公开(公告)号：EP1436252A1

公开(公告)日：2004-07-14

申请号：EP02761382.7

申请日：2002-09-09

申请人： TAISHO PHARMACEUTICAL CO., LTD ,  BOARD OF REGENTS THE UNIVERSITY OF TEXAS SYSTEM

发明人： FALCK, John, R.,c/o THE UNIVERSITY OF TEXAS ,  MIYATA, Noriyuki,c/o TAISHO PHARMA. CO., LTD. ,  ONO, Naoya,c/o TAISHO PHARMACEUTICAL CO., LTD. ,  CHONAN, Tomomichi,c/o TAISHO PHARMA. CO., LTD. ,  HIRANO, Hitomi,c/o TAISHO PHARMACEUTICAL CO. LTD. ,  TODA, Yoshihisa,c/o TAISHO PHARMACEUTICAL CO. LTD ,  TANAMI, Tohru,c/o TAISHO PHARMACEUTICAL CO., LTD. ,  OKUYAMA, Shigeru,c/o TAISHO PHARMA. CO. LTD.

IPC分类号： C07C309/01 ,  C07C309/02 ,  C07C309/03 ,  C07C309/04 ,  C07C309/07 ,  C07C309/63 ,  C07C309/64 ,  C07C309/65 ,  C07C309/67 ,  C07C309/68 ,  C07C303/36

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 C¿1-8? 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; R?2¿ is a hydrogen atom or a methyl group; R?1 and R2¿ together with the carbon atom to which they are attached may form a C¿3-8? cycloalkyl group; R?3¿ is a hydrogen atom or a C¿2-8? acyl group; R?4 is OR5 or NHR6¿, wherein R5 is a hydrogen atom, a C¿1-4? alkyl group, an alkali metal, an alkaline earth metal or an ammonium group and R?6¿ is a hydrogen atom or a C¿1-4? 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）表示的羟基甲磺酸类似物：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是1〜5的整数， n是0〜4的整数，R 1是C 1-8〜 烷基，C3-8环烷基，被C3-8环烷基取代的C1-4烷基，被芳基取代的C1-4烷基或被芳氧基取代的C1-4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水合物。 本发明的化合物可用作弹性蛋白酶释放抑制剂。