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1. 发明授权

US5110820A Dihydropyridine compounds which process both calcium (2+)-antagonistic and beta receptor blocking activities 失效
标题翻译：二钙二氢化合物（2 +） - 拮抗剂和受体阻断活性
公开(公告)号：US5110820A
公开(公告)日：1992-05-05
申请号：US611340
申请日：1990-11-13
申请人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Masaharu Asano , Toichi Takenaka
发明人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Masaharu Asano , Toichi Takenaka
IPC分类号： A61K31/4427 , A61K31/455 , A61P3/00 , A61P3/14 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07D211/90
摘要： Dihydropyridine compounds and salts thereof are provided which exhibit both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities and therefore are useful for the treatment of ischemic heart diseases and hypertension. The compounds have the formula ##STR1## wherein A represents a straight or branched carbon chain alkylene group having 1 to 10 carbon atoms which may be interrupted by an oxygen atom(s); R.sup.1 and R.sup.4, which may be the same or different, each represents a lower alkyl group; R.sup.2 represents an amino group, ##STR2## R.sup.3 represents a straight or branched carbon chain alkyl group having 1 to 10 carbon atoms which may be interrupted by an oxygen atom(s), or ##STR3## R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a trifluoromethyl group, a cyano group, a lower alkyl group, a lower alkoxy group or a lower alkenyloxy group; R.sup.7 represents a hydrogen atom, a cyano group, a halogen atom, a lower alkoxy group or a lower alkanoyl group; R.sup.8 and R.sup.9, which may be the same or different, each represents a lower alkyl group or an aralkyl group; and n represents an integer of 1 to 2: these symbols, hereafter, have the same significances.
摘要翻译：提供二氢吡啶化合物及其盐，其表现出Ca 2+ +拮抗性和肾上腺素能β受体阻断活性，因此可用于治疗缺血性心脏病和高血压。化合物具有式（I）的化合物，其中A表示可被氧原子间隔的具有1-10个碳原子的直链或支链碳链亚烷基; R 1和R 4可以相同或不同，各自表示低级烷基; R 2表示氨基，R 3表示可被氧原子间隔的具有1〜10个碳原子的直链或支链碳链烷基，或者R 5和R 6 可以相同或不同，分别表示氢原子，硝基，卤素原子，三氟甲基，氰基，低级烷基，低级烷氧基或低级链烯氧基。 R7表示氢原子，氰基，卤素原子，低级烷氧基或低级烷酰基; R 8和R 9可以相同或不同，各自表示低级烷基或芳烷基; n表示1〜2的整数，以下，符号相同。

2. 发明授权

US4727082A Dihydropyridine compounds and pharmaceutical compositions containing them 失效
标题翻译：二氢吡啶化合物和含有它们的药物组合物
公开(公告)号：US4727082A
公开(公告)日：1988-02-23
申请号：US908350
申请日：1986-09-17
申请人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Yasuo Isomura , Masaharu Asano , Toichi Takenaka
发明人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Yasuo Isomura , Masaharu Asano , Toichi Takenaka
IPC分类号： C07D211/82 , A61K31/44 , A61K31/455 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P25/28 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07C317/00 , C07C323/00 , C07D211/90
摘要： A dihydropyridine compound of the following general formula (I) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, each represents a C.sub.1 to C.sub.10 alkyl group, a lower alkyl group which is interrupted by oxygen atom(s), or a lower alkyl group substituted by C.sub.3 to C.sub.6 alicyclic group(s); R.sup.3 and R.sup.4, which are the same or different, each represents a lower alkyl group; R.sup.5 and R.sup.6, which are the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkylsulfonyl group, or a lower alkylsulfinyl group; R.sup.7 and R.sup.8, which are the same or different, each represents a hydrogen atom, a halogen atom, a cyano group, a lower alkoxy group, or a lower alkanoylamino group, or R.sup.7 may combine with R.sup.8 to form a naphthyl group together with the adjacent phenyl group; A represents a single bond, a vinylene group (--CH.dbd.CH--), or a ethynylene group (--C.dbd.C--); B represents a single bond or --CH.sub. 2 O--; and m and n, which are the same or different, each represents 0 or an integer of 1 to 5.The compounds are useful for the treatment of various cardiovascular disorders, since they possess both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities.
摘要翻译：下列通式（I）的二氢吡啶化合物或其盐：其中R 1和R 2相同或不同，各自表示C1至C10烷基，低级烷基其被氧原子或被C3-C6脂环族基团取代的低级烷基取代; R 3和R 4相同或不同，各自表示低级烷基; R 5和R 6相同或不同，分别表示氢原子，硝基，卤素原子，低级烷基，低级烷氧基，低级烷硫基，低级烷基磺酰基或低级烷基亚磺酰基 ; R 7和R 8相同或不同，各自表示氢原子，卤素原子，氰基，低级烷氧基或低级烷酰氨基，或者可以与R 8结合形成萘基，相邻苯基; A表示单键，亚乙烯基（-CH = CH-）或亚乙炔基（-C = C-）; B表示单键或-CH 2 O-; 和m和n相同或不同，各自表示0或1至5的整数。该化合物可用于治疗各种心血管疾病，因为它们具有Ca 2+拮抗剂和肾上腺素能β受体阻断活性。

