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1. 发明授权

US4973576A Bisphophonic acid derivatives and pharmaceutical compositions containing the same 失效
标题翻译：双膦酸衍生物和含有它们的药物组合物
公开(公告)号：US4973576A
公开(公告)日：1990-11-27
申请号：US165741
申请日：1988-03-09
申请人： Shuichi Sakamoto , Makoto Takeuchi , Yasuo Isomura , Kunihiro Niigata , Tetsushi Abe , Kousei Kawamuki , Masafumi Kudou
发明人： Shuichi Sakamoto , Makoto Takeuchi , Yasuo Isomura , Kunihiro Niigata , Tetsushi Abe , Kousei Kawamuki , Masafumi Kudou
IPC分类号： C07F9/653
CPC分类号： C07F9/653
摘要： "Novel bisphosphonic acid derivatives, and a bone resorption-inhibitor and an anti-arthritis containing a bisphosphonic acid derivative represented by the formula (I): ##STR1## wherein R.sup.2 represents a hydrogen atom, an alkyl group, etc.,R.sup.2 represents a hydrogen atom or a lower alkanoyl group,R.sup.3, R.sup.4, R.sup.5 and R.sup.6 may be the same or different, each represents a hydrogen atom or lower alkyl group."

2. 发明授权

US5198587A Phenethylamine derivatives 失效
标题翻译：苯乙胺衍生物
公开(公告)号：US5198587A
公开(公告)日：1993-03-30
申请号：US737976
申请日：1991-07-30
申请人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto , Toichi Takenaka , Kazuo Honda
发明人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto , Toichi Takenaka , Kazuo Honda
IPC分类号： C07C217/60
CPC分类号： C07C217/60
摘要： Phenethylamine derivatives shown by the general formula ##STR1## wherein Ro represents a lower alkyl group; R.sub.1 represents a lower alkyl group or a lower alkoxy group; R.sub.2 represents hydrogen atom or a hydroxyl group; R.sub.3 and R.sub.4 each represents hydrogen atom or a lower alkyl group; R.sub.5 represents hydrogen atom or a lower alkoxy group; X represents oxygen atom or a methylene group; m is an integer of 1-3; and n is an integer of 0-2 and the acid addition salts thereof.These compounds exhibit a strong .alpha.-adrenergic blocking action and are useful as an antihypertensive agent.
摘要翻译：苯乙胺衍生物，其通式为：其中R a代表低级烷基; R1表示低级烷基或低级烷氧基; R2表示氢原子或羟基; R3和R4各自表示氢原子或低级烷基; R5表示氢原子或低级烷氧基; X表示氧原子或亚甲基; m为1-3的整数; n为0-2的整数，及其酸加成盐。这些化合物表现出强的α-肾上腺素能阻断作用，可用作抗高血压药。

3. 发明授权

US4987152A Use of sulfamoyl-substituted phenethylamine derivatives in treatment of lower urinary tract dysfunction 失效
标题翻译：使用氨磺酰取代的苯乙胺衍生物治疗下尿路功能障碍
公开(公告)号：US4987152A
公开(公告)日：1991-01-22
申请号：US436125
申请日：1989-11-13
申请人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto
发明人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto
IPC分类号： A61K31/18 , A61K31/205 , A61K31/255 , A61P9/04 , A61P9/12 , C07C67/00 , C07C301/00 , C07C303/40 , C07C311/15 , C07C311/16 , C07C311/29 , C07C311/37 , C07C317/00 , C07D203/10
CPC分类号： C07D203/10 , C07C309/00
摘要： Novel sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure.

