基本信息:
- 专利标题: PROTEASE INHIBITORS
- 专利标题(中):PROTEASE抑制剂
- 申请号:PCT/EP2009/062408 申请日:2009-09-24
- 公开(公告)号:WO2010034790A1 公开(公告)日:2010-04-01
- 发明人: ODÉN, Lourdes, Salvadore , JOHANSSON, Per-Olof , KAHNBERG, Pia , NILSSON, Magnus , SAMUELSSON, Bertil , GRABOWSKA, Urszula
- 申请人: MEDIVIR AB , ODÉN, Lourdes, Salvadore , JOHANSSON, Per-Olof , KAHNBERG, Pia , NILSSON, Magnus , SAMUELSSON, Bertil , GRABOWSKA, Urszula
- 申请人地址: P.O. Box 1086 S-141 22 Huddinge SE
- 专利权人: MEDIVIR AB,ODÉN, Lourdes, Salvadore,JOHANSSON, Per-Olof,KAHNBERG, Pia,NILSSON, Magnus,SAMUELSSON, Bertil,GRABOWSKA, Urszula
- 当前专利权人: MEDIVIR AB,ODÉN, Lourdes, Salvadore,JOHANSSON, Per-Olof,KAHNBERG, Pia,NILSSON, Magnus,SAMUELSSON, Bertil,GRABOWSKA, Urszula
- 当前专利权人地址: P.O. Box 1086 S-141 22 Huddinge SE
- 代理机构: GOODALL, Scott et al.
- 优先权: GB0817424.5 20080924
- 主分类号: C07D491/048
- IPC分类号: C07D491/048 ; A61K31/496 ; A61P19/00
摘要:
Compounds of the formula II: wherein R 1 forms an ethynyl bond and R 2 is H or C 3 -C 6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF 3 , OMe or halo; 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 subsituted with fluoro; R 4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, 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.
摘要(中):
式II化合物:其中R1形成乙炔基,R2是H或任选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的C 3 -C 6环烷基; 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是键,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; 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。
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D491/00 | 杂环化合物,在稠环系中含有1个或多个有氧原子作为仅有的杂环原子的环,且含有1个或多个有氮原子作为仅有的杂环原子的环,不包含在C07D451/00至C07D459/00、C07D463/00、C07D477/00或C07D489/00组中 |
--------C07D491/02 | .在稠环系中含有两个杂环 |
----------C07D491/04 | ..邻位稠合系 |
------------C07D491/044 | ...在含氧环上仅有1个氧原子作为杂环原子 |
--------------C07D491/048 | ....含氧环是五元环 |