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    INDOLE DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS
    1.
    发明公开
    INDOLE DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS 失效
    吲哚衍生物作为内皮素受体拮抗剂USED

    公开(公告)号：EP0901470A1

    公开(公告)日：1999-03-17

    申请号：EP97920690.0

    申请日：1997-04-11

    申请人： PFIZER INC. ,  Pfizer Limited

    发明人： RAWSON, David, James ,  DACK, Kevin, Neil ,  DICKINSON, Roger, Peter ,  JAMES, Kim

    IPC分类号： A61K31 ,  A61P9 ,  A61P11 ,  A61P13 ,  A61P15 ,  A61P43 ,  C07D209 ,  C07D405 ,  C07D409 ,  C07D413

    CPC分类号： C07D405/06 ,  C07D209/18 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

    摘要： Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R?1 and R2¿ are optional substituents and independently represent C¿1-6? alkyl, C2-6 alkenyl [optionally substituted by CO2H or CO2(C1-6 alkyl)], C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr?1, (CH¿2)mHet1, (CH2)mCONR?7R8, (CH¿2)mCO2R8, O(CH¿2?)qCO2R?8, (CH¿2)mCOR8, (CH2)mOR8, O(CH¿2?)pOR?8, (CH¿2)mNR7R8, CO2(CH2)qNR?7R8, (CH¿2)mCN, S(O)nR8, SO2NR7R8, CONH(CH¿2)mAr?1 or CONH(CH¿2?)mHet?1; R3¿ represents H, C¿1-6? alkyl, (CH2)pNR?9R10, SO¿2R10, SO2NR?9R10, (CH¿2)mCOR10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR?9R10, (CH¿2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH¿2?)pOR?10; R4¿ represents H or C¿1-6? alkyl; R?5¿ represents H or OH; R6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar?2 or Het2¿; Z represents CO¿2?H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar?3, CO¿2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO¿2?(CH2)qAr?3¿ or CONHSO¿2?(C1-6 alkyl); Ar?1-3¿ independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het1 and Het2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.

    INDOLE DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS
    6.
    发明授权
    INDOLE DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS 失效
    吲哚衍生物作为内皮素受体拮抗剂USED

    公开(公告)号：EP0901470B1

    公开(公告)日：2004-03-31

    申请号：EP97920690.1

    申请日：1997-04-11

    申请人： PFIZER INC. ,  Pfizer Limited

    发明人： RAWSON, David, James ,  DACK, Kevin, Neil ,  DICKINSON, Roger, Peter ,  JAMES, Kim

    IPC分类号： C07D209/18 ,  C07D405/06 ,  A61K31/40

    CPC分类号： C07D405/06 ,  C07D209/18 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

    摘要： Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R?1 and R2¿ are optional substituents and independently represent C¿1-6? alkyl, C2-6 alkenyl [optionally substituted by CO2H or CO2(C1-6 alkyl)], C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr?1, (CH¿2)mHet1, (CH2)mCONR?7R8, (CH¿2)mCO2R8, O(CH¿2?)qCO2R?8, (CH¿2)mCOR8, (CH2)mOR8, O(CH¿2?)pOR?8, (CH¿2)mNR7R8, CO2(CH2)qNR?7R8, (CH¿2)mCN, S(O)nR8, SO2NR7R8, CONH(CH¿2)mAr?1 or CONH(CH¿2?)mHet?1; R3¿ represents H, C¿1-6? alkyl, (CH2)pNR?9R10, SO¿2R10, SO2NR?9R10, (CH¿2)mCOR10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR?9R10, (CH¿2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH¿2?)pOR?10; R4¿ represents H or C¿1-6? alkyl; R?5¿ represents H or OH; R6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar?2 or Het2¿; Z represents CO¿2?H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar?3, CO¿2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO¿2?(CH2)qAr?3¿ or CONHSO¿2?(C1-6 alkyl); Ar?1-3¿ independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het1 and Het2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.