| 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<SUP>1 </SUP>is -(CH<SUB>2</SUB>)<SUB>m</SUB>-X-(CH<SUB>2</SUB>)<SUB>n</SUB>-A<SUP>1 </SUP>etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A<SUP>1 </SUP>is a substituted C<SUB>3-14 </SUB>hydrocarbon ring group, etc.; R<SUP>2 </SUP>and R<SUP>3 </SUP>are the same or different and each is a hydrogen atom, -(CH<SUB>2</SUB>)<SUB>p</SUB>-X<SUB>1</SUB>-(CH<SUB>2</SUB>)<SUB>q</SUB>-A<SUP>2</SUP>, etc., wherein p and q are the same or different and each is 0 to 6, X<SUB>1 </SUB>is a single bond, etc. and A<SUP>2 </SUP>is an optionally substituted C<SUB>3-14 </SUB>hydrocarbon ring group, etc.; R<SUP>4 </SUP>is -CO<SUB>2</SUB>R<SUP>9</SUP>, etc., wherein R<SUP>9 </SUP>is a hydrogen atom, etc.; and R<SUP>20 </SUP>and R<SUP>21 </SUP>are the same or different and each is a hydrogen atom, -(CH<SUB>2</SUB>)<SUB>m12</SUB>-X<SUB>12</SUB>-(CH<SUB>2</SUB>)<SUB>m12</SUB>-R<SUP>30</SUP>, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X<SUB>12 </SUB>is a single bond, etc. and R<SUP>30 </SUP>is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof. |
| 申请人 |
JAPAN TOBACCO INC. |
发明人 |
INABA, TAKASHI;HAAS, JULIA;SHIOZAKI, MAKOTO;LITTMANN, NICOLE M.;YASUE, KATSUTAKA;ANDREWS, STEVEN W.;SAKAI, ATSUSHI;FRYER, ANDREW M.;MATSUO, TAKAFUMI;LAIRD, ELLEN R.;SUMA, AKIRA;SHINOZAKI, YUICHI;HORI, YOSHIKAZU;IMAI, HIROTO;NEGORO, TAMOTSU |
