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36 条记录 (耗时 0.036 秒)

    Heteroalkyl-substituted biphenyl-4-carboxylic acid arylamide analogues
    32.
    发明申请
    Heteroalkyl-substituted biphenyl-4-carboxylic acid arylamide analogues 审中-公开
    异丁烷基取代的联苯-4-羧酸芳酰胺类似物

    公开(公告)号：US20070191363A1

    公开(公告)日：2007-08-16

    申请号：US10591383

    申请日：2005-03-02

    申请人： Kevin Hodgetts ,  Stephane De Lombaert

    发明人： Kevin Hodgetts ,  Stephane De Lombaert

    IPC分类号： A61K31/5377 ,  A61K31/4545 ,  A61K31/44 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D213/56 ,  C07D401/12 ,  C07D413/12

    摘要： Heteroalkyl-substituted biphenyl-4-carboxylic acid arylamide analogues are provided, of the formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

    摘要翻译： 提供了下式的杂烷基取代的联苯-4-羧酸芳酰胺类似物：其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

    Aminoalkyl substituted pyrrolo[3,2-e] pyridine and pyrrolo[2,3-b]pyrimidine derivatives: modulators of CRF1 receptors
    34.
    发明授权
    Aminoalkyl substituted pyrrolo[3,2-e] pyridine and pyrrolo[2,3-b]pyrimidine derivatives: modulators of CRF1 receptors 失效
    氨基烷基取代的吡咯并[3,2-e]吡啶和吡咯并[2,3-b]嘧啶衍生物：CRF1受体的调节剂

    公开(公告)号：US06436932B1

    公开(公告)日：2002-08-20

    申请号：US09947045

    申请日：2001-09-04

    申请人： Ping Ge ,  Raymond F. Horvath ,  Stephane De Lombaert

    发明人： Ping Ge ,  Raymond F. Horvath ,  Stephane De Lombaert

    IPC分类号： A61K31519

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Disclosed are compounds of the formula: wherein Ar, Q1, Q2, R1, W and X are substituents as defined herein, which compounds are water-soluble CRF1 receptor antagonists, and are therefore useful for the treatment of psychiatric disorders and neurological diseases, including major depression, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders, as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.

    摘要翻译： 公开了下式的化合物：其中Ar，Q1，Q2，R1，W和X是本文定义的取代基，该化合物是水溶性CRF1受体拮抗剂，因此可用于治疗精神疾病和神经疾病，包括 重症抑郁症，焦虑相关疾病，创伤后应激障碍，核上性麻痹和进食障碍，以及治疗与精神病理学障碍和应激相关的免疫学，心血管或心脏相关疾病和结肠超敏反应。

    Antihypertensive tricyclic azepine derivatives useful as inhibitors of enkephalinase and ACE
    35.
    发明授权
    Antihypertensive tricyclic azepine derivatives useful as inhibitors of enkephalinase and ACE 失效
    抗高血压三环吖庚因衍生物可用作脑啡肽酶和ACE的抑制剂

    公开(公告)号：US5644055A

    公开(公告)日：1997-07-01

    申请号：US569117

    申请日：1995-12-20

    申请人： Stephane De Lombaert

    发明人： Stephane De Lombaert

    IPC分类号： A61K31/55 ,  A61K38/00 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/24 ,  A61P25/26 ,  C07D471/04 ,  C07D471/06 ,  C07D487/06 ,  C07K5/078 ,  A61K31/47 ,  C07D487/04

    CPC分类号： C07D471/06 ,  C07D487/06 ,  C07K5/06139 ,  A61K38/00

    摘要： Disclosed are the compounds of formula I ##STR1## wherein X represents oxo, one hydroxy or lower alkoxy and one hydrogen, or two hydrogens;R.sub.a and R.sub.b independently represent hydrogen, hydroxy, lower alkoxy, nitro, amino or halogen; or R.sub.a and R.sub.b on adjacent carbons taken together represent lower alkylenedioxy;R.sub.c represents hydrogen, lower alkyl or aryl-lower alkyl;R represents hydrogen or acyl;R.sub.1 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl, biaryl-lower alkyl or trifluoromethyl;R.sub.2 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 together with the carbon to which they are attached represent cycloalkylene or benzo-fused cycloalkylene;m represents one or two;n represents zero or one;COOR.sub.3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; disulfide derivatives formed from said compounds wherein R is hydrogen;and pharmaceutically acceptable salts thereof;pharmaceutical compositions comprising said compounds; methods for preparation of said compounds; intermediates; and methods of treating disorders in mammals which are responsive to ACE and NEP inhibition by administration of said compounds to mammals in need of such treatment.

    摘要翻译： PCT No.PCT / EP94 / 01978 Sec。 371 1995年12月20日第 102（e）1995年12月20日，PCT PCT 1994年6月17日PCT公布。 公开号WO95 / 01353 日期1995年1月12日公开是式I的化合物或低级烷氧基和一个氢或两个氢; R a和R b独立地表示氢，羟基，低级烷氧基，硝基，氨基或卤素; 或相邻碳原子上的Ra和Rb代表低级亚烷基二氧基; Rc表示氢，低级烷基或芳基 - 低级烷基; R代表氢或酰基; R 1表示氢，低级烷基，芳基，芳基 - 低级烷基，环烷基，环烷基 - 低级烷基，联芳基，联芳基 - 低级烷基或三氟甲基; R2代表氢或低级烷基; 或R 1和R 2与它们所连接的碳一起代表亚环烷基或苯并稠合的亚环烷基; m表示一个或两个; n表示0或1; COOR3表示以药学上可接受的酯的形式衍生的羧基或羧基; 由所述化合物形成的二硫化物衍生物，其中R是氢; 及其药学上可接受的盐; 包含所述化合物的药物组合物; 所述化合物的制备方法; 中间体 以及通过向需要这种治疗的哺乳动物施用所述化合物来治疗对ACE和NEP抑制有反应的哺乳动物疾病的方法。

    Phosphono substituted tetrazole derivatives
    36.
    发明授权
    Phosphono substituted tetrazole derivatives 失效
    膦酰取代的四唑衍生物

    公开(公告)号：US5273990A

    公开(公告)日：1993-12-28

    申请号：US940118

    申请日：1992-09-03

    申请人： Stephane De Lombaert

    发明人： Stephane De Lombaert

    IPC分类号： C07F9/6524 ,  C07D257/04 ,  A01N57/24

    CPC分类号： C07F9/6524

    摘要： The present invention relates to the N-phosphonomethyl substituted tetrazole derivatives of formula I ##STR1## and tautomers thereof wherein R.sub.1 is aryl or biaryl; n is zero, 1 or 2 pharmaceutically acceptable mono- or di-ester derivatives thereof in which one or both of the acidic hydroxy groups of the phosphono functional group are esterified in form of a pharmaceutically acceptable mono- or di-ester; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of neutral endopeptidases by administration of said compounds to mammals in need of such treatment.

    摘要翻译： 本发明涉及式I的N-膦酰基甲基取代的四唑衍生物（Ⅰ）及其互变异构体，其中R 1是芳基或联芳基; n是0,1或2个药学上可接受的单酯或二酯衍生物，其中膦酰基官能团的酸性羟基中的一个或两个以药学上可接受的单酯或二酯的形式酯化; 及其药学上可接受的盐; 包含所述化合物的药物组合物; 制备所述化合物和制备中间体的方法; 以及通过向需要这种治疗的哺乳动物施用所述化合物来治疗哺乳动物疾病的方法，所述疾病对中性内肽酶的抑制有反应。