Indazolyl-substituted pyrroline compounds as kinase inhibitors
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Abstract
The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I):
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Citations
16 Claims
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1. A compound of Formula (I):
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)
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2. The compound of claim 1 wherein R1 and R2 are independently selected from the group consisting of:
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hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl {wherein alkyl, alkenyl and alkynyl are optionally substituted with one to two substituents independently selected from the group consisting of —
O—
(C1-4)alkyl, —
O—
(C1-4)alkyl-OH, —
O—
(C1-4)alkyl-O—
(C1-4)alkyl, —
O—
(C1-4)alkyl-NH2, —
O—
(C1-4)alkyl-NH—
(C1-4)alkyl, —
O—
(C1-4)alkyl-N[(C1-4)alkyl]2, —
O—
(C1-4)alkyl-S—
(C1-4)alkyl, —
O—
(C1-4)alkyl-SO2—
(C1-4)alkyl, —
O—
(C1-4)alkyl-SO2—
NH2, —
O—
(C1-4)alkyl-SO2—
NH—
(C1-4)alkyl, —
O—
(C1-4)alkyl-SO2—
N[(C1-4)alkyl]2, —
O—
C(O)H, —
O—
C(O)—
(C1-4)alkyl, —
O—
C(O)—
NH2, —
O—
C(O)—
NH—
(C1-4)alkyl, —
O—
C(O)—
N[(C1-4)alkyl]2, —
O—
(C1-4)alkyl-C(O)H, —
O—
(C1-4)alkyl-C(O)—
(C1-4)alkyl, —
O—
(C1-4)alkyl-CO2H, —
O—
(C1-4)alkyl-C(O)—
O—
(C1-4)alkyl, —
O—
(C1-4)alkyl-C(O)—
NH2, —
O—
(C1-4)alkyl-C(O)—
NH—
(C1-4)alkyl, —
O—
(C1-4)alkyl-C(O)—
N[(C1-4)alkyl]2, —
C(O)H, —
C(O)—
(C1-4)alkyl, —
CO2H, —
C(O)—
O—
(C1-4)alkyl, —
C(O)—
NH2, —
C(NH)—
NH2, —
C(O)—
NH—
(C1-4)alkyl, —
C(O)—
N[(C1-4)alkyl]2, —
SH, —
S—
(C1-4)alkyl, —
S—
(C1-4)alkyl-S—
(C1-4)alkyl, —
S—
(C1-4)alkyl-O—
(C1-4)alkyl, —
S—
(C1-4)alkyl-O—
(C1-4)alkyl-OH, —
S—
(C1-4)alkyl-O—
(C1-4)alkyl-NH2, —
S—
(C1-4)alkyl-O—
(C1-4)alkyl-NH—
(C1-4)alkyl, —
S—
(C1-4)alkyl-O—
(C1-4)alkyl-N[(C1-4)alkyl]2, —
S—
(C1-4)alkyl-NH—
(C1-4)alkyl, —
SO2—
(C1-4)alkyl, —
SO2—
NH2, —
SO2—
NH—
(C1-4)alkyl, —
SO2—
N[(C1-4)alkyl]2, amino (substituted with two substituents independently selected from the group consisting of hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, —
(C1-4)alkyl-OH, —
(C1-4)alkyl-O—
(C1-4)alkyl, —
(C1-4)alkyl-NH2, —
(C1-4)alkyl-NH—
(C1-4)alkyl, —
(C1-4)alkyl-N[(C1-4)alkyl]2, —
(C1-4)alkyl-S—
(C1-4)alkyl, —
C(O)—
(C1-4)alkyl, —
C(O)—
O—
(C1-4)alkyl, —
C(O)—
NH2, —
C(O)—
NH—
(C1-4)alkyl, —
C(O)—
N[(C1-4)alkyl]2, —
SO2—
(C1-4)alkyl, —
SO2—
NH2, —
SO2—
NH—
(C1-4)alkyl, —
SO2—
N[(C1-4)alkyl]2, —
C(N)—
NH2, aryl and aryl(C1-4)alkyl (wherein aryl is optionally substituted with one to three substituents independently selected from the group consisting of halogen, C1-4alkyl, C1-4alkoxy, amino (substituted with two substituents selected from the group consisting of hydrogen and C1-4alkyl), cyano, halo, (halo)1-3(C1-4)alkyl, (halo)1-3(C1-4)alkoxy, hydroxy, hydroxy(C1-4)alkyl and nitro)), cyano, (halo)1-3, hydroxy, nitro, oxo, heterocyclyl, aryl and heteroaryl (wherein heterocyclyl, aryl and heteroaryl are optionally substituted with one to three substituents independently selected from the group consisting of C1-4alkyl, C1-4alkoxy, amino (substituted with two substituents selected from the group consisting of hydrogen and C1-4alkyl), cyano, halo, (halo)1-3(C1-4)alkyl, (halo)1-3(C1-4)alkoxy, hydroxy, hydroxy(C1-4)alkyl and nitro)},—
