Invention Application
- Patent Title: Cyclopropane compounds and pharmaceutical use thereof
- Patent Title (中): 环丙烷化合物及其药物用途
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Application No.: US12457391Application Date: 2009-06-09
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Publication No.: US20100105894A1Publication Date: 2010-04-29
- Inventor: Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafuml Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
- Applicant: Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafuml Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
- Assignee: Japan Tobacco Inc.
- Current Assignee: Japan Tobacco Inc.
- Main IPC: C07D243/08
- IPC: C07D243/08 ; C07C229/02 ; C07C307/00 ; C07D409/02 ; C07D231/10 ; C07D401/02 ; C07D261/06 ; C07D333/34 ; C07D241/04 ; C07D271/06 ; C07D257/04 ; C07D295/00 ; C07D215/14 ; C07D205/04 ; C07D413/02 ; C07D241/36 ; C07D413/14 ; C07D223/14

Abstract:
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.
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