发明申请
- 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: US20060199826A1公开(公告)日: 2006-09-07
- 发明人: Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole Littmann , Katsutaka Yasue , Steven Andrews , Atushi Sakai , Andrew Fryer , Takafumi Matsuo , Ellen Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
- 申请人: Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole Littmann , Katsutaka Yasue , Steven Andrews , Atushi Sakai , Andrew Fryer , Takafumi Matsuo , Ellen Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
- 主分类号: A61K31/496
- IPC分类号: A61K31/496 ; A61K31/4436 ; A61K31/416 ; C07D49/02
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, X1 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
- US07351825B2 Cyclopropane compounds and pharmaceutical use thereof 公开/授权日:2008-04-01
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