3. 发明授权

US5591757A Dihydropyridine composition 失效
标题翻译：二氢吡啶组成
公开(公告)号：US5591757A
公开(公告)日：1997-01-07
申请号：US418262
申请日：1995-04-06
申请人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Masaharu Asano , Toichi Takenaka
发明人： Takashi Fujikura , Noriki Ito , Yuzo Matsumoto , Masaharu Asano , Toichi Takenaka
IPC分类号： A61K31/4427 , A61K31/455 , A61P3/00 , A61P3/14 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07D211/90
摘要： Pharmaceutical composition of certain dihydropyridine compounds and salts thereof are provided which exhibit both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities and therefore are useful for the treatment of ischemic heart diseases and hypertension. The pharmaceutical compositions contains either 4-(2-hydroxy-3-phenoxy-propylamino)-butyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate or 6-(2-hydroxy-3-phenoxypropylamino) hexyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate or their pharmaceutically acceptable salts.
摘要翻译：提供某些二氢吡啶化合物及其盐的药物组合物，其表现出Ca 2+拮抗剂和肾上腺素能β受体阻断活性，因此可用于治疗缺血性心脏病和高血压。药物组合物含有4-（2-羟基-3-苯氧基 - 丙基氨基） - 丁基甲基2,6-二甲基-4-（间硝基苯基）-1,4-二氢吡啶-3,5-二羧酸酯或6-（ 2-羟基-3-苯氧基丙基氨基）己基甲基2,6-二甲基-4-（间硝基苯基）-1,4-二氢吡啶-3,5-二羧酸酯或其药学上可接受的盐。

4. 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。

5. 发明授权

US5063246A Phenethylamine derivative compositions and use 失效
标题翻译：苯乙烯衍生物组合物和用途
公开(公告)号：US5063246A
公开(公告)日：1991-11-05
申请号：US569780
申请日：1990-08-21
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： A61K20060101 , A61K31/135 , A61K31/255
CPC分类号： A61K31/135 , A61K31/255
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 0-2and the acid addition salts thereof.These compounds exhibit a strong .alpha.-adrenergic blocking action and are useful as an antihypertensive agent.

6. 发明授权

US4868216A 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：US4868216A
公开(公告)日：1989-09-19
申请号：US311366
申请日：1989-02-14
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
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.

7. 发明授权

US4880841A Process of producing phenethylamine derivatives 失效
标题翻译：生产苯乙胺衍生物的方法
公开(公告)号：US4880841A
公开(公告)日：1989-11-14
申请号：US307200
申请日：1989-02-03
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： A61K20060101 , A61K31/135 , A61K31/255
CPC分类号： A61K31/135 , A61K31/255
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.-adreneregic 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烈的α肾上腺素能阻断作用，可用作抗高血压药。

8. 发明授权

US4703063A Sulfamoyl substituted phenethylamine derivatives and process of producing them 失效
标题翻译：磺酰胺取代的苯乙胺衍生物及其制备方法
公开(公告)号：US4703063A
公开(公告)日：1987-10-27
申请号：US756790
申请日：1985-07-18
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 , 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 , C07C143/78 , 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.

9. 发明授权

US4217305A Phenylethanolamine derivatives 失效
标题翻译：苯乙醇胺衍生物
公开(公告)号：US4217305A
公开(公告)日：1980-08-12
申请号：US946192
申请日：1978-09-27
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： C07C311/37 , A61K31/137 , A61P9/12 , C07C43/23 , C07C317/32 , C07C323/67 , C07D303/34 , C07D317/64 , C07D319/20 , C07C143/78 , A61K31/18 , A61K31/335 , C07D319/18
CPC分类号： C07D317/64 , C07C43/23 , C07D303/34 , C07D319/20
摘要： Novel phenylethanolamine derivatives represented by the formula ##STR1## wherein R represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, an amino group, a lower acylamino group, a lower alkylsulfonyl group, or a lower alkylsulfonylamino group; R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, each represents hydrogen or a lower alkyl group; R.sub.5 represents an aryl group which may have a substituent, a benzodioxane ring group which may have a substituent, an aryloxy group which may have a substituent, or an arylthio group which may have a substituent; said R.sub.5 being, however, a benzodioxane ring group which may have a substituent, an aryloxy group which may have a substituent, or an arylthio group which may have a substituent when R is a hydroxyl group; and n represents 0 or an integer of 1-3 and the acid addition salts thereof.The compounds of this invention exhibit .alpha.- and .beta.-adrenergic blocking actions and are useful as antihypertensive agents.
摘要翻译：其中R表示氢原子，卤素原子，羟基，低级烷基，低级烷氧基，低级烷硫基，氨基，低级酰氨基，低级烷基氨基，低级烷基磺酰基或低级烷基磺酰基氨基; R 1，R 2，R 3和R 4可以相同或不同，各自表示氢或低级烷基; R5表示可以具有取代基的芳基，可以具有取代基的苯并二恶烷环基，可以具有取代基的芳氧基或可以具有取代基的芳硫基; 然而，R 5表示可以具有取代基的苯并二恶烷环基，可以具有取代基的芳氧基或当R为羟基时可具有取代基的芳硫基; n表示0或1-3的整数，以及其酸加成盐。本发明的化合物显示出α-和β-肾上腺素能阻断作用并且可用作抗高血压药。

10. 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。

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