutyl, azetidinyl, cyclopentyl and cyclohexyl, said ring system optionally substituted independently with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, OH, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, benzyl or phenyl.
-
-
20. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound according to claim 11.
-
23. A method of modulating in a subject a protein kinase enzyme selected from the group consisting of KDR, Lck, p38, tie2 and a combination thereof, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
25. A method of treating a disorder related to at least one of Tie-2, Lck, KDR and P38 in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
27. A method of treating a proliferation-related disorder in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
28. The method of claim 27 wherein the disorder is selected from the group consisting of myocardial infarction, coronary artery disease, peripheral vascular disease, stroke, ocular neovascularization, retinopathy, diabetic retinopathy, age-related macular degeneration, psoriasis, hemangioblastoma, hemangioma, arteriosclerosis, inflammatory disease rheumatoid arthritis, asthma, arterial or post-transplantational atherosclerosis, endometriosis, leukemia and combinations thereof.
-
30. A method of treating cancer in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
31. The method of claim 30 wherein administering the effective amount of the compound to the subject comprises administering the compound in combination with one or more compounds selected from antineoplastic agents, anti-angiogenic agents, chemotherapeutic agents and peptidal cancer therapy agents.
-
32. The method of claim 31 wherein the antineoplastic agents are selected from antibiotic-type agents, alkylating agents, antimetabolite agents, hormonal agents, immunological agents, interferon-type agents, kinase inhibitors, miscellaneous agents and combinations thereof.
-
34. A method of treating cancer in a subject, the method comprising administering to the subject an effective dosage amount of the pharmaceutical composition of claim 20.
-
36. A method of treating angiogenesis in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
38. A method of reducing blood flow in a tumor in a subject, said method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
40. A method of reducing tumor size in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
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42. A method of treating inflammation in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
44. A method of inhibiting T cell activation and proliferation in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
46. A method of treating arthritis, rheumatoid arthritis, psoriatic arthritis, or osteoarthritis in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
47. A method of treating organ transplant, acute transplant or heterograft or homograft rejection, or transplantation tolerance induction in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
48. A method of treating ischemic or reperfusion injury, myocardial infarction, or stroke in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
-
49. A method of treating multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn'"'"'s disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto'"'"'s thyroiditis, Sjogren'"'"'s syndrome, autoimmune hyperthyroidism, Addison'"'"'s disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia greata, chronic actinic dermatitis, eczema, Behcet'"'"'s disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary'"'"'s syndrome, atopic dermatitis, systemic schlerosis, morphea or atopic dermatitis in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
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50. A method of treating colon carcinoma or thymoma in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
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52. A method of decreasing the level of one or more of TNF-α
- , IL-β
, IL-6 and IL-8 in a subject, the method comprising administering to the subject an effective dosage amount of a compound according to claim 11.
- , IL-β
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54. A method of treating rheumatoid spondylitis, gouty arthritis, adult respiratory distress syndrome (ARDS), anaphylaxis, muscle degeneration, cachexia, Reiter'"'"'s syndrome, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer'"'"'s disease, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, and myalgias due to infection, or which subject is infected by HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses (including HSV-1, HSV-2), or herpes zoster in a subject, the method comprising administering to the subject a pharmaceutical composition comprising an effective dosage amount of a compound according to claim 11.
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55. A method of manufacturing a medicament for the treatment of inflammation or cancer, the method comprising combining an effective dosage amount of a compound according to claim 11 with a pharmaceutically acceptable carrier to manufacture the medicament.
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56. A method of manufacturing a medicament for the inhibition of T cell activation and proliferation in a subject, the method comprising combining an effective dosage amount of a compound according to claim 11 with a pharmaceutically acceptable carrier to manufacture the medicament.
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57. A method of manufacturing a medicament for the treatment of arthritis, rheumatoid arthritis, psoriatic arthritis, or osteoarthritis in a subject, the method comprising combining an effective dosage amount of a compound according to claim 11 with a pharmaceutically acceptable carrier to manufacture the medicament.
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58. A method of manufacturing a medicament for the treatment of organ transplant, acute transplant or heterograft or homograft rejection, or transplantation tolerance induction in a subject, the method comprising combining an effective dosage amount of a compound according to claim 11 with a pharmaceutically acceptable carrier to manufacture the medicament.
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59. A method of manufacturing a medicament for the treatment of ischemic or reperfusion injury, myocardial infarction, or stroke in a subject, the method comprising combining an effective dosage amount of a compound according to claim 11 with a pharmaceutically acceptable carrier to manufacture the medicament.
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60. A method of manufacturing a medicament for the treatment of multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn'"'"'s disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto'"'"'s thyroiditis, Sjogren'"'"'s syndrome, autoimmune hyperthyroidism, Addison'"'"'s disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia greata, chronic actinic dermatitis, eczema, Behcet'"'"'s disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary'"'"'s syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, rheumatoid spondylitis, gouty arthritis, adult respiratory distress syndrome (ARDS), anaphylaxis, muscle degeneration, cachexia, Reiter'"'"'s syndrome, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer'"'"'s disease, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, and myalgias due to infection, or which subject is infected by HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses (including HSV-1, HSV-2), or herpes zoster, the method comprising combining an effective dosage amount of a compound according to claim 11 with a pharmaceutically acceptable carrier to manufacture the medicament.
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61. A method of manufacturing a medicament for the treatment of colon carcinoma or thymoma, the method comprising combining an effective dosage amount of a compound according to claim 11 with a pharmaceutically acceptable carrier to manufacture the medicament.
Specification