发明授权
- 专利标题: Cyclopropane compounds and pharmaceutical use thereof
- 专利标题(中): 环丙烷化合物及其药物用途
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申请号: US11011773申请日: 2004-12-15
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公开(公告)号: US07351825B2公开(公告)日: 2008-04-01
- 发明人: Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
- 申请人: Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
- 申请人地址: JP Tokyo
- 专利权人: Japan Tobacco Inc.
- 当前专利权人: Japan Tobacco Inc.
- 当前专利权人地址: JP Tokyo
- 代理机构: Finnegan, Henderson, Farabow, Garrett & Dunner, LLP
- 主分类号: C07D265/00
- IPC分类号: C07D265/00 ; C07D295/00 ; C07D237/00 ; C07D409/00 ; C07D411/00 ; C07D217/00 ; C07D211/00 ; C07D213/00 ; C07D271/00 ; C07D413/00 ; C07D498/00 ; C07D277/00 ; C07D257/00 ; C07D233/00 ; C07D231/00 ; C07D207/00 ; C07D333/00 ; C07D307/00 ; C07D303/00 ; C07D309/00 ; C07D311/00
摘要:
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
公开/授权文献
- US20060199826A1 Cyclopropane compounds and pharmaceutical use thereof 公开/授权日:2006-09-07
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