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1. 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。

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

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。

4. 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。

5. 发明授权

US4534980A Antiinflammatory and antipyretic cream 失效
标题翻译：抗炎和解热霜
公开(公告)号：US4534980A
公开(公告)日：1985-08-13
申请号：US633139
申请日：1984-07-23
申请人： Yasuo Itoh , Hideo Kato , Kugako Matsumura , Tomoyasu Nishikawa , Akira Hisano , Takehisa Yamada , Eiichi Koshinaka
发明人： Yasuo Itoh , Hideo Kato , Kugako Matsumura , Tomoyasu Nishikawa , Akira Hisano , Takehisa Yamada , Eiichi Koshinaka
IPC分类号： A61K9/06 , A61K9/00 , A61K31/165 , A61K31/19 , A61K47/00 , A61K47/16 , A61K47/18 , A61P17/00 , A61P25/04 , A61P29/00
CPC分类号： A61K9/0014 , A61K31/165 , A61K31/19 , A61K47/18 , Y10S514/871
摘要： Creams for external or topical use comprising ketoprofen as an effective component and crotamiton as an agent for preventing crystalline precipitation of the effective component. The creams possess an antiinflammatory and antipyretic effect and are excellent in permeation and absorption into the skin which enables the topical and external use of the creams.
摘要翻译：用于外用或局部用途的霜剂，其包含酮洛芬作为有效成分，克罗他米通作为用于防止有效成分的结晶沉淀的试剂。乳霜具有抗炎和解热作用，并且在皮肤中的渗透和吸收优异，能够局部和外部使用霜剂。

6. 发明授权

US4612329A Pharmaceutical alpha-aminoalkyl-alpha-alkylphenylacetonitriles 失效
标题翻译：药物α-氨基烷基-α-烷基苯基乙腈
公开(公告)号：US4612329A
公开(公告)日：1986-09-16
申请号：US786742
申请日：1985-10-11
申请人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Sakae Kurata , Hiroyuki Nishino , Toshihiko Yoshida
发明人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Sakae Kurata , Hiroyuki Nishino , Toshihiko Yoshida
IPC分类号： A61K31/275 , A61K31/445 , C07C20060101 , C07C255/58 , C07D20060101 , C07D211/08 , C07D295/08 , C07C121/78
CPC分类号： C07C255/00
摘要： Novel alpha-aminoalkyl-alpha-alkylphenylacetonitrile derivatives useful for treatment of cartino vaso diseases, a peripheral circulatory insufficiency and cerebral circulation failure are disclosed.
摘要翻译：公开了用于治疗纸浆血管疾病，外周循环功能不全和脑循环衰竭的新型α-氨基烷基-α-烷基苯基乙腈衍生物。

7. 发明授权

US4983633A Amide compounds, process for preparing the same, and composition for activating gastric motor function containing the same 失效
标题翻译：酰胺化合物，其制备方法和用于激活含有其的运动功能的组合物
公开(公告)号：US4983633A
公开(公告)日：1991-01-08
申请号：US241028
申请日：1988-09-02
申请人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Hiroyuki Nishino , Jun Sakaguchi
发明人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Hiroyuki Nishino , Jun Sakaguchi
IPC分类号： A61K31/165 , C07C233/12 , C07C233/73 , C07C235/48 , C07C311/15 , C07D295/08 , C07D295/092 , C07D317/68
CPC分类号： C07D295/088 , C07C255/00 , C07D317/68
摘要： Amide-compounds represented by the formula (I): ##STR1## wherein R.sub.1 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino which can be substituted by lower alkyl, nitro, cyano, sulfamoyl which can be substituted by lower alkyl, R.sub.2 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino, nitro, wherein R.sub.1 and R.sub.2 can be combined to form methylenedioxy, R.sub.3 means hydrogen, lower alkyl, halogen, or amino, R.sub.4 and R.sub.5 may be the same or different and each represents lower alkyl or wherein R.sub.4 and R.sub.5 may be combined together with nitrogen to form 1-pyrrolidinyl or piperidino, and pharmacologically-acceptable acid-addition salts thereof, which exhibit excellent effects in the activation of gastric motor function, a process for preparation pharmaceutical compositons thereof, as well as a method for the treatment of a subject suffering from an ailment associated with inadequate gastric motor function by administrating such a compound to the said subject, are all disclosed.

