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    • 6. 发明申请
    • Protease Inhibitors
    • 蛋白酶抑制剂
    • US20110039862A1
    • 2011-02-17
    • US12739489
    • 2009-09-24
    • Lourdes Salvadore OdénMagnus NilssonPia KahnbergBertil SamuelssonUrszula Grabowska
    • Lourdes Salvadore OdénMagnus NilssonPia KahnbergBertil SamuelssonUrszula Grabowska
    • A61K31/496C07D491/048A61P19/10A61P1/02A61P35/00A61P29/00A61P19/02A61P19/08A61P7/00
    • C07D277/40C07D491/048C07D495/04
    • Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 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.
    • 式II化合物:其中R 1和R 2独立地是H,F或CH 3; 或R1形成乙炔基,R2是H或C3-C6环烷基,其任选地被一个或两个独立地选自甲基,CF 3,OMe或卤素的取代基取代; R 3是C 1 -C 3烷基或C 3 -C 6环烷基,当R 3是C 3 -C 6环烷基时,它们任选被一个或两个甲基和/或氟,三氟甲基或甲氧基取代,也可以被氟取代; 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; 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; R7是H,C1-C4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骼 转移。
    • 10. 发明授权
    • Protease inhibitors
    • 蛋白酶抑制剂
    • US08242119B2
    • 2012-08-14
    • US12739489
    • 2009-09-24
    • Lourdes Salvador OdénMagnus NilssonPia KahnbergBertil SamuelssonUrszula Grabowska
    • Lourdes Salvador OdénMagnus NilssonPia KahnbergBertil SamuelssonUrszula Grabowska
    • A61K31/496C07D491/04
    • C07D277/40C07D491/048C07D495/04
    • Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 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.
    • 式II化合物:其中R 1和R 2独立地为H,F或CH 3; 或R1形成乙炔基,R2是H或C3-C6环烷基,其任选地被一个或两个独立地选自甲基,CF 3,OMe或卤素的取代基取代; R 3是C 1 -C 3烷基或C 3 -C 6环烷基,当R 3是C 3 -C 6环烷基时,它们任选被一个或两个甲基和/或氟,三氟甲基或甲氧基取代,也可以被氟取代; 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; 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; R7是H,C1-C4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骼 转移。