公开(公告)号：US20050020680A1

公开(公告)日：2005-01-27

申请号：US10489204

申请日：2002-09-09

申请人： John Falck ,  Noriyuki Miyata ,  Naoya Ono ,  Tomomichi Chonan ,  Hitomi Hirano ,  Yoshihisa Toda ,  Tohru Tanami ,  Shigeru Okuyama

发明人： John Falck ,  Noriyuki Miyata ,  Naoya Ono ,  Tomomichi Chonan ,  Hitomi Hirano ,  Yoshihisa Toda ,  Tohru Tanami ,  Shigeru Okuyama

IPC分类号： C07C33/044 ,  C07C33/42 ,  C07C59/42 ,  C07C59/46 ,  C07C59/60 ,  C07C69/708 ,  C07C235/28 ,  C07C255/15 ,  C07C259/06 ,  C07C309/10 ,  C07C309/20 ,  C07C309/23 ,  C07C309/24 ,  C07C309/68 ,  C07C311/17 ,  C07C311/51 ,  C07C317/44 ,  C07C323/52 ,  C07C323/66 ,  C07D257/04 ,  C07D277/34 ,  A61K31/185 ,  C07

CPC分类号： C07D257/04 ,  C07C33/044 ,  C07C33/423 ,  C07C33/426 ,  C07C59/42 ,  C07C59/46 ,  C07C59/60 ,  C07C69/708 ,  C07C235/28 ,  C07C255/15 ,  C07C259/06 ,  C07C309/10 ,  C07C309/20 ,  C07C309/23 ,  C07C309/24 ,  C07C309/68 ,  C07C311/17 ,  C07C311/51 ,  C07C317/44 ,  C07C323/52 ,  C07C323/66 ,  C07C2601/08 ,  C07C2601/14 ,  C07D277/34

摘要： A hydroxyfattysulfonic acid analog represented by Formula (I): wherein X is an ethylene group, a vinylene group or an ethynylene group; Y is an ethylene group, a vinylene group, an ethynylene group, OCH2 or S(O)pCH2 wherein p is 0, 1 or 2; m is an integer of 1 to 5 inclusive; n is an integer of 0 to 4 inclusive; R1 is a C1-8 alkyl group, a C3-8 cycloalkyl group, a C1-4 alkyl group substituted with a C3-8 cycloalkyl group, a C1-4 alkyl group substituted with an aryl group or a C1-4 alkyl group substituted with an aryloxy group; R2 is a hydrogen atom or a methyl group; R1 and R2 together with the carbon atom to which they are attached may form a C3-8 cycloalkyl group; R3 is a hydrogen atom or a C2-8 acyl group; R4 is OR5 or NHR6, wherein R5 is a hydrogen atom, a C1-4 alkyl group, an alkali metal, an alkaline earth metal or an ammonium group and R6 is a hydrogen atom or a C1-4 alkyl group; or a pharmaceutically acceptable salt or a hydrate thereof. The compounds of the present invention are useful as an elastase release inhibitor.

摘要翻译： 由式（I）表示的羟基脂肪磺酸类似物：其中X是亚乙基，亚乙烯基或亚乙炔基; Y是亚乙基，亚乙烯基，亚乙炔基，OCH 2或S（O）pCH 2，其中p是0,1或2; m为1〜5的整数， n为0〜4的整数， R 1是C 1-8烷基，C 3-8环烷基，被C 3-8环烷基取代的C 1-4烷基，被芳基取代的C 1-4烷基或C 1-4 被芳氧基取代的烷基; R 2是氢原子或甲基; R 1和R 2与它们所连接的碳原子一起可以形成C 3-8环烷基; R 3是氢原子或C 2-8酰基; R 4是OR 5或NHR 6，其中R 5是氢原子，C 1-4烷基，碱金属，碱土金属或铵基，R 6是 氢原子或C 1-4烷基; 或其药学上可接受的盐或其水合物。 本发明的化合物可用作弹性蛋白酶释放抑制剂。