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1. 发明授权

US5463064A Dihydropyridine-3,5-dicarboxylic acid ester derivatives 失效
标题翻译：二氢吡啶-3,5-二羧酸酯衍生物
公开(公告)号：US5463064A
公开(公告)日：1995-10-31
申请号：US238537
申请日：1994-05-05
申请人： Kazuharu Tamazawa , Tadao Kojima , Hideki Arima , Yukiyasu Murakami , Yasuo Isomura , Minoru Okada , Kiyoshi Takanobu , Toichi Takenaka
发明人： Kazuharu Tamazawa , Tadao Kojima , Hideki Arima , Yukiyasu Murakami , Yasuo Isomura , Minoru Okada , Kiyoshi Takanobu , Toichi Takenaka
IPC分类号： C07D207/24 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07D207/24 , C07D211/90
摘要： A dextro-rotatory optical isomer of diastereoisomer A of (.+-.)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl)ester 5-methyl ester is provided having the formula ##STR1## and wherein the melting point of the hydrochloride of the dextro-rotatory optical isomer is 223.degree. to 230.degree. C. (decomp.), or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：（+/-） - 2,6-二甲基-4-（3-硝基苯基）-1,4-二氢吡啶-3,5-二羧酸3-（1-苄基吡咯烷-3-酮）的非对映异构体A的右旋旋光异构体 - 基）酯5-甲酯，其具有式“IMAGE”，其中右旋旋光异构体的盐酸盐的熔点为223〜230℃（分解），或药学上可接受的酸加成的盐。

2. 发明授权

US4220649A 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives 失效
标题翻译： 1,4-二氢吡啶-3,5-二羧酸酯衍生物
公开(公告)号：US4220649A
公开(公告)日：1980-09-02
申请号：US8085
申请日：1979-01-31
申请人： Tadao Kojima , Toichi Takenaka
发明人： Tadao Kojima , Toichi Takenaka
IPC分类号： C07D207/12 , A61K31/44 , A61K31/4427 , A61P9/12 , C07D211/90 , C07D401/12 , C07D213/55
CPC分类号： C07D401/12 , Y10S514/929
摘要： 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives shown by the formula ##STR1## wherein R represents a lower alkyl group and R' represents a hydrogen atom, a lower alkyl group or an aralkyl group, and the therapeutically non-toxic salts thereof.These compounds possess a vasodilative activity and an antihypertensive activity.
摘要翻译：式中，R表示低级烷基，R'表示氢原子，低级烷基或芳烷基，可以列举式（I）所示的1,4-二氢吡啶-3,5-二羧酸酯衍生物，其毒性盐。这些化合物具有血管扩张活性和抗高血压活性。

3. 发明授权

US5616715A Dihydropyridine-3, 5-dicarboxylic acid ester derivatives 失效
标题翻译：二氢吡啶-3,5-二羧酸酯衍生物
公开(公告)号：US5616715A
公开(公告)日：1997-04-01
申请号：US491793
申请日：1995-06-19
申请人： Kazuharu Tamazawa , Tadao Kojima , Hideki Arima , Yukiyasu Murakami , Yasuo Isomura , Minoru Okada , Toichi Takenaka , Kiyoshi Takanobu
发明人： Kazuharu Tamazawa , Tadao Kojima , Hideki Arima , Yukiyasu Murakami , Yasuo Isomura , Minoru Okada , Toichi Takenaka , Kiyoshi Takanobu
IPC分类号： C07D207/24 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07D207/24 , C07D211/90
摘要： A process is provided for producing diastereoisomer A or a pharmaceutically acceptable acid addition salt of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl) ester 5-methyl ester which comprises subjecting a mixture of diastereoisomers A and B of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl) ester 5-methyl ester to column chromatography using silica gel as a carrier and a mixture of ethyl acetate and acetic acid as an eluant, and then separating the acetate of diastereoisomer A from the eluate, or treating the acetate with a base, or further treating the resulting diastereoisomer A with a pharmaceutically acceptable acid.
摘要翻译：提供了一种制备非对映异构体A或2,6-二甲基-4-（3-硝基苯基）-1,4-二氢吡啶-3,5-二羧酸的3-（1-苄基吡咯烷-3-基） - 基）酯5-甲酯，其包括使2,6-二甲基-4-（3-硝基苯基）-1,4-二氢吡啶-3,5-二羧酸3-（1- 苄基吡咯烷-3-基）酯将5-甲酯与硅胶作为载体和乙酸乙酯与乙酸的混合物作为洗脱剂进行柱色谱分离，然后将非对映异构体A的乙酸酯与洗脱液分离，或用碱，或用药学上可接受的酸进一步处理所得的非对映异构体A.

