CYCLOPROPANE COMPOUNDS AND PHARMACEUTICAL USE THEREOF

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 R<1> is - (CH2) m-X- (CH2)n-A<1> etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A<1> is a substituted C3-14 hydrocarbon ring group, etc.; R<2> and R<3> are the same or different and each is a hydrogen atom, -(CH2)p-X1-(CH2)q-A<2>, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A<2> is an optionally substituted C3-14 hydrocarbon ring group, etc.; R<4> is -C02R<9>, etc., wherein R<9> is a hydrogen atom, etc.; and R<20 >and R<21 >are the same or different and each is a hydrogen atom, - (CH2)m12-X12- (CH2)m12-R<30>, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R<30 >is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.