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36 条记录 (耗时 0.05 秒)

    Phosphono/biaryl substituted amino acid derivatives
    23.
    发明授权
    Phosphono/biaryl substituted amino acid derivatives 失效
    膦酰/联芳基取代的氨基酸衍生物

    公开(公告)号：US5250522A

    公开(公告)日：1993-10-05

    申请号：US959000

    申请日：1992-10-09

    申请人： Stephane De Lombaert

    发明人： Stephane De Lombaert

    IPC分类号： C07F9/38 ,  C07F9/40 ,  A61K31/66

    CPC分类号： C07F9/3808 ,  C07F9/4006

    摘要： The present invention relates to the N-phosphonomethyl-biaryl substituted amino acid derivatives of formula I ##STR1## wherein X represents a direct bond, C.sub.1-4 -alkylene or C.sub.2 -C.sub.4 -alkenylene; R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, .alpha.-(trichloromethyl, carboxyl, esterified carboxyl or amidated carboxyl)substituted-(lower alkyl or aryl-lower alkyl), acyloxymethyl optionally monosubstituted on methyl carbon by C.sub.1-20 -alkyl, by C.sub.5 -C.sub.7 -cycloalkyl, by aryl or by aryl-lower alkyl; R.sub.1 represents monocyclic carbocyclic or monocyclic heterocyclic aryl; COR.sub.3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; R.sub.2 and R.sub.4 represent hydrogen, lower alkyl, trifluoromethyl, lower alkoxy or halogen; 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 - 联芳基取代的氨基酸衍生物，其中X表示直接键，C 1-4 - 亚烷基或C 2 -C 4亚烯基; R和R'独立地表示氢，碳环芳基，6-四氢萘基，5-二氢化茚基，α-（三氯甲基，羧基，酯化羧基或酰胺基羧基）取代的 - （低级烷基或芳基 - 低级烷基），在甲基碳上任选单取代的酰氧基甲基 C 1-20烷基，C 5 -C 7 - 环烷基，芳基或芳基 - 低级烷基; R1表示单环碳环或单环杂环芳基; COR3表示以药学上可接受的酯的形式衍生的羧基或羧基; R2和R4代表氢，低级烷基，三氟甲基，低级烷氧基或卤素; 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。

    Aryl substituted purine analogues
    25.
    发明申请
    Aryl substituted purine analogues 审中-公开
    芳基取代的嘌呤类似物

    公开(公告)号：US20070197559A1

    公开(公告)日：2007-08-23

    申请号：US10591553

    申请日：2005-03-02

    申请人： Rajagopal Bakthavatchalam ,  Stephane De Lombaert

    发明人： Rajagopal Bakthavatchalam ,  Stephane De Lombaert

    IPC分类号： A61K31/519 ,  A61K31/52 ,  C07D473/12 ,  C07D487/02

    CPC分类号： C07D473/34 ,  C07D473/12 ,  C07D487/04

    摘要： Aryl-substituted purine analogues are provided, of the formula: (I) 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： 提供芳基取代的嘌呤类似物，其具有下式：（I），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。

    Phosphono/biaryl substituted dipeptide derivatives
    29.
    发明授权
    Phosphono/biaryl substituted dipeptide derivatives 失效
    PHOSPHONO / BIARYL取代的二肽衍生物

    公开(公告)号：US5155100A

    公开(公告)日：1992-10-13

    申请号：US694533

    申请日：1991-05-01

    申请人： Mark D. Erion ,  Stephane De Lombaert

    发明人： Mark D. Erion ,  Stephane De Lombaert

    IPC分类号： A61K31/66 ,  A61K38/00 ,  A61P43/00 ,  C07F9/38 ,  C07F9/40 ,  C07F9/655 ,  C07F9/6553 ,  C07K1/113 ,  C07K5/06 ,  C07K14/81 ,  C12N9/99

    CPC分类号： C07F9/655345 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/65515 ,  C07K5/06191 ,  A61K38/00

    摘要： The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.7 -cycloalkyl-lower alkyl, amino-lower alkyl, hydroxyl-lower alkyl, lower alkylthio-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkylthio-lower alkyl or aryl-lower alkoxy-lower alkyl; biaryl represents phenyl substituted by carbocyclic or heterocyclic aryl; and pharmaceutically acceptable mono-, di- or tri-ester derivatives thereof in which one, two or three of the acidic hydroxy groups of the carboxyl and phosphono functional groups are esterified in form of a mono-, di- or tri- pharmaceutically acceptable ester; and pharmaceutically acceptable amide derivatives thereof wherein the carboxyl group is derivatized in form of a pharmaceutically acceptable amide; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for the 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.

    Indolizine inhibitors of leukotriene production
    30.
    发明授权
    Indolizine inhibitors of leukotriene production 有权
    吲哚嗪抑制剂白三烯生产

    公开(公告)号：US08618300B2

    公开(公告)日：2013-12-31

    申请号：US13061996

    申请日：2009-08-25

    申请人： Todd Bosanac ,  Stephane De Lombaert ,  Ho Yin Lo ,  Peter Allen Nemoto ,  Alan Olague

    发明人： Todd Bosanac ,  Stephane De Lombaert ,  Ho Yin Lo ,  Peter Allen Nemoto ,  Alan Olague

    IPC分类号： C07D221/02

    CPC分类号： C07D471/04

    摘要： The present invention relates to compounds of formula (I): and pharmaceutically acceptable salt thereof, wherein X1 to X4, R1 to R4, A, B, D and m are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

    摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中X 1至X 4，R 1至R 4，A，B，D和m如本文所定义。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。