C(O)—
(C1-4)alkyl, —
C(O)-aryl, —
C(O)—
O—
(C1-4)alkyl, —
C(O)—
O-aryl, —
C(O)—
NH—
(C1-4)alkyl, —
C(O)—
NH-aryl, —
C(O)—
N[(C1-4)alkyl]2, —
SO2—
(C1-4)alkyl, —
SO2-aryl,aryl and heteroaryl {wherein aryl and heteroaryl are optionally substituted with one to three substituents independently selected from the group consisting of C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, —
C(O)H, —
C(O)—
(C1-4)alkyl, —
CO2H, —
C(O)—
O—
(C1-4)alkyl, —
C(O)—
NH2, —
C(NH)—
NH2, —
C(O)—
NH—
(C1-4)alkyl, —
C(O)—
N[(C1-4)alkyl]2, —
SH, —
S—
(C1-4)alkyl, —
SO2—
(C1-4)alkyl, —
SO2—
NH2, —
SO2—
NH—
(C1-4)alkyl, —
SO2—
N[(C1-4)alkyl]2, amino (substituted with two substituents independently selected from the group consisting of hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, —
(C1-4)alkyl-NH2, —
C(O)—
(C1-4)alkyl, —
C(O)—
O—
(C1-4)alkyl, —
C(O)—
NH2, —
C(O)—
NH—
(C1-4)alkyl, —
C(O)—
N[(C1-4)alkyl]2, —
SO2—
(C1-4)alkyl, —
SO2—
NH2, —
SO2—
NH—
(C1-4)alkyl, —
SO2—
N[(C1-4)alkyl]2 and —
C(NH)—
NH2), amino-(C1-4)alkyl- (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, —
(C1-4)alkyl-NH2, —
C(O)—
(C1-4)alkyl, —
C(O)—
O—
(C1-4)alkyl, —
C(O)—
NH2, —
C(O)—
NH—
(C1-4)alkyl, —
C(O)—
N[(C1-4)alkyl]2, —
SO2—
(C1-4)alkyl, —
SO2—
NH2, —
SO2—
NH—
(C1-4)alkyl, —
SO2—
N[(C1-4)alkyl]2 and —
C(NH)—
NH2), cyano, halo, (halo)1-3(C1-4)alkyl, (halo)1-3(C1-4)alkoxy, hydroxy, hydroxy(C1-4)alkyl, nitro, aryl, —
(C1-4)alkyl-aryl, heteroaryl and —
(C1-4)alkyl-heteroaryl};
with the proviso that if R2 is selected from the group consisting of hydrogen, unsubstituted C1-4alkyl and —
(C1-4)alkyl-(halo)1-3, then R1 is selected from the group consisting of other than hydrogen, C1-4alkyl, aryl (limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo, unsubstituted C1-4alkyl, hydroxy, C1-4alkoxy, (halo)1-3(C1-4)alkyl, nitro, unsubstituted amino and cyano), —
(C1-4)alkyl-aryl (wherein aryl is limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo, unsubstituted C1-4alkyl, hydroxy, C1-4alkoxy, (halo)1-3(C1-4)alkyl, nitro, unsubstituted amino and cyano), —
(C1-4)alkyl(C1-4)alkoxy, —
(C1-4)alkyl-hydroxy, —
(C1-4)alkyl-(halo)1-3, —
(C1-4)alkyl-amino (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen and —
C1-4alkyl), —
(C1-4)alkyl-amino(C1-4)alkylamino, —
C1-4alkyl-NH—
C(O)—
(C1-4)alkyl, —
C1-4alkyl-NH—
SO2—
(C1-4)alkyl, —
(C1-4)alkyl-SH, —
(C1-4)alkyl-S—
(C1-4)alkyl, —
(C1-4)alkyl-SO2—
(C1-4)alkyl, —
(C1-4)alkyl-O—
C(O)—
(C1-4)alkyl, —
(C1-4)alkyl-C(N), —
(C1-4)alkyl-C(NH)—
NH2, —
(C1-4)alkyl-CO2H, —
(C1-4)alkyl-C(O)—
O—
(C1-4)alkyl, —
(C1-4)alkyl-C(O)—
NH2, —
(CH2)24-heterocyclyl, —
(CH2)2-4-T-C(V)-Z (wherein T is NH, V is O and Z is amino (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl))with the provision that for R1 and R2 heteroaryl shall mean pyridinyl, quinolinyl or isoquinolinyl.
