公开(公告)号：EP1431285B1

公开(公告)日：2009-01-07

申请号：EP02767899.4

申请日：2002-09-05

申请人： KAKEN PHARMACEUTICAL CO., LTD.

发明人： SHIMANO, Masanao. C.R.L. KAKEN PHARMACEUTICAL CO., LTD ,  KAMEI, Noriyuki. C.R.L. KAKEN PHARMACEUTICAL CO., LTD ,  TANAKA, Tomohiro. C.R.L. KAKEN PHARMACEUTICAL CO., LTD ,  HARADA, Tatsuhiro. C.R.L. KAKEN PHARMACEUTICAL CO., LTD ,  HAINO, Makoto. C.R.L. KAKEN PHARMACEUTICAL CO., LTD ,  OKUYAMA, Akihiro. C.R.L. KAKEN PHARMACEUTICAL CO., LTD ,  ARAKAWA, Yoshio. C.R.L. KAKEN PHARMACEUTICAL CO., LTD ,  MURAKAMI, Yoshiko. C.R.L. KAKEN PHARMACEUTICAL CO., LTD

IPC分类号： C07C317/40 ,  C07D213/30 ,  C07D215/14 ,  C07D317/72 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D491/113 ,  C07C317/28 ,  C07C317/32 ,  C07D211/70 ,  C07D213/42 ,  C07D277/14 ,  C07D319/06 ,  A61K31/165 ,  A61K31/357 ,  A61K31/435 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/55 ,  A61P35/00

CPC分类号： C07D409/12 ,  C07C317/28 ,  C07C2601/14 ,  C07D207/20 ,  C07D211/70 ,  C07D213/30 ,  C07D213/42 ,  C07D215/14 ,  C07D277/14 ,  C07D317/72 ,  C07D319/06 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

摘要： Reverse hydroxamic acid derivatives having specific structures represented by the general formula (Ia): (Ia) (wherein A represents hydrogen, etc.; Ar1 represents arylene, etc.; Ar2 represents optionally substituted aryl, heteroaryl, etc.; R1 represents hydrogen, alkyl, etc.; and R2a represents substituted cycloalkyl, heterocycloalkyl, etc.) and the general formula (I): (I) (wherein A, Ar1, ar2, and R1 are the same as defined above and R2 represents hydrogen, R2a, etc.) and salts of the derivatives. They have TNF-α converting enzyme (TACE) inhibitory activity.