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公开(公告)号：EP1425258A2
公开(公告)日：2004-06-09
申请号：EP02761383.5
申请日：2002-09-09
发明人： FALCK, John R. , MIYATA, Noriyuki , ONO, Naoya , CHONAN, Tomomichi , HIRANO, Hitomi , TODA, Yoshihisa , TANAMI, Tohru , OKUYAMA, Shigeru
IPC分类号： C07C59/00 , C07C255/00 , A61K31/42 , A61K31/425 , C07D277/00
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 hydroxyeicosenoic acid analog represented by the following Formula (I), the bond represents a cis-vinylene group or an ethynylene group; Y represents CH2, O or S(O)p wherein p is 0, 1 or 2; m represents an integer of 1 to 4 inclusive; n represents an integer of 0 to 3 inclusive; the sum of m and n is an integer of 3 to 7 inclusive; R1 represents a C1-4 alkyl group or a C3-8 cycloalkyl group; R2 represents a hydrogen atom or a methyl group; R3 represents COR4, a nitrile group, a halogen atom, a tetrazole group or a thiazolidinedione group; R4 represents OR6, NHR6, N(OH)R?6, NHSO2R5¿, glycerol or functionalized glycerols; R5 represents a C¿1-15? alkyl group, a C6-10 aryl group or a C7-14 aryl group substituted with alkyl groups, halogens or amino groups; R?6¿ represents a hydrogen, a C¿1-10? alkyl group or a C1-10 alkyl group substituted with a hydroxyl group, or a pharmaceutically acceptable salt or hydrate thereof. The compounds of the present invention are useful as an elastase release inhibitor.
摘要翻译： 由下式（I）表示的羟基二十碳烯酸类似物，该键代表顺式亚乙烯基或亚乙炔基; Y代表CH 2，O或S（O）p，其中p是0,1或2; m表示1〜4的整数， n表示0〜3的整数， m和n的总和是3〜7的整数， R1代表C1-4烷基或C3-8环烷基; R2代表氢原子或甲基; R3代表COR4，腈基，卤素原子，四唑基或噻唑烷二酮基; R4代表OR6，NHR6，N（OH）R6 6，NHSO2R5，甘油或官能化甘油; R5代表C 1-15？ 烷基，被烷基，卤素或氨基取代的C 6-10芳基或C 7-14芳基; R 6表示氢，C 1-10 - 烷基或被羟基取代的C1-10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。
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