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3. The compound of claim 1 wherein R1 and R2 are independently selected from the group consisting of:
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hydrogen, C1-4alkyl, C2-4alkenyl {wherein alkyl is substituted with one to two substituents independently selected from the group consisting of —
O—
(C1-4)alkyl, —
O—
(C1-4)alkyl-OH, —
O—
(C1-4)alkyl-NH—
(C1-4)alkyl, —
O—
C(O)—
(C1-4)alkyl, —
C(O)H, —
CO2H, —
C(O)—
O—
(C1-4)alkyl, amino (substituted with two substituents independently selected from the group consisting of hydrogen, C1-4alkyl, —
(C1-4)alkyl-OH, —
C(O)—
O—
(C1-4)alkyl and aryl(C1-4)alkyl), hydroxy, heterocyclyl, aryl and heteroaryl (wherein heterocyclyl, aryl and heteroaryl are optionally substituted with one to three substituents independently selected from the group consisting of C1-4alkyl and halo)},aryl and heteroaryl {wherein aryl and heteroaryl are optionally substituted with one to two substituents independently selected from the group consisting of C1-4alkyl, C1-4alkoxy, amino (substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl), cyano, halo, (halo)1-3(C1-4)alkyl, (halo)1-3(C1-4)alkoxy, hydroxy, hydroxy(C1-4)alkyl, aryl and heteroaryl};
with the proviso that if R2 is selected from the group consisting of hydrogen and unsubstituted C1-4alkyl, then R1 is selected from the group consisting of other than hydrogen, C1-4alkyl, aryl (limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo, unsubstituted C1-4alkyl, hydroxy, C1-4alkoxy, (halo)1-3(C1-4)alkyl, unsubstituted amino and cyano), —
(C1-4)alkyl-aryl (wherein aryl is limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo and unsubstituted C1-4alkyl), —
(C1-4)alkyl(C1-4)alkoxy, —
(C1-4)alkyl-hydroxy, —
(C1-4)alkyl-amino (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen and —
C1-4alkyl), —
(C1-4)alkyl-O—
C(O)—
(C1-4)alkyl, —
(C1-4)alkyl-CO2H, —
(C1-4)alkyl-C(O)—
O—
(C1-4)alkyl and —
(CH2)24-heterocyclyl,with the provision that for R1 and R2 heteroaryl shall mean pyridinyl, quinolinyl or isoquinolinyl.
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4. The compound of claim 1 wherein R1 is selected from the group consisting of:
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hydrogen, C1-4alkyl, C2-4alkenyl {wherein alkyl is substituted with one to two substituents independently selected from the group consisting of —
O—
(C1-4)alkyl-NH—
(C1-4)alkyl, amino (substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl), hydroxy, heterocyclyl, aryl and heteroaryl (wherein heterocyclyl, aryl and heteroaryl are optionally substituted with one to three substituents independently selected from the group consisting of C1-4alkyl and halo)},aryl and heteroaryl (wherein aryl and heteroaryl are optionally substituted with one to two substituents independently selected from the group consisting of C1-4alkyl, C1-4alkoxy, amino (substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl), cyano, halo, (halo)1-3(C1-4)alkyl, (halo)1-3(C1-4)alkoxy, hydroxy, hydroxy(C1-4)alkyl, aryl and heteroaryl};
with the proviso that if R2 is selected from the group consisting of hydrogen, unsubstituted C1-4alkyl and —
(C1-4)alkyl-(halo)1-3, then R1 is selected from the group consisting of other than hydrogen, C1-4alkyl, aryl (limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo, unsubstituted C1-4alkyl, hydroxy, C1-4alkoxy, (halo)1-3(C1-4)alkyl, unsubstituted amino and cyano), —
(C1-4)alkyl-aryl (wherein aryl is limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo and unsubstituted C1-4alkyl), —
(C1-4)alkyl-hydroxy, —
(C1-4)alkyl-amino (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl) and —
(CH2)24-heterocyclyl;
with the provision that for R1 and R2 heteroaryl shall mean pyridinyl, quinolinyl or isoquinolinyl.
