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1. 发明授权

US4021434A Sodium .beta.-[2,6-dimethyl-3,5-bis(ethoxycarbonyl)-4-(3-nitrophenyl)-1,4-dihyd ropyridine-1-yl]ethyl sulfate 失效
标题翻译： {62- {8,2,6-二甲基-3,5-双（乙氧基羰基）-4-（3-硝基苯基）-1,4-二氢吡啶-1-基{乙酸乙酯
公开(公告)号：US4021434A
公开(公告)日：1977-05-03
申请号：US606728
申请日：1975-08-21
申请人： Masuo Murakami , Kozo Takahashi , Teruaki Ozasa , Kazuharu Tamazawa , Ryutaro Kawai , Toichi Takenaka , Norio Sato
发明人： Masuo Murakami , Kozo Takahashi , Teruaki Ozasa , Kazuharu Tamazawa , Ryutaro Kawai , Toichi Takenaka , Norio Sato
IPC分类号： C07D211/82 , C07D211/90 , C07D219/06 , C07D401/04 , C07D405/04 , C07D213/55
CPC分类号： C07D401/04 , C07D211/82 , C07D211/90 , C07D219/06 , C07D405/04 , Y10S514/929
摘要： Novel 1-substituted-1, 4-dihydropyridine derivatives, particularly diethyl 1-ethoxymethyl-4-(3-nitrophenyl)-2, 6-dimethyl-1, 4-dihydropyridine-3,5-dicarboxylate are provided. The novel derivatives have cerebral vascular dilator activity with low toxicity.
摘要翻译：提供新的1-取代-1,4-二氢吡啶衍生物，特别是1-乙氧基甲基-4-（3-硝基苯基）-2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸二乙酯。该新型衍生物具有低毒性的脑血管扩张剂活性。

2. 发明授权

US3985758A 1,4-Dihydropyridine derivatives 失效
标题翻译： 1,4-二氢吡啶衍生物
公开(公告)号：US3985758A
公开(公告)日：1976-10-12
申请号：US584268
申请日：1975-06-06
申请人： Masuo Murakami , Kozo Takahashi , Masaru Iwanami , Masaharu Fujimoto , Tadao Shibanuma , Ryutaro Kawai , Toichi Takenaka
发明人： Masuo Murakami , Kozo Takahashi , Masaru Iwanami , Masaharu Fujimoto , Tadao Shibanuma , Ryutaro Kawai , Toichi Takenaka
IPC分类号： C07D211/90 , C07D213/55
CPC分类号： C07D211/90 , Y10S514/929
摘要： There are provided novel 1,4-dihydropyridine derivatives, particularly 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-.beta.-(N-benzyl-N-methylamino)ethyl ester and 5-methyl ester. The 1,4-dihydropyridine derivatives are characterized by cerebral vascular dilator activity.
摘要翻译：提供新的1,4-二氢吡啶衍生物，特别是2,6-二甲基-4-（3'-硝基苯基）-1,4-二氢吡啶-3,5-二羧酸3-β-（N-苄基-N- 甲基氨基）乙酯和5-甲酯。 1,4-二氢吡啶衍生物的特征在于脑血管扩张剂活性。

3. 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。

4. 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.

5. 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。

6. 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.

7. 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。

8. 发明授权

US4045482A 4-(3-Isopropylamino-2-hydroxypropoxy indene 失效
标题翻译： 4-（3-异丙基氨基-2-羟基丙氧基茚
公开(公告)号：US4045482A
公开(公告)日：1977-08-30
申请号：US568097
申请日：1975-04-14
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。

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

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。

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