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Organic Compounds and Their Uses

  • US 20100069368A1
  • Filed: 03/13/2008
  • Published: 03/18/2010
  • Est. Priority Date: 03/15/2007
  • Status: Active Grant
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First Claim
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1. A compound of Formula I:

  • and pharmaceutically acceptable salts thereof, whereinR1 is phenyl which may be unsubstituted or substituted;

    R2 is het with at least one heteroring atom being N, and which may be unsubstituted or substituted;

    L is lower alkyl, (CH2)1-2-A, A-(CH2)1-2, or CH2-A-CH2, and A is O, S, NH, or N-alkyl, wherein lower alkyl may be unsubstituted or substituted with lower alkyl, or one or more fluorines;

    X is N or CH, and at least one X is N;

    Y is a bond, CH2, C(O), or SO2;

    R3 is aryl or het, which is substituted;

    Z is H, lower alkyl, lower alkoxy, oxo, C(O)OR6, or —

    CN;

    in which lower alkyl and lower alkoxy may be unsubstituted or substituted with one or more halo, —

    OH, —

    CN, —

    NH2, or oxo, and two Z connected to the same atom can form a cycloalkyl ring, and m is 0 to 3;

    substitutions of phenyl, aryl or het of R1, R2, or R3 may be one or more of alkyl, cycloalkyl, alkoxy, cycloalkoxy, halo, —

    CN, oxo, aryl, carbalkoxy, OCF3, CF3, OH, —

    C(O)N(R6)2, C(O)R6, —

    C(O)OR6, —

    N(R6)2, —

    NHC(O)R6, —

    SO2(R6), —

    SO2N(R6)2;

    CH2OC(O)N(R6)2, —

    CH2N(R6)2, —

    NHC(O)OR6, NHC(O)N(R6)2, —

    CH2NHC(O)R6, CH2NHC(O)N(R6)2, CH2NHSO2(R6), CH2NHC(O)OR6—

    OC(O)R6, NHC(O)R6, O-aryl, het, or O-het, in which alkyl, het, cycloalkyl, cycloalkoxy, N(R6)2, aryl, carbalkoxy, and alkoxy can be unsubstituted or substituted with one or more halo, —

    OCH3, —

    OCF3, —

    OH, —

    NH2, alkyl, OR6, oxo, —

    N(H)0-2—

    R6, —

    CN, —

    C(O)N(R6)2, C(O)R6, C(O)OR6, —

    N(R6)2, NHC(O)R6, —

    SO2(R6), SO2N(R6)2, OSO2R6, —

    CH2N(R6)2, —

    CH2NHC(O)R6, —

    OC(O)R6, aryl, NHC(O)(R6), O-aryl, het, O-het, or cycloalkyl;

    R6 is H, alkyl, alkenyl, aryl, het, or two R6 on one atom may form cycloalkyl, aryl, or het; and

    alkyl, alkenyl, aryl, het, cycloalkyl, or het may be unsubstituted or substituted by OH, oxo, alkoxy, NR6, Nalkyl, acyl, aryl or het group;

    het is a 5-7 membered monocyclic heterocyclic ring which may be aromatic or non-aromatic, containing 1-4 heteroring atoms selected from N, O, and S;

    or an 8-12 membered fused ring system that includes at least one 5-7 membered heterocyclic ring which may be aromatic or non-aromatic, containing 1, 2, or 3 heteroring atoms selected from N, O and S, which het is unsubstituted or substituted;

    aryl is an aromatic radical having 6 to 14 ring carbon atoms, and no ring heteroatoms, in which said aryl group may be monocyclic or fused bicyclic or tricyclic, which may be unsubstituted or substituted by one or more substituents; and

    n is 0, 1, 2, or 3.

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