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1. 发明授权

US4792547A Pyrazine-2-carboxamide derivatives useful in treating allergic disease 失效
标题翻译：吡嗪-2-甲酰胺衍生物，用于治疗过敏性疾病
公开(公告)号：US4792547A
公开(公告)日：1988-12-20
申请号：US941918
申请日：1986-12-15
申请人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kazuya Mitani
发明人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kazuya Mitani
IPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , A61K31/55 , A61K31/495
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14
摘要： Novel pyrazine derivatives useful for treatment of bronchial asthma, allergic gastorenteric trouble, hay fever urticaria, allertic rhinitis, and allergic conjunctivitis, and pharmaceutical compositions thereof, are disclosed. The compounds have the formula I as follows: ##STR1## wherein R represents hydrogen or ##STR2## wherein R.sub.1 and R.sub.2 may be the same or different and each independently represents hydrogen, straight or branched-chain lower-alkyl, or cycloalkyl having three to six carbon atoms inclusive, phenyl which may be substituted with halogen, lower-alkyl, or lower-alkoxy, or wherein R.sub.1 and R.sub.2 together represent alkylene of four to six carbon atoms, inclusive, optionally interrupted by one or two nitrogen atoms or one oxygen atom and said ring being optionally substituted by straight or branched-chain lower-alkyl having one to six carbon atoms inclusive, hydroxy, or phenyl,and pharmaceutically-acceptable salts thereof.
摘要翻译：用于治疗支气管哮喘，过敏性胃炎，花粉荨麻疹，过敏性鼻炎和过敏性结膜炎的新颖吡嗪衍生物及其药物组合物。化合物具有如下式I：其中R表示氢或者其中R 1和R 2可以相同或不同，并且各自独立地表示氢，直链或支链低级烷基或具有三个至 6个碳原子，可被卤素，低级烷基或低级烷氧基取代的苯基，或其中R 1和R 2一起代表四至六个碳原子的亚烷基，包括任选地被一个或两个氮原子或一个氧所述环任选被具有1-6个碳原子的直链或支链低级烷基，羟基或苯基取代，及其药学上可接受的盐。

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

US4525356A N-substituted flavone-8-carboxamides 失效
标题翻译： N-取代的黄酮-8-甲酰胺
公开(公告)号：US4525356A
公开(公告)日：1985-06-25
申请号：US546481
申请日：1983-10-28
申请人： Yasuo Itho , Hideo Kato , Nobuo Ogawa , Kagari Yamagishi , Eiichi Koshinaka , Kazuya Mitani
发明人： Yasuo Itho , Hideo Kato , Nobuo Ogawa , Kagari Yamagishi , Eiichi Koshinaka , Kazuya Mitani
IPC分类号： C07D311/30 , C07D405/12 , A61K31/35 , C07D405/10
CPC分类号： C07D405/12 , C07D311/30
摘要： Derivatives of N-substituted flavone-8-carboxamides represented by general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an ethyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a halogen atom or a nitro group, R.sub.3 represents a hydrogen atom or a lower alkyl group, k represents 0, 1, 2, or 3, m represents 0 or 1; X and Y, which must be different, represent a hydrogen atom or methyl group. A represents an amino group having the formula ##STR2## wherein, R.sub.4 and R.sub.5, which may be the same or different, represent a lower alkyl group or a cyclic amino group together with the nitrogen atom and with or without an oxygen atom, R.sub.6 represents a lower alkyl group and n represents 2 or 3, are disclosed, as well as pharmaceutical compositions thereof and method of treating therewith.The N-substituted flavone-8-carboxamides derivatives are useful as agents for treatment of dysurea.
摘要翻译：由通式（I）表示的N-取代的黄酮-8-甲酰胺的衍生物其中R1表示氢原子，甲基或乙基，R2表示氢原子，低级烷基，低级烷氧基卤素原子或硝基，R3表示氢原子或低级烷基，k表示0,1,2或3，m表示0或1; X和Y必须不同，表示氢原子或甲基。 A表示具有式“IMAGE”的氨基，其中可以相同或不同的R 4和R 5与氮原子一起表示低级烷基或环状氨基，并且具有或不具有氧原子，R6表示低级烷基和n代表2或3，以及其药物组合物和其处理方法。 N-取代的黄酮-8-甲酰胺衍生物可用作治疗尿素的药剂。

4. 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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