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    Indole derivatives useful as endothelin receptor antagonists
    2.
    发明授权
    Indole derivatives useful as endothelin receptor antagonists 失效
    用作内皮素受体拮抗剂的吲哚衍生物

    公开(公告)号：US06306852B1

    公开(公告)日：2001-10-23

    申请号：US09556651

    申请日：2000-04-24

    申请人： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

    发明人： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

    IPC分类号： A61P910

    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 R1 and R2 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)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a herterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 or CONHSO2(C1-4 alkyl); Ar1-3 indenpendently 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.

    摘要翻译： 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任选被CO 2 H或CO 2（C 1-6烷基）取代的C 1-6烷基，C 2-6烯基，C 2-6炔基 ，（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，C 1 -C 3全氟烷基，（CH 2）mr 1，（CH 2）m Het1，（CH 2）m CONR 7 R 8， （CH2）mNR7R8，CO2（CH2）qNR7R8，（CH2）mCN，S（O）nR8，SO2NR7R8，CONH（CH2）mAr1或CONH（CH2）mHet1; R3表示H，C1-6烷基，（CH2）pNR9R10，SO2R10，SO2NR9R10，（CH2）mCO2R10，C2-6烯基，C2-6炔基，（CH2）

    Indole derivatives useful as endothelin receptor antagonists
    3.
    发明授权
    Indole derivatives useful as endothelin receptor antagonists 失效
    用作内皮素受体拮抗剂的吲哚衍生物

    公开(公告)号：US06384070B2

    公开(公告)日：2002-05-07

    申请号：US09756835

    申请日：2001-01-09

    申请人： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

    发明人： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

    IPC分类号： A61K314025

    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 R1 and R2 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)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 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 Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 or CONHSO2(C1-4 alkyl); Ar1-3 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.

    摘要翻译： 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任选被CO 2 H或CO 2（C 1-6烷基）取代的C 1-6烷基，C 2-6烯基，C 2-6炔基 ，（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，C 1 -C 3全氟烷基，（CH 2）mr 1，（CH 2）m Het1，（CH 2）m CONR 7 R 8， （CH2）mNR7R8，CO2（CH2）qNR7R8，（CH2）mCN，S（O）nR8，SO2NR7R8，CONH（CH2）mAr1或CONH（CH2）mHet1; R3表示H，C1-6烷基，（CH2）pNR9R10，SO2R10，SO2NR9R10，（CH2）mCO2R10，C2-6烯基，C2-6炔基，（CH2）

    Indole derivatives useful as endothelin receptor antagonists
    8.
    发明授权
    Indole derivatives useful as endothelin receptor antagonists 失效
    用作内皮素受体拮抗剂的吲哚衍生物

    公开(公告)号：US6136843A

    公开(公告)日：2000-10-24

    申请号：US414361

    申请日：1999-10-07

    申请人： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

    发明人： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

    IPC分类号： A61K31/40 ,  A61K31/405 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P13/08 ,  A61P13/12 ,  A61P15/00 ,  A61P43/00 ,  C07D209/18 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

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

    摘要： ##STR1## Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R
    1 and R
    2 are optional substituents and independently represent C
    1-6 alkyl, C
    2-6 alkenyl optionally substituted by CO
    2 H or CO
    2 (C
    1-6 alkyl, C
    2-6 alkynyl, halogen, C
    1-3 perfluoroalkyl, (CH
    2 )
    m Ar
    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 COR
    8 , (CH
    2 )
    m OR
    8 , O(CH
    2 )
    p OR
    8 , (CH
    2 )
    m NR
    7 R
    8 , CO
    2 (CH
    2 )
    q NR
    7 R
    8 , (CH
    2 )
    m CN, S(O)
    n R
    8 , SO
    2 NR
    7 R
    8 , CONH(CH
    2 )
    m Ar
    1 or CONH(CH
    2 )
    m Het
    1 ; R
    3 represents H, C
    1-6 alkyl, (CH
    2 )
    p CONR
    9 R
    10 , SO
    2 R
    10 , SO
    2 NR
    9 R
    10 , (CH
    2 )
    m COR
    10 , C
    2-6 alkenyl, C
    2-6 alkynyl, (CH
    2 )
    m CONR
    9 R
    10 , (CH
    2 )
    m CO
    2 R
    10 , (CH
    2 )
    p CN, (CH
    2 )
    p R
    10 or (CH
    2 )
    p OR
    10 ; R
    4 represents H or C
    1-6 alkyl; R
    5 represents H or OH; R
    6 represents phenyl optionally fused to a heterocylic ring, the group as a whole being optionally substituted; R
    7-10 are fully defined herein and may independently represent Ar
    2 or Het
    2 ; Z represents CO
    2 H, CONH(tetrazol-5-yl), CONHSO
    2 O(C
    1-4 alkyl), CO
    2 Ar
    3 , CO
    2 (C
    1-6 alkyl), tetrazol-5-yl, CONHSO
    2 Ar
    3 , CONHSO
    2 (CH
    2 )
    q Ar
    3 or CONHSO
    2 (C
    1-6 alkyl); Ar
    1-3 independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het
    1 and Het
    2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.

