Japan Tobacco Inc.

Atushi Sakai

Steven Wade Andrews

Julia Haas

Takashi Inaba

Ellen Ruth Laird

Yoshikazu Hori

Makoto Shiozaki

Akira Suma

Andrew M Fryer

Takafumi Matsuo

Yuichi Shinozaki

Hiroto Imai

Nicole M Littmann

Tamotsu Negoro

Katsutaka Yasue

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 Ris &#x2014;(CH)&#x2014;X&#x2014;(CH)-Aetc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and Ais a substituted Chydrocarbon ring group, etc.; Rand Rare the same or different and each is a hydrogen atom, &#x2014;(CH)&#x2014;X&#x2014;(CH)-A, etc., wherein p and q are the same or different and each is 0 to 6, Xis a single bond, etc. and Ais an optionally substituted Chydrocarbon ring group, etc.; Ris &#x2014;COR, etc., wherein Ris a hydrogen atom, etc.; and Rand Rare the same or different and each is a hydrogen atom, &#x2014;(CH)&#x2014;X&#x2014;(CH)&#x2014;R, etc., wherein m12 and m12 are the same or different and each is 0 to 6, Xis a single bond, etc. and Ris a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.

Cyclopropane compounds and pharmaceutical use thereof

Growing community of inventors

Osaka, Japan

Atushi Sakai