4. 发明授权

US5508296A Bisheterocyclic derivative or salt thereof 失效
标题翻译： Bephropocyclic衍生物或其盐
公开(公告)号：US5508296A
公开(公告)日：1996-04-16
申请号：US190093
申请日：1994-01-31
申请人： Kunihiro Niigata , Takumi Takahashi , Takashi Yoneda , Osamu Noshiro , Reiko Koike , Akiyoshi Shimaya
发明人： Kunihiro Niigata , Takumi Takahashi , Takashi Yoneda , Osamu Noshiro , Reiko Koike , Akiyoshi Shimaya
IPC分类号： C07D263/44 , C07D277/20 , C07D277/34 , C07D277/36 , C07D493/04 , A61K31/42 , A61K31/425
CPC分类号： C07D263/44 , C07D277/20 , C07D277/34 , C07D493/04 , Y02P20/55
摘要： ##STR1## A bisheterocyclic compound represented by general formula (I), stereoisomers thereof, tautomers thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a pharmaceutical composition containing the same, and a process for the production thereof. In formula (I), R
1 and R
2 may be the same or different from each other and each represents (II) or (III), R
3 represents hydrogen or a protective group, X, Y
1 and Y
2 may be the same or different from one another and each represents oxygen or sulfur, B
1 and B
2 represent each phenylene, B
3 represents phenylene, naphthylene, cyclohexylene or furo[3,2-b]furanylene, L
1 and L
2 represent each --(O)
n --A--, n represents 0 or 1, and A represents a single bond or lower alkylene, provided that when n is 1, A represents alkylene and the oxygen atom of each of L
1 and L
2 is bonded to B
3 . The above compounds are useful as a hypoglycemic drug based on the activity of enhancing insulin sensitivity.
摘要翻译： PCT No.PCT / JP92 / 00954 Sec。 371日期1994年1月31日 102（e）日期1994年1月31日PCT提交1992年7月28日PCT公布。公开号WO93 / 03021 通式（I）其通式（I），其立体异构体，其互变异构体，其药学上可接受的盐或药学上可接受的溶剂化物，含有相同，以及其生产方法。在式（I）中，R 1和R 2可以相同或不同，各自表示（II）或（III），R 3表示氢或保护基，X，Y 1和Y 2可以相同或不同另一个和每个代表氧或硫，B1和B2表示各亚苯基，B3表示亚苯基，亚萘基，亚环己基或呋喃并[3,2-b]呋喃，L1和L2表示 - （O）nA-，n表示0或1 A表示单键或低级亚烷基，条件是当n为1时，A表示亚烷基，L1和L2各自的氧原子与B3结合。基于增强胰岛素敏感性的活性，上述化合物可用作降血糖药物。

5. 发明授权

US4761500A Sulfamoyl-substituted phenethylamine derivatives, their preparation, and pharmaceutical compositions, containing them 失效
标题翻译：磺酰胺取代的苯乙胺衍生物，它们的制备方法和含有它们的药物组合物
公开(公告)号：US4761500A
公开(公告)日：1988-08-02
申请号：US828052
申请日：1986-02-10
申请人： Kunihiro Niigata , Takashi Fujikura
发明人： Kunihiro Niigata , Takashi Fujikura
IPC分类号： A61K31/18 , A61K31/205 , A61K31/255 , A61P9/04 , A61P9/12 , C07C67/00 , C07C301/00 , C07C303/40 , C07C311/15 , C07C311/16 , C07C311/29 , C07C311/37 , C07C317/00 , C07D203/10 , C07C143/80
CPC分类号： C07D203/10 , C07C309/00
摘要： A novel process is provided for the preparation of optical isomers of certain sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking agents which can be used for various treatments such as for the treatment of congestive heart failure.

6. 发明授权

US4558156A Sulfamoyl-substituted phenethylamine derivatives 失效
标题翻译：磺酰基取代的苯乙胺衍生物
公开(公告)号：US4558156A
公开(公告)日：1985-12-10
申请号：US632258
申请日：1984-07-18
申请人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto , Toichi Takenaka
发明人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto , Toichi Takenaka
IPC分类号： A61K31/18 , C07C311/15 , C07D203/10 , C07C143/78
CPC分类号： C07D203/10 , C07C309/00
摘要： Novel sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure.
摘要翻译：新的氨磺酰取代的苯乙胺衍生物，其表现出α-肾上腺素能阻断作用并且可用作抗高血压剂和用于治疗充血性心力衰竭的药剂。

7. 发明授权

US4464384A 2-Phenylimidazo[2,1-b]benzothiazole compounds, salts thereof, process of producing them, and pharmaceutical compositions containing them 失效
标题翻译： 2-苯基咪唑并[2,1-b]苯并噻唑化合物，其盐，制备方法和含有它们的药物组合物
公开(公告)号：US4464384A
公开(公告)日：1984-08-07
申请号：US449759
申请日：1982-12-14
申请人： Kiyoshi Murase , Toshiyasu Mase , Hideki Arima , Kunihiro Niigata , Kenichi Tomioka , Shinichiro Kobayashi
发明人： Kiyoshi Murase , Toshiyasu Mase , Hideki Arima , Kunihiro Niigata , Kenichi Tomioka , Shinichiro Kobayashi
IPC分类号： C07D513/04 , A61K31/425
CPC分类号： C07D513/04
摘要： Novel 2-phenylimidazo[2,1-b]benzothiazole compounds shown by general formula I ##STR1## and the salts thereof, a process of producing the compounds, and pharmaceutical compositions containing the compounds.The compounds of this invention act on immune response, in particular, suppress a delayed type hypersensitivity reaction, and are useful as antiallergic agents, antirheumatics, therapeutic agents for autoimmune diseases, and suppressants of rejection at tissue transplantation and skin graft.
摘要翻译：由通式I所示的新型2-苯基咪唑并[2,1-b]苯并噻唑化合物及其盐，制备该化合物的方法和含有该化合物的药物组合物。本发明化合物作用于免疫应答，特别是抑制迟发型超敏反应，可用作抗过敏药，抗风湿药，自身免疫性疾病的治疗剂，组织移植和皮肤移植排斥抑制剂。

