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1. 发明授权

US5597848A Benzenesulfonamide derivatives and use thereof 失效
标题翻译：苯磺酰胺衍生物及其用途
公开(公告)号：US5597848A
公开(公告)日：1997-01-28
申请号：US397068
申请日：1995-03-16
申请人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Nobuo Ogawa , Shunichiro Sakurai , Tomio Suzuki
发明人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Nobuo Ogawa , Shunichiro Sakurai , Tomio Suzuki
IPC分类号： C07C311/19 , C07C311/29 , A61K31/24
CPC分类号： C07C311/29 , C07C311/19
摘要： A benzenesulfonamide derivative represented by the following general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group or a halogen atom; R.sup.2 represents a C.sub.1 -C.sub.10 straight- or branched-chain alkyl group, a C.sub.3 -C.sub.8 cycloalkyl group which may be substituted with one or more C.sub.1 -C.sub.6 alkyl groups on its ring, a C.sub.1 -C.sub.6 alkyl group substituted with one or more C.sub.3 -C.sub.8 cycloalkyl groups, 1-adamantylmethyl group, 2-norbornylmethyl group, or a C.sub.1 -C.sub.6 alkyl group substituted with one or more phenyl groups whose benzene ring may have one or more substituents; R.sup.3 represents a hydrogen atom or a lower alkyl group; and n is an integer of from 2 to 4, and a pharmacologically acceptable salt thereof. The present compounds have thromboxane A.sub.2 antagonistic activity, leucotriene antagonistic activity and the like and useful as a platelet aggregation inhibitor, antithrombotic agent, antiasthmatic agent and antiallergic agent.
摘要翻译： PCT No.PCT / JP93 / 01382 Sec。 371日期1995年3月16日 102（e）1995年3月16日PCT PCT 1993年9月29日PCT公布。公开号WO94 / 07848 日本1994年4月14日由以下通式表示的苯磺酰胺衍生物：其中R 1表示氢原子，低级烷基，低级烷氧基或卤素原子; R2表示C1-C10直链或支链烷基，可以在其环上被一个或多个C 1 -C 6烷基取代的C 3 -C 8环烷基，被一个或多个C 3取代的C 1 -C 6烷基 -C8环烷基，1-金刚烷基甲基，2-降冰片基甲基或被苯环可以具有一个或多个取代基的一个或多个苯基取代的C 1 -C 6烷基; R3表示氢原子或低级烷基; n为2〜4的整数，及其药理学上可接受的盐。本发明化合物具有血栓素A2拮抗活性，白三烯拮抗活性等，可用作血小板聚集抑制剂，抗血栓形成剂，止喘剂和抗过敏剂。

2. 发明授权

US4971990A Phenoxyethylamine derivatives, for preparing the same and composition for exhibiting excellent .alpha..sub.1 -blocking activity containing the same 失效
标题翻译：苯氧基乙胺衍生物，其制备方法和用于表现出优异的α1-阻断活性的组合物
公开(公告)号：US4971990A
公开(公告)日：1990-11-20
申请号：US301354
申请日：1989-01-24
申请人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kazuya Mitani , Shunichiro Sakurai
发明人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kazuya Mitani , Shunichiro Sakurai
IPC分类号： C07C311/27 , C07D295/26
CPC分类号： C07D295/26 , C07C311/27
摘要： Phenoxyethylamine derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 and R.sub.5 represent lower-alkyl, R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen or lower-alkyl, or ##STR2## represents a 5- or 6-membered ring system which may include nitrogen, oxygen or sulfur as a ring membered atom, R.sub.4 represents hydrogen or lower-alkyl, and n represents an integer selected from 1 to 3, their optical isomers and pharmacologically-acceptable acid addition salts, which exhibit excellent .alpha..sub.1 -blocking activity, a process for their preparation, pharmaceutical compositions thereof, and a method for the treatment of a subject afflicted with hypertension or dysuria by administrating such a compound, are all disclosed.

3. 发明授权

US4943581A Isoquinolinesulfonamides 失效
标题翻译：异喹啉磺酰胺
公开(公告)号：US4943581A
公开(公告)日：1990-07-24
申请号：US371392
申请日：1989-06-26
申请人： Hiroyoshi Hidaka , Toshio Tanaka , Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Kazuya Mitani , Shunichiro Sakurai
发明人： Hiroyoshi Hidaka , Toshio Tanaka , Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Kazuya Mitani , Shunichiro Sakurai
IPC分类号： C07D217/02 , A61K31/47 , A61K31/472 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D217/04
CPC分类号： C07D217/04 , Y02P20/55
摘要： An isoquinolinesulfonamide selected from those represented by the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different, and each represent hydrogen or lower-alkyl, and X represents hydrogen or halogen, and pharmacologically-acceptable acid addition salts thereof, pharmaceutical compositions thereof, and use thereof in the treatment of circular disorders, are disclosed.
摘要翻译：选自由下式表示的异喹啉磺酰胺：其中R 1，R 2和R 3可以相同或不同，并且各自表示氢或低级烷基，X表示氢或卤素，以及其药学上可接受的酸加成盐，其药物组合物及其在治疗循环障碍中的用途。

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