    摘要翻译： 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，任选被CO 2 H或CO 2取代的C 2-6烯基（C 1-6烷基，C 2-6炔基，卤素 ，（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 CO 2 R 8， ）mNR7R8，CO2（CH2）qNR7R8，（CH2）mCN，S（O）nR8，SO2NR7R8，CONH（CH2）mAr1或CONH（CH2）mHet1; R3表示H，C1-6烷基，（CH2）pCONR9R10，SO2R10， SO2NR9R10，（CH2）mCOR10，C2-6烯基，C2-6炔基，（CH2）m CONR9R10，（CH2）mCO2R10，（CH2）pCN，（CH2）pR10或（CH2）pOR10; R4表示H或C1-6 烷基; R 5表示H或OH; R 6表示任选地与杂环的稠合的苯基，该基团整体上可以被取代; R 7-10在本文中是完全定义的，可独立地表示Ar 2或Het 2; Z代表CO 2 H，CONH（四唑 - （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）q A r3或CONHSO2（C1-6烷基）; Ar1-3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; Het1和Het2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。

    Indole derivatives useful as endothelin receptor antagonists
    9.
    发明授权
    Indole derivatives useful as endothelin receptor antagonists 失效
    用作内皮素受体拮抗剂的吲哚衍生物

    公开(公告)号：US6017945A

    公开(公告)日：2000-01-25

    申请号：US147096

    申请日：1998-10-05

    申请人： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

    发明人： David James Rawson ,  Kevin Neil Dack ,  Roger Peter Dickinson ,  Kim James

    IPC分类号： A61K31/40 ,  A61K31/405 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P13/08 ,  A61P13/12 ,  A61P15/00 ,  A61P43/00 ,  C07D209/18 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D405/02

    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.sup.1 and R.sup.2 are optional substituents and independently represent C.sub.1-6 alkyl, C.sub.2-6 alkenyl [optionally substituted by CO.sub.2 H or CO.sub.2 (C.sub.1-6 alkyl)], C.sub.2-6 alkynyl, halogen, C.sub.1-3 perfluoroalkyl, (CH.sub.2).sub.m Ar.sup.1, (CH.sub.2).sub.m Het.sup.1, (CH.sub.2).sub.m CONR.sup.7 R.sup.8, (CH.sub.2).sub.m CO.sub.2 R.sup.8, O(CH.sub.2).sub.q CO.sub.2 R.sup.8, (CH.sub.2).sub.m COR.sup.8, (CH.sub.2).sub.m OR.sup.8, O(CH.sub.2).sub.p OR.sup.8, (CH.sub.2).sub.m NR.sup.7 R.sup.8, CO.sub.2 (CH.sub.2).sub.q NR.sup.7 R.sup.8, (CH.sub.2).sub.m CN, S(O).sub.n R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, CONH(CH.sub.2).sub.m Ar.sup.1 or CONH(CH.sub.2).sub.m Het.sup.1 ; R.sup.3 represents H, C.sub.1-6, alkyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, SO.sub.2 R.sup.10, SO.sub.2 NR.sup.9 R.sup.10, (CH.sub.2).sub.m COR.sup.10, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, (CH.sub.2).sub.m CONR.sup.9 R.sup.10, (CH.sub.2).sub.m CO.sub.2 R.sup.10, (CH.sub.2).sub.p CN, (CH.sub.2).sub.p R.sup.10 or (CH.sub.2).sub.p OR.sup.10 ; R.sup.4 represents H or C.sub.1-6 alkyl; R.sup.5 represents H or OH; R.sup.6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R.sup.7-10 are fully defined herein and may independently represent Ar.sup.2 or Het.sup.2 ; Z represents CO.sub.2 H, CONH(tetrazol-5-yl), CONHSO.sub.2 O(C.sub.1-4 alkyl), CO.sub.2 Ar.sup.3, CO.sub.2 (C.sub.1-6 alkyl), tetrazol-5-yl, CONHSO.sub.2 Ar.sup.3, CONHSO.sub.2 (CH.sub.2).sub.q Ar.sup.3 or CONHSO.sub.2 (C.sub.1-6 alkyl); Ar.sup.1-3 independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het.sup.1 and Het.sup.2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.

    摘要翻译： PCT No.PCT / EP97 / 01882 Sec。 371日期：1998年10月5日 102（e）日期1998年10月5日PCT 1997年4月11日PCT PCT。 公开号WO97 / 43260 PCT 日期1997年11月20日式（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） ，（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）m OR 8， O（CH2）pOR8，（CH2）mNR7R8，CO2（CH2）qNR7R8，（CH2）mCN，S（O）nR8，SO2NR7R8，CONH（CH2）mAr1或CONH（CH2）mHet1; R3代表H，C1-6，烷基，（CH2）pNR9R10，SO2R10，SO2NR9R10，（CH2）mCOR10，C2-6烯基，C2-6炔基，（CH2）mCONR9R10，（CH2）mCO2R10，（CH2） CH2）pR10或（CH2）pOR10; R 4表示H或C 1-6烷基; R5表示H或OH; R6表示任选地与杂环稠合的苯基，该基团作为整体任选被取代; 本文完全定义R7-10，并且可以独立地表示Ar2或Het2; 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 ）; Ar1-3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; Het1和Het2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。