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1. 发明授权

US4826814A Tripeptide derivatives 失效
公开(公告)号：US4826814A
公开(公告)日：1989-05-02
申请号：US046189
申请日：1987-05-05
申请人： Tadahiro Sawayama , Masatoshi Tsukamoto , Takashi Sasagawa , Kazuya Nishimura , Kanoo Hosoki , Kunihiko Takeyama
发明人： Tadahiro Sawayama , Masatoshi Tsukamoto , Takashi Sasagawa , Kazuya Nishimura , Kanoo Hosoki , Kunihiko Takeyama
IPC分类号： A61K38/00 , A61K38/05 , A61K38/06 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/068 , C07K5/08 , C07K14/81 , A61K37/43
CPC分类号： C07K5/06086 , C07K5/0215 , A61K38/00
摘要： There are provided tripeptide compounds represented by the following formula ##STR1## wherein R.sub.1 represents a C.sub.1-10 alkyl group, a C.sub.4-7 cycloalkyl or C.sub.5-7 cycloalkyl-lower alkyl group, a phenyl or phenyl-lower alkyl group in which the benzene ring may optionally be substituted by a substituent selected from halogen, lower alkyl, lower alkoxy, phenyl, methylenedioxy, ethylenedioxy, amino, di(lower alkyl)amino and hydroxy, a naphthyl or naphthyl-lower alkyl group in which the naphthalene ring may optionally be substituted by a substituent selected from halogen, lower alkyl, lower alkoxy and hydroxy, a heterocyclic or heterocyclic-lower alkyl group in which the heterocycle is a saturated or unsaturated 5- or 6-membered ring containing a nitrogen, oxygen or sulfur atom as the hetero atom, and may optionally be substituted by a substituent selected from halogen, lower alkyl, lower alkoxy, amino, di(lower alkyl)amino, hydroxy, oxo and saturated 5- or 6-membered nitrogen-containing heterocyclic group, and further may optionally be fused to a benzene ring, or an imidazolylvinyl group; R.sub.2 represents a hydrogen atom, a C.sub.1-10 alkyl group or a benzyl group; R.sub.3 represents a group of the formula ##STR2## represents a benzene, cyclopentane or cyclohexane ring, R.sub.4 represents a hydrogen atom, a C.sub.1-10 alkyl group or a benzyl group, p is 0 or 1, q is 1, 2, or 3, and X represents a phenyl group which may optionally be substituted by a substituent selected from halogen, lower alkoxy and hydroxy, a C.sub.4-8 cycloalkyl group, or a C.sub.5-7 cycloalkyl group which is fused to a benzene, and Y represents a hydrogen atom or a lower alkyl group, or X and Y, together with the nitrogen and carbon atoms to which they are bonded, forms a 5- or 6-membered heterocycle which may contain a nitrogen, oxygen or sulfur atom,W represents a single bond, --O-- or --NH--, T represents a single bond, ##STR3## and m is 2 or 3, or salts thereof and processes for production thereof. The compounds are useful as antihypertensive agents.

2. 发明授权

US5179125A N-substituted mercaptopropanamide derivatives 失效
标题翻译： N-取代巯基丙酰胺衍生物
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。

3. 发明授权

US5210266A N-substituted mercaptopropanamide derivatives 失效
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.

4. 发明授权

US4299945A Thermoplastic polyamide imide copolymers and method of preparation 失效
标题翻译：热塑性聚酰胺酰亚胺共聚物及其制备方法
公开(公告)号：US4299945A
公开(公告)日：1981-11-10
申请号：US133854
申请日：1980-03-25
申请人： Toshihiko Aya , Takashi Sasagawa , Sho Kadoi
发明人： Toshihiko Aya , Takashi Sasagawa , Sho Kadoi
IPC分类号： C08G73/00 , C08G73/14 , C08G69/32
CPC分类号： C08G73/14
摘要： Thermoplastic polyamide imide copolymers are provided which are excellent in both heat stability and melt viscosity characteristics at a temperature of from about 300.degree. C. to about 400.degree. C., and method of preparation.
摘要翻译：提供热塑性聚酰胺酰亚胺共聚物，其在约300℃至约400℃的温度下的热稳定性和熔体粘度特性都优异，以及制备方法。

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