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5. The compound of claim 1 wherein R1 is selected from the group consisting of:
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hydrogen, C1-4alkyl, C2-3alkenyl {wherein alkyl is substituted with one to two substituents independently selected from the group consisting of —
O—
(C1-4)alkyl-NH—
(C1-4)alkyl, amino (substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl), hydroxy, pyrrolidinyl, morpholinyl, piperazinyl (wherein piperazinyl is optionally substituted with methyl), phenyl, naphthalenyl and quinolinyl (wherein phenyl and benzo[b]thienyl are optionally substituted with one to two chloro substituents)},phenyl, naphthalenyl, pyridinyl, quinolinyl and isoquinolinyl (wherein phenyl, naphthalenyl and pyridinyl are optionally substituted with one to two substituents independently selected from the group consisting of C1-4alkyl, C1-4alkoxy, halo and hydroxy; and
, wherein phenyl is optionally substituted with one substituent selected from the group consisting of phenyl and thienyl);
with the proviso that if R2 is selected from the group consisting of hydrogen, unsubstituted C1-4alkyl and —
(C1-4)alkyl-(halo)1-3, then R1 is selected from the group consisting of other than hydrogen, C1-4alkyl, phenyl (wherein phenyl is unsubstituted or substituted with one or more substituents selected from the group consisting of halo, unsubstituted C1-4alkyl, hydroxy and C1-4alkoxy), —
(C1-4)alkyl-phenyl (wherein phenyl is unsubstituted or substituted with one or more chloro substituents), —
(C1-4)alkyl-hydroxy, —
(C1-4)alkyl-amino (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl) and —
(CH2)2-4-heterocyclyl,with the provision that for R1 and R2 heteroaryl shall mean pyridinyl, quinolinyl or isoquinolinyl.
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6. The compound of claim 1 wherein R2 is selected from the group consisting of:
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hydrogen, C1-4alkyl {wherein alkyl is substituted with one to two substituents independently selected from the group consisting of —
O—
(C1-4)alkyl, —
O—
(C1-4)alkyl-OH, —
O—
(C1-4)alkyl-NH—
(C1-4)alkyl, —
O—
C(O)—
(C1-4)alkyl, —
C(O)H, —
CO2H, —
C(O)—
O—
(C1-4)alkyl, amino (substituted with two substituents independently selected from the group consisting of hydrogen, C1-4alkyl, —
(C1-4)alkyl-OH, —
C(O)—
O—
(C1-4)alkyl and aryl(C1-4)alkyl), hydroxy and heterocyclyl (wherein heterocyclyl is optionally substituted with one to two C1-4alkyl substituents)} and heteroaryl;
with the proviso that if R2 is selected from the group consisting of hydrogen and unsubstituted C1-4alkyl, then R1 is selected from the group consisting of other than hydrogen, C1-4alkyl, aryl (limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo, unsubstituted C1-4alkyl, hydroxy, C1-4alkoxy, (halo)1-3(C1-4)alkyl, nitro, unsubstituted amino and cyano), —
(C1-4)alkyl-aryl (wherein aryl is limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo, unsubstituted C1-4alkyl, hydroxy, C1-4alkoxy, (halo)1-3(C1-4)alkyl, nitro, unsubstituted amino and cyano), —
(C1-4)alkyl(C1-4)alkoxy, —
(C1-4)alkyl-hydroxy, —
(C1-4)alkyl-(halo)1-3, —
(C1-4)alkyl-amino (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl), —
(C1-4)alkyl-amino(C1-4)alkylamino, —
C1-4alkyl-NH—
C(O)—
(C1-4)alkyl, —
C1-4alkyl-NH—
SO2—
(C1-4)alkyl, —
(C1-4)alkyl-SH, —
(C1-4)alkyl-S—
(C1-4)alkyl, —
(C1-4)alkyl-SO2—
(C1-4)alkyl, —
(C1-4)alkyl-O—
C(O)—
(C1-4)alkyl, —
(C1-4)alkyl-C(N), —
(C1-4)alkyl-C(NH)—
NH2, —
(C1-4)alkyl-CO2H, —
(C1-4)alkyl-C(O)—
O—
(C1-4)alkyl, —
(C1-4)alkyl-C(O)—
NH2, —
(CH2)24-heterocyclyl, —
(CH2)2-4-T-C(V)-Z (wherein T is NH, V is O and Z is amino (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl));
with the provision that for R1 and R2 heteroaryl shall mean pyridinyl, quinolinyl or isoquinolinyl.
