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    • 5. 发明申请
    • PROTEASE INHIBITORS
    • PROTEASE抑制剂
    • WO2010034789A1
    • 2010-04-01
    • PCT/EP2009/062407
    • 2009-09-24
    • Medivir ABIVANOV, VladimirSAMUELSSON, BertilJOHANSSON, Per-OlaKAHNBERG, PiaWÄHLING, Horst
    • IVANOV, VladimirSAMUELSSON, BertilJOHANSSON, Per-OlaKAHNBERG, PiaWÄHLING, Horst
    • C07D491/048A61K31/496A61P19/00
    • C07D491/048
    • Compounds of the formula II, wherein R 3 is C 1 -C 3 alkyl or C 3 -C 6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R 3 is C 3 -C 6 cycloalkyl it may alternatively be gem substituted with fluoro; R 4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A 1 is CH or N, A 2 is CR 6 R 7 or NR 6 , provided at least one of A 1 and A 2 comprises N; n is 0 or 1 such that the ring containing A 1 and A 2 is a saturated, nitrogen-containing ring of 5 or 6 ring atoms; R 6 is H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 3 alkyl-O-C 1 -C 3 alkyl, or when A 2 is C, R 6 can also be C 1 -C 4 alkoxy or F; R 7 is H, C 1 -C 4 alkyl or F; or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
    • 其中R 3为C 1 -C 3烷基或C 3 -C 6环烷基,其中R 3为C 3 -C 6环烷基时,任选被一个或两个甲基和/或氟,三氟甲基或甲氧基取代, 被氟取代; R4是甲基或氟; m为0,1或2; E是任选被甲基或氟取代的键或噻唑基; A1是CH或N,A2是CR6R7或NR6,条件是A1和A2中的至少一个包括N; n为0或1,使得含有A 1和A 2的环是5或6个环原子的饱和的含氮环; R6是H,C1-C4烷基,C1-C4卤代烷基,C1-C3烷基-O-C1-C3烷基,或当A2是C时,R6也可以是C1-C4烷氧基或F; R 7为H,C 1 -C 4烷基或F; 或其药学上可接受的盐,N-氧化物或其水合物,可用于治疗组织蛋白酶K不适当表达或活化的疾病,例如骨质疏松症,骨关节炎,类风湿性关节炎或骨转移。