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    • 5. 发明申请
    • CATHEPSIN PROTEASES INHIBITORS
    • CATHEPSIN蛋白抑制剂
    • WO2008051763A1
    • 2008-05-02
    • PCT/US2007/081635
    • 2007-10-17
    • IRM LLCRUSSO, RossEPPLE, Robert
    • EPPLE, Robert
    • C07D498/08A61K31/395A61P11/06A61P19/02A61P19/10A61P35/00A61P37/00
    • C07D498/08
    • The invention provides compounds (I) and pharmaceutical compositions thereof, and more particularly, bicyclic carbamates, which are useful as cathepsin inhibitors, and methods for using such compounds or pharmaceutically acceptable salts thereof, wherein X is 0 or S; R 1 is OR 2 , halo, (CR 2 ) n R 3 , nitro, cyano, amino, aniido, sulfonamide, or an optionally substituted C 1-6 alkyl, C 2-6 alkenyl, or C 3-6 alkynyl;R 2 is H, (CR 2 )nR 3 , or an optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 3-6 alkynyl; R 3 is an optionally substituted aryl, heteroaryl, carbocyciic ring or heterocyclic ring; m is 1-3; and n is 0-4.
    • 本发明提供了可用作组织蛋白酶抑制剂的化合物(I)及其药物组合物,更具体地是双环氨基甲酸酯,以及使用这些化合物或其药学上可接受的盐的方法,其中X为0或S; R 1是OR 2,卤素,(CR 2)n R 3,R 3, ,硝基,氰基,氨基,脒基,磺酰胺或任选取代的C 1-6烷基,C 2-6链烯基或C 3-6烯基, R 2是H,(CR 2)n R 3或任选取代的C 1-6烷基, C 1-6烷基,C 2-6烯基或C 3-6亚炔基; R 3是任选取代的芳基,杂芳基,碳环或杂环; m为1-3; n为0-4。