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7. The compound of claim 1 wherein R2 is selected from the group consisting of:
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hydrogen, C1-4alkyl {wherein alkyl is substituted with one to two substituents independently selected from the group consisting of —
O—
(C1-4)alkyl, —
O—
(C1-4)alkyl-OH, —
O—
(C1-4)alkyl-NH—
(C1-4)alkyl, —
O—
C(O)—
(C1-4)alkyl, —
C(O)H, —
CO2H, —
C(O)—
O—
(C1-4)alkyl, amino (substituted with two substituents independently selected from the group consisting of hydrogen, C1-4alkyl, —
(C1-4)alkyl-OH, —
C(O)—
O—
(C1-4)alkyl and phenyl(C1-4)alkyl), hydroxy, pyrrolidinyl, 1,3-dioxolanyl, morpholinyl and piperazinyl (wherein piperazinyl is optionally substituted with methyl)} and pyridinyl;
with the proviso that if R2 is selected from selected from the group consisting of hydrogen and unsubstituted C1-4alkyl, then R1 is selected from the group consisting of other than hydrogen, C1-4alkyl, aryl (limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo, unsubstituted C1-4alkyl, hydroxy, C1-4alkoxy, (halo)1-3(C1-4)alkyl, nitro, unsubstituted amino and cyano), —
(C1-4)alkyl-aryl (wherein aryl is limited to phenyl unsubstituted or substituted with one or more substituents selected from the group consisting of halo, unsubstituted C1-4alkyl, hydroxy, C1-4alkoxy, (halo)1-3(C1-4)alkyl, nitro, unsubstituted amino and cyano), —
(C1-4)alkyl(C1-4)alkoxy, —
(C1-4)alkyl-hydroxy, —
(C1-4)alkyl-(halo)1-3, —
(C1-4)alkyl-amino (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl), —
(C1-4)alkyl-amino(C1-4)alkylamino, —
C1-4alkyl-NH—
C(O)—
(C1-4)alkyl, —
C1-4alkyl-NH—
SO2—
(C1-4)alkyl, —
(C1-4)alkyl-SH, —
(C1-4)alkyl-S—
(C1-4)alkyl, —
(C1-4)alkyl-SO2—
(C1-4)alkyl, —
(C1-4)alkyl-O—
C(O)—
(C1-4)alkyl, —
(C1-4)alkyl-C(N), —
(C1-4)alkyl-C(NH)—
NH2, —
(C1-4)alkyl-CO2H, —
(C1-4)alkyl-C(O)—
O—
(C1-4)alkyl, —
(C1-4)alkyl-C(O)—
NH2, —
(CH2)24-heterocyclyl, —
(CH2)24-T-C(V)-Z (wherein T is NH, V is O and Z is amino (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen and C1-4alkyl));
with the provision that for R1 and R2 heteroaryl shall mean pyridinyl, quinolinyl or isoquinolinyl.
