公开(公告)号：US5179125A

公开(公告)日：1993-01-12

申请号：US504654

申请日：1990-04-04

申请人： Tetsutaro Mimura ,  Yasuhisa Nakamura ,  Junko Nishino ,  Tadahiro Sawayama ,  Takashi Sasagawa ,  Takashi Deguchi ,  Hideo Nakamura

发明人： Tetsutaro Mimura ,  Yasuhisa Nakamura ,  Junko Nishino ,  Tadahiro Sawayama ,  Takashi Sasagawa ,  Takashi Deguchi ,  Hideo Nakamura

IPC分类号： C07C229/08 ,  C07C229/24 ,  C07C229/26 ,  C07C229/34 ,  C07C229/60 ,  C07C323/60 ,  C07C327/06 ,  C07C327/12 ,  C07C327/16 ,  C07C327/24 ,  C07C327/32 ,  C07C329/06 ,  C07C333/06 ,  C07D213/50 ,  C07D261/20 ,  C07D265/30 ,  C07D295/088 ,  C07D295/155 ,  C07D307/68 ,  C07D333/22 ,  C07D333/38

CPC分类号： C07D265/30 ,  C07C229/08 ,  C07C229/24 ,  C07C229/26 ,  C07C229/34 ,  C07C229/60 ,  C07C323/60 ,  C07C327/06 ,  C07C327/12 ,  C07C327/16 ,  C07C327/24 ,  C07C327/32 ,  C07C329/06 ,  C07C333/06 ,  C07D213/50 ,  C07D261/20 ,  C07D295/088 ,  C07D295/155 ,  C07D307/68 ,  C07D333/22 ,  C07D333/38 ,  C07C2101/02 ,  C07C2101/08 ,  C07C2101/16

摘要： Novel N-substituted mercaptopropanamide derivatives of the formula: ##STR1## wherein R.sub.1 is mercapto or a group convertible into mercapto when cleaved within the biobody, W is hydrogen atom, an alkyl or an aralkyl, R.sub.2 is an aryl which may optionally have substituent(s), a heterocyclic group which may optionally have substituent(s), or an alkyl which may optionally have substituent(s), X is a cycloalkylene, a cycloalkylidene, or a phenylene which may optionally have substituent(s) or may optionally be fused with other ring, and R.sub.3 is carboxyl or a group convertible into carboxyl when cleaved within the biobody, or a pharmaceutically acceptable salt thereof, and a solid solution of said N-substituted mercaptopropanamide derivative with an amino acid, which have excellent enkephalinase inhibitory activity and are useful for the treatment of mild to moderate pain, and a pharmaceutical composition containing said compounds as an active ingredient, and processes for preparing these compounds.

摘要翻译： 新型N-取代巯基丙酰胺衍生物，其分子式如下：其中R 1为巯基或当在生物体内切割时可转化成巯基的基团，W为氢原子，烷基或芳烷基，R2为可任意选择的芳基 具有取代基，可以任选具有取代基的杂环基或可任选具有取代基的烷基，X是可以任选具有取代基的亚环烷基，亚环烷基或亚苯基， 可任选地与其它环稠合，并且R3是羧基或当在生物体内切割时可转化成羧基的基团或其药学上可接受的盐，以及所述N-取代的巯基丙酰胺衍生物与氨基酸的固溶体，其具有优异的 脑啡肽酶抑制活性，并且可用于治疗轻度至中度疼痛，以及含有所述化合物作为活性成分的药物组合物，以及制备这些化合物的方法 ds。

公开(公告)号：US5210266A

公开(公告)日：1993-05-11

申请号：US609450

申请日：1990-11-05

申请人： Tetsutaro Mimura ,  Yasuhisa Nakamura ,  Junko Nishino ,  Tadahiro Sawayama ,  Takashi Sasagawa ,  Takashi Deguchi ,  Hideo Nakamura

发明人： Tetsutaro Mimura ,  Yasuhisa Nakamura ,  Junko Nishino ,  Tadahiro Sawayama ,  Takashi Sasagawa ,  Takashi Deguchi ,  Hideo Nakamura

IPC分类号： C07C229/08 ,  C07C229/24 ,  C07C229/26 ,  C07C229/34 ,  C07C229/60 ,  C07C323/60 ,  C07C327/06 ,  C07C327/12 ,  C07C327/16 ,  C07C327/24 ,  C07C327/32 ,  C07C329/06 ,  C07C333/06 ,  C07D213/50 ,  C07D261/20 ,  C07D265/30 ,  C07D295/088 ,  C07D295/155 ,  C07D307/68 ,  C07D333/22 ,  C07D333/38

CPC分类号： C07D265/30 ,  C07C229/08 ,  C07C229/24 ,  C07C229/26 ,  C07C229/34 ,  C07C229/60 ,  C07C323/60 ,  C07C327/06 ,  C07C327/12 ,  C07C327/16 ,  C07C327/24 ,  C07C327/32 ,  C07C329/06 ,  C07C333/06 ,  C07D213/50 ,  C07D261/20 ,  C07D295/088 ,  C07D295/155 ,  C07D307/68 ,  C07D333/22 ,  C07D333/38 ,  C07C2101/02 ,  C07C2101/08 ,  C07C2101/16

摘要： Novel N-substituted mercaptopropanamide derivatives of the formula: ##STR1## wherein R.sub.1 is mercapto or a group convertible into mercapto when cleaved within the biobody, W is hydrogen atom, an alkyl or an aralkyl, R.sub.2 is an aryl which may optionally have substituent(s), a heterocyclic group which may optionally have substituent(s), or an alkyl which may optionally have substituent(s), X is a cycloalkylene, a cycloalkylidene, or a phenylene which may optionally have substituent(s) or may optionally be fused with other ring, and R.sub.3 is carboxyl or a group convertible into carboxyl when cleaved within the biobody, or a pharmaceutically acceptable salt thereof, and a solid solution of said N-substituted mercaptopropanamide derivative with an amino acid, which have excellent enkephalinase inhibitory activity and are useful for the treatment of mild to moderate pain, and a pharmaceutical composition containing said compounds as an active ingredient, and processes for preparing these compounds.