8. 发明授权

US4912116A Propiophenone derivatives for treatment of pollakiuria (frequency urination) 失效
标题翻译：用于治疗尿频的苯丙酮衍生物（排尿）
公开(公告)号：US4912116A
公开(公告)日：1990-03-27
申请号：US136912
申请日：1987-12-22
申请人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Kouji Morikawa , Toshie Yamauchi
发明人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Kouji Morikawa , Toshie Yamauchi
IPC分类号： C07D295/10 , A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/445 , A61K31/535 , A61K31/54 , A61K31/55 , A61P13/02 , A61P15/00 , C07D307/79 , C07D317/58 , C07D405/06
CPC分类号： A61K31/535 , A61K31/40 , A61K31/445 , A61K31/55 , Y10S514/906
摘要： A method for the treatment of pollakiurea in a subject in need thereof, comprising the step of administering to said subject an effective antipollakiurea amount of a propiophenone of the formula (I) ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each independently represents hydrogen, halogen, lower alkyl- or halogeno-lower-alkyl, lower-alkoxy, or cycloalkyl having 3-8 carbon atoms, two of which R.sub.1, R.sub.2, and R.sub.3 groups may combine to form methylenedioxy or ethyleneoxy, R.sub.4 represents hydrogen or a lower-alkyl, and A represents pyrrolidinyl-, piperidinyl-, morpholinyl-, or azepinyl or a pharmaceutically-acceptable acid addition salt thereof, is disclosed.

9. 发明授权

US4528287A 6-Fluoro-1, 4-dihydro-4-oxo-7-substituted piperazinylquinoline-3-carboxylic acids and the method for preparing the same 失效
标题翻译： 6-氟-1,4-二氢-4-氧代-7-取代的哌嗪基喹啉-3-羧酸及其制备方法
公开(公告)号：US4528287A
公开(公告)日：1985-07-09
申请号：US651423
申请日：1984-09-17
申请人： Yasuo Itoh , Hideo Kato , Nobuo Ogawa , Eiichi Koshinaka , Tomio Suzuki , Noriyuki Yagi
发明人： Yasuo Itoh , Hideo Kato , Nobuo Ogawa , Eiichi Koshinaka , Tomio Suzuki , Noriyuki Yagi
IPC分类号： C07D401/02 , C07D215/56 , A61K31/47 , C07D401/04
CPC分类号： C07D215/56
摘要： The invention is concerned with the novel piperazinylquinoline-3-carboxylic acids represented by formula (I) ##STR1## or a pharmacologically-acceptable salt thereof, a process for the preparation of them, and a pharmaceutical composition which contains these new compounds as active ingredient and can be used as the therapeutic agent against bacteria.
摘要翻译：本发明涉及由式（I）表示的新型哌嗪基喹啉-3-羧酸或其药学上可接受的盐，其制备方法和含有这些新化合物的药物组合物作为活性成分，可以用作抗细菌的治疗剂。

10. 发明授权

US5126337A Thiazetoquinoline-3-carboxylic acid derivative and a pharmaceutical composition comprising the same 失效
标题翻译：噻唑烷-3-羧酸衍生物和包含其的药物组合物
公开(公告)号：US5126337A
公开(公告)日：1992-06-30
申请号：US505138
申请日：1990-04-05
申请人： Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Noriyuki Yagi , Toshihiko Yoshida , Tomio Suzuki
发明人： Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Noriyuki Yagi , Toshihiko Yoshida , Tomio Suzuki
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： A thiazetoquinoline-3-carboxylic acid derivative represented by the general formula (I) ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl group; R.sub.2 is a fluorine atom or a chlorine atom; R.sub.3 is a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a halogenated lower alkanoyl, or alkoxycarbonyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, and a pharmacologically acceptable salt thereof, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for the treatment of an infectious disease by administering the same, are disclosed.

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