Azacycloalkyl substituted acetic acid derivatives for use as MMP inhibitors
    1.
    发明申请
    Azacycloalkyl substituted acetic acid derivatives for use as MMP inhibitors 审中-公开
    用作MMP抑制剂的氮杂环烷基取代的乙酸衍生物

    公开(公告)号:US20070060569A1

    公开(公告)日:2007-03-15

    申请号:US11591861

    申请日:2006-11-02

    摘要: Compound of the formula wherein R represents OH or NHOH; R1 represents hydrogen, optically substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or acyl derived from a carboxylic acid, from a carbonic acid, from a carbamic acid or from a sulfonic acid; R2 represents biarylsulfonyl or aryloxyrylsulfonyl; R3 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl or acyl derived from a carboxylic acid, from a carbonic acid or from a carbamic acid; R4 and R5 represent independently hydrogen, lower alkyl, lower alkoxycarbonyl, aryl-lower alkyl or cycloalkyl-lower alkyl; m is zero, 1, 2 or 3; pharmaceutically acceptable prodrug derivatives thereof; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; and their use for inhibiting matrix degrading metalloproteinases and preventing or treating matrix metalloproteinase dependent conditions in mammals.

    摘要翻译: 下式的化合物其中R表示OH或NHOH; R 1表示氢,光取代的低级烷基,芳基 - 低级烷基,环烷基 - 低级烷基或衍生自羧酸的酰基,来自碳酸,氨基甲酸或磺酸; R 2表示联芳基磺酰基或芳氧基酰基磺酰基; R 3表示氢,任选取代的低级烷基,芳基 - 低级烷基,环烷基 - 低级烷基或衍生自羧酸的酰基,来自碳酸或氨基甲酸; R 4和R 5独立地表示氢,低级烷基,低级烷氧基羰基,芳基 - 低级烷基或环烷基 - 低级烷基; m为零,1,2或3; 其药学上可接受的前药衍生物; 其药学上可接受的盐; 包含所述化合物的药物组合物; 以及它们用于抑制基质降解金属蛋白酶和预防或治疗哺乳动物中基质金属蛋白酶依赖性条件的用途。

    Methods and compositions for treatment of cancer pain
    3.
    发明申请
    Methods and compositions for treatment of cancer pain 审中-公开
    治疗癌症疼痛的方法和组合物

    公开(公告)号:US20060004104A1

    公开(公告)日:2006-01-05

    申请号:US10512015

    申请日:2003-04-22

    IPC分类号: A61K31/195

    CPC分类号: A61K31/196

    摘要: The invention provides a method of treating cancer pain, e.g. bone cancer pain, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor; advantageously a compound of formula (I); wherein R, R1, R2, R3, R4, and R5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug ester thereof.

    摘要翻译: 本发明提供了治疗癌症疼痛的方法,例如, 在需要这种治疗的受试者中包括对受试者施用有效量的COX-2抑制剂的骨癌疼痛; 有利地是式(I)的化合物; 其中R 1,R 1,R 2,R 3,R 4和R 5, / SUB>如定义; 其药学上可接受的盐; 或其药学上可接受的前药酯。