利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

42 条记录 (耗时 0.04 秒)

    Pharmaceutically active compounds
    6.
    发明授权
    Pharmaceutically active compounds 失效
    药物活性化合物

    公开(公告)号：US06440982B1

    公开(公告)日：2002-08-27

    申请号：US09650848

    申请日：2000-08-29

    申请人： Graham Nigel Maw ,  David James Rawson

    发明人： Graham Nigel Maw ,  David James Rawson

    IPC分类号： A61K3152

    CPC分类号： C07D473/30

    摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.

    摘要翻译： 提供式IA和式IB的化合物，其中R1，R2，R3，Het1和X具有描述中给出的含义，其可用于治疗和预防性治疗环状鸟苷3' ，需要5'-单磷酸磷酸二酯酶（例如cGMP PDE5）。

    Indole derivatives useful as endothelin receptor antagonists
    7.
    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）