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8. The compound of claim 1 wherein R3 and R4 are independently selected from the group consisting of hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, —
- C(O)H, —
C(O)—
(C1-4)alkyl, —
CO2H, —
C(O)—
O—
(C1-4)alkyl, —
C(O)—
NH2, —
C(NH)—
NH2, —
C(O)—
NH—
(C1-4)alkyl, —
C(O)—
N[(C1-4)alkyl]2, —
SH, —
S—
(C1-4)alkyl, —
SO2—
(C1-4)alkyl, —
SO2—
NH2, —
SO2—
NH—
(C1-4)alkyl, —
SO2—
N[(C1-4)alkyl]2, amino (substituted with two substituents independently selected from the group consisting of hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, —
(C1-4)alkyl-NH2, —
C(O)—
(C1-4)alkyl, —
C(O)—
O—
(C1-4)alkyl, —
C(O)—
NH2, —
C(O)—
NH—
(C1-4)alkyl, —
C(O)—
N[(C1-4)alkyl]2, —
SO2—
(C1-4)alkyl, —
SO2—
NH2, —
SO2—
NH—
(C1-4)alkyl, —
SO2—
N[(C1-4)alkyl]2 and —
C(NH)—
NH2), amino-(C1-4)alkyl- (wherein amino is substituted with two substituents independently selected from the group consisting of hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, —
(C1-4)alkyl-NH2, —
C(O)—
(C1-4)alkyl, —
C(O)—
O—
(C1-4)alkyl, —
C(O)—
NH2, —
C(O)—
NH—
(C1-4)alkyl, —
C(O)—
N[(C1-4)alkyl]2, —
SO2—
(C1-4)alkyl, —
SO2—
NH2, —
SO2—
NH—
(C1-4)alkyl, —
SO2—
N[(C1-4)alkyl]2 and —
C(NH)—
NH2), cyano, halo, (halo)1-3(C1-4)alkyl, (halo)1-3(C1-4)alkoxy, hydroxy, hydroxy(C1-4)alkyl, nitro, aryl, and —
(C1-4)alkyl-aryl.
- C(O)H, —
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9. The compound of claim 1 wherein R3 and R4 are independently selected from the group consisting of hydrogen, C1-4alkyl, C1-4alkoxy, cyano and halogen.
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10. The compound of claim 1 wherein R3 and R4 are independently selected from the group consisting of hydrogen, methyl, methoxy, cyano and chloro.
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11. The compound of claim 1 wherein Y and Z are independently selected from the group consisting of O and (H,H);
- with the proviso that one of Y and Z is O, and the other is selected from the group consisting of O and (H,H).
-
12. The compound of claim 1 wherein R5 is selected from the group consisting of:
-
hydrogen, halogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl {wherein alkyl, alkenyl and alkynyl are optionally substituted with one to two substituents independently selected from the group consisting of amino (substituted with two substituents selected from the group consisting of hydrogen and C1-4alkyl), cyano, halo, hydroxy, nitro, oxo, and aryl}, aryl and heteroaryl {wherein aryl is optionally substituted with one to two substituents independently selected from the group consisting of C1-4alkyl, C1-4alkoxy, amino (substituted with two substituents selected from the group consisting of hydrogen and C1-4alkyl), cyano, halo, hydroxy and nitro}.
-
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13. The compound of claim 1 wherein R5 is selected from the group consisting of C1-4alkyl and aryl.
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14. The compound of claim 1 wherein R5 is selected from the group consisting of methyl and naphthalenyl.
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15. The compound of claim 1 wherein the compound of Formula (I) is a compound selected from Formula (Ic):
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16. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
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2. The compound of claim 1 wherein R1 and R2 are independently selected from the group consisting of:
Specification
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Current AssigneeOrtho-McNeil-Janssen Pharmaceuticals Incorporated (Johnson & Johnson)
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Original AssigneeOrtho-McNeil-Janssen Pharmaceuticals Incorporated (Johnson & Johnson)
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InventorsHecker, Leonard, McComsey, David, Ye, Hong, Zhang, Han-Cheng, White, Kimberly, Maryanoff, Bruce, Conway, Bruce
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Granted Patent
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Time in Patent OfficeDays
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Field of Search
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US Class Current514/406
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CPC Class CodesA61P 11/06 AntiasthmaticsA61P 17/00 Drugs for dermatological di...A61P 17/06 AntipsoriaticsA61P 25/00 Drugs for disorders of the ...A61P 25/04 Centrally acting analgesics...A61P 25/18 Antipsychotics, i.e. neurol...A61P 25/28 for treating neurodegenerat...A61P 29/00 Non-central analgesic, anti...A61P 3/10 for hyperglycaemia, e.g. an...A61P 31/18 for HIVA61P 35/00 Antineoplastic agentsA61P 37/00 Drugs for immunological or ...A61P 43/00 Drugs for specific purposes...A61P 9/00 Drugs for disorders of the ...A61P 9/10 for treating ischaemic or a...A61P 9/12 AntihypertensivesC07D 401/14 containing three or more he...C07D 403/14 containing three or more he...C07D 405/14 containing three or more he...C07D 409/14 containing three or more he...