4. 发明授权

US5364872A Dihydropyridine-3,5-dicarboxylic acid ester derivatives 失效
标题翻译：二氢吡啶-3,5-二羧酸酯衍生物
公开(公告)号：US5364872A
公开(公告)日：1994-11-15
申请号：US826232
申请日：1992-01-23
申请人： Kazuharu Tamazawa , Tadao Kojima , Hideki Arima , Yukiyasu Murakami , Yasuo Isomura , Minoru Okada , Toichi Takenaka , Kiyoshi Takanobu
发明人： Kazuharu Tamazawa , Tadao Kojima , Hideki Arima , Yukiyasu Murakami , Yasuo Isomura , Minoru Okada , Toichi Takenaka , Kiyoshi Takanobu
IPC分类号： C07D207/24 , C07D211/90 , C07D401/12 , A61K31/44
CPC分类号： C07D401/12 , C07D207/24 , C07D211/90
摘要： The diastereoisomer A of a dihydropyridine-3,5-dicarboxylic acid ester derivative is provided as well as its pharmaceutically acceptable acid addition salts. The invention further discloses a process for producing the compounds and their use as medicaments in imparting vasodilating activity.
摘要翻译：提供二氢吡啶-3,5-二羧酸酯衍生物的非对映异构体A以及其药学上可接受的酸加成盐。本发明还公开了一种制备化合物的方法及其作为赋予血管舒张活性的药物的用途。

5. 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。

6. 发明授权

US4063025A 4-Substituted amino-.alpha.-aminomethylbenzyl alcohol derivatives 失效
标题翻译： 4-取代的氨基 - {6-氨基甲基苄醇衍生物
公开(公告)号：US4063025A
公开(公告)日：1977-12-13
申请号：US651738
申请日：1976-01-23
申请人： Masuo Murakami , Kozo Takahashi , Kiyoshi Murase , Toshiyasu Mase , Hisashi Ida , Toichi Takenaka
发明人： Masuo Murakami , Kozo Takahashi , Kiyoshi Murase , Toshiyasu Mase , Hisashi Ida , Toichi Takenaka
IPC分类号： C07C275/40 , C07C125/06
CPC分类号： C07C275/40 , Y10S514/826
摘要： There are disclosed novel 4-substituted amino-.alpha.-aminomethylbenzyl alcohol derivatives represented by the formula: ##STR1## wherein X represents a halogen atom; Y represents a hydrogen atom or a halogen atom; R.sub.1 represents a lower alkyl group, a carbamoyl group, a mono- or di-lower alkyl-substituted carbamoyl group, a phenyl-substituted carbamoyl group, a lower alkoxycarbonyl group, a lower alkoxy-substituted lower alkoxycarbonyl group, a phenyl-substituted lower alkoxycarbonyl group, or a cycloalkyloxycarbonyl group; and R.sub.2 represents a lower alkyl group, a cycloalkyl group, or the group shown by the formula ##STR2## wherein R.sub.3 represents a hydrogen atom or a lower alkyl group and R.sub.4 represents a hydrogen atom, a hydroxy group, or a lower alkoxy group and the pharmaceutically acceptable nontoxic salts thereof.These compounds are antiasthmatic agents useful for the prophylaxis and treatment of asthma.
摘要翻译：公开了由下式表示的新型4-取代氨基-α-氨基甲基苄醇衍生物：其中X表示卤素原子; Y表示氢原子或卤素原子; R 1表示低级烷基，氨基甲酰基，一或二低级烷基取代的氨基甲酰基，苯基取代的氨基甲酰基，低级烷氧基羰基，低级烷氧基取代的低级烷氧基羰基，苯基取代的低级烷氧基羰基或环烷氧基羰基; 和R 2表示低级烷基，环烷基或下式所示的基团，其中R 3表示氢原子或低级烷基，R 4表示氢原子，羟基或低级烷氧基，其药学上可接受的无毒盐。

7. 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。

8. 发明授权

US4145363A 4-Carbamoylamino-.alpha.-aminomethylbenzyl alcohol derivatives 失效
标题翻译： 4-氨基甲酰胺 - 氨基乙基苄醇衍生物
公开(公告)号：US4145363A
公开(公告)日：1979-03-20
申请号：US809998
申请日：1977-06-27
申请人： Masuo Murakami , Kozo Takahashi , Kiyoshi Murase , Toshiyasu Mase , Hisashi Ida , Toichi Takenaka
发明人： Masuo Murakami , Kozo Takahashi , Kiyoshi Murase , Toshiyasu Mase , Hisashi Ida , Toichi Takenaka
IPC分类号： C07C275/40 , C07C127/17 , A61K31/17
CPC分类号： C07C275/40 , Y10S514/826
摘要： There are disclosed novel 4-substituted amino-.alpha.-aminomethylbenzyl alcohol derivatives represented by the formula: ##STR1## wherein X represents a halogen atom; Y represents a hydrogen atom or a halogen atom; R.sub.1 represents a lower alkyl group, a carbamoyl group, a mono- or di-lower alkyl-substituted carbamoyl group, a phenyl-substituted carbamoyl group, a lower alkoxycarbonyl group, a lower alkoxy-substituted lower alkoxycarbonyl group, a phenyl-substituted lower alkoxycarbonyl group, or a cycloalkyloxycarbonyl group; and R.sub.2 represents a lower alkyl group, a cycloalkyl group, or the group shown by the ##STR2## wherein R.sub.3 represents a hydrogen atom or a lower alkyl group and R.sub.4 represents a hydrogen atom, a hydroxy group, or a lower alkoxy group and the pharmaceutically acceptable nontoxic salts thereof. These compounds are antiasthmatic agents useful for the prophylaxis and treatment of asthma.

9. 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.

10. 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.

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