8. 发明授权

US4373106A Sulfamoyl-substituted phenethylamine derivatives and process of producing them 失效
标题翻译：磺酰基取代的苯乙胺衍生物及其制备方法
公开(公告)号：US4373106A
公开(公告)日：1983-02-08
申请号：US231421
申请日：1981-02-04
申请人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto , Toichi Takenaka
发明人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto , Toichi Takenaka
IPC分类号： A61K31/18 , A61K31/205 , A61K31/255 , A61P9/04 , A61P9/12 , C07C67/00 , C07C301/00 , C07C303/40 , C07C311/15 , C07C311/16 , C07C311/29 , C07C311/37 , C07C317/00 , C07D203/10 , C07C143/80
CPC分类号： C07D203/10 , C07C309/00
摘要： Novel sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure.
摘要翻译：新的氨磺酰取代的苯乙胺衍生物，其表现出α-肾上腺素能阻断作用并且可用作抗高血压剂和用于治疗充血性心力衰竭的药剂。

9. 发明授权

US4127675A 4-(Alkylamino-2-hydroxypropoxy)-indenes and method of use 失效
标题翻译： 4-（烷基氨基-2-羟基丙氧基） - 茚和使用方法
公开(公告)号：US4127675A
公开(公告)日：1978-11-28
申请号：US734514
申请日：1976-10-21
申请人： Masuo Murakami , Kiyoshi Murase , Kunihiro Niigata , Shiro Tachikawa , Toichi Takenaka
发明人： Masuo Murakami , Kiyoshi Murase , Kunihiro Niigata , Shiro Tachikawa , Toichi Takenaka
IPC分类号： A61K31/135 , F16B2/06 , C07C93/06
CPC分类号： A61K31/135 , F16B2/06
摘要： Novel indene derivatives represented by the general formula ##STR1## wherein R represents lower alkyl, phenylloweralkyl or lower cycloalkyl, and acid addition salts thereof useful as .beta.-receptor antagonists.
摘要翻译：由通式表示的新型茚衍生物，其中R表示低级烷基，苯基低级烷基或低级环烷基，及其作为β-受体拮抗剂的酸加成盐。

10. 发明授权

US5447958A Sulfamoyl-substituted phenethylamine derivatives, their preparation, and pharmaceutical compositions, containing them 失效
标题翻译：磺酰胺取代的苯乙胺衍生物，它们的制备方法和含有它们的药物组合物
公开(公告)号：US5447958A
公开(公告)日：1995-09-05
申请号：US314322
申请日：1994-09-28
申请人： Kunihiro Niigata , Takashi Fujikura
发明人： Kunihiro Niigata , Takashi Fujikura
IPC分类号： A61K31/18 , C07C311/16 , C07C311/24 , C07C317/14 , C07D203/10 , A01N41/06 , C07C311/10
CPC分类号： C07D203/10 , C07C309/00
摘要： Pharmaceutical compositions are provided for the treatment of disorders in a subject, such as hypertension, congestive heart failure, angina pectoris, lower urinary tract dysfunction and prostatic hypertrophy. The compositions when administered to a subject produce an .alpha.-adrenergic blocking action and contain as an active ingredient sulfamoyl-substituted phenethylamine derivatives, such as optically active 5-2-[ 2-(2-ethoxyphenoxy)ethylamino] -2-methylethyl-2-methoxybenzenesulfonamide 2-methoxybenzenesulfonamide, and a pharmaceutically acceptable carrier.
摘要翻译：提供药物组合物用于治疗受试者中的疾病，例如高血压，充血性心力衰竭，心绞痛，下尿路功能障碍和前列腺肥大。给予受试者时的组合物产生α-肾上腺素能阻断作用并含有作为活性成分的氨磺酰基取代的苯乙胺衍生物，例如光学活性的5-2- [2-（2-乙氧基苯氧基）乙基氨基] -2-甲基乙基-2 - 甲氧基苯磺酰胺2-甲氧基苯磺酰胺和药学上可接受的载体。

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