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    • 3. 发明申请
    • INDOLE DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS
    • 内含衍生物作为内皮素受体拮抗剂有用
    • WO1997043260A1
    • 1997-11-20
    • PCT/EP1997001882
    • 1997-04-11
    • PFIZER INC.PFIZER LIMITEDRAWSON, David, JamesDACK, Kevin, NeilDICKINSON, Roger, PeterJAMES, Kim
    • PFIZER INC.PFIZER LIMITED
    • C07D209/18
    • C07D405/06C07D209/18C07D405/14C07D409/14C07D413/14
    • Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R and R are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl [optionally substituted by CO2H or CO2(C1-6 alkyl)], C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr , (CH2)mHet , (CH2)mCONR R , (CH2)mCO2R , O(CH2)qCO2R , (CH2)mCOR , (CH2)mOR , O(CH2)pOR , (CH2)mNR R , CO2(CH2)qNR R , (CH2)mCN, S(O)nR , SO2NR R , CONH(CH2)mAr or CONH(CH2)mHet ; R represents H, C1-6 alkyl, (CH2)pNR R , SO2R , SO2NR R , (CH2)mCOR , C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR R , (CH2)mCO2R , (CH2)pCN, (CH2)pR or (CH2)pOR ; R represents H or C1-6 alkyl; R represents H or OH; R represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R are fully defined herein and may independently represent Ar or Het ; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar , CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar , CONHSO2(CH2)qAr or CONHSO2(C1-6 alkyl); Ar independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het and Het independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.
    • 式(I)化合物及其药学上可接受的衍生物,其中R 1和R 2是任选的取代基并且独立地表示C 1-6烷基,C 2-6烯基[任选被CO 2 H或CO 2(C 1-6烷基 )],C 2-6炔基,卤素,C 1-3全氟烷基,(CH 2)mAr 1,(CH 2)m Het 1,(CH 2)m CONR 7 R 8,(CH 2)m CO 2 R 8, ,O(CH 2)q CO 2 R 8,(CH 2)m COOR 8,(CH 2)mOR 8,O(CH 2)pOR 8,(CH 2)m NR 7 R 8,CO 2 )qNR 7 R 8,(CH 2)mCN,S(O)n R 8,SO 2 NR 7 R 8,CONH(CH 2)mAr 1或CONH(CH 2)m Het 1 ; R 3表示H,C 1-6烷基,(CH 2)p NR R 10,SO 2 R 10,SO 2 NR 9 R 10,(CH 2)m COR 10,C 2-6烯基 ,C 2-6炔基,(CH 2)m CONR 9 R 10,(CH 2)m CO 2 R 10,(CH 2)pCN,(CH 2)p R 10或(CH 2)pOR 10; R 4表示H或C 1-6烷基; R 5表示H或OH; R 6表示任选地与杂环稠合的苯基,该基团整体上任选被取代; R 7-10>全部定义,并且可以独立地表示Ar 2或Het 2; Z表示CO 2 H,CONH(四唑-5-基),CONHSO 2 O(C 1-4烷基),CO 2 Ar 3,CO 2(C 1-6烷基),四唑-5-基,CONHSO 2 Ar 3,CONHSO 2(CH 2)qAr 3或CONHSO 2(C 1-6烷基); Ar <1-3>独立地表示苯基,萘基或芳族杂环,这些基团任选地稠合并任选被取代; Het 1和Het 2独立地表示任选被取代的非芳族杂环; 可用于治疗再狭窄,肾衰竭和肺动脉高压。