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21. 发明授权

US4406906A Cerebral therapeutic agent and its use 失效
标题翻译：脑治疗剂及其用途
公开(公告)号：US4406906A
公开(公告)日：1983-09-27
申请号：US346319
申请日：1982-02-05
申请人： Horst Meyer , Friedrich Bossert , Stanislav Kazda , Friedrich Hoffmeister , Wulf Vater
发明人： Horst Meyer , Friedrich Bossert , Stanislav Kazda , Friedrich Hoffmeister , Wulf Vater
IPC分类号： A61K31/44 , A61K31/455 , A61K47/38 , A61P9/08 , A61P25/28 , C07D211/90
CPC分类号： C07D211/90 , A61K31/44
摘要： The invention provides pharmaceutical compositions and medicaments, useful for the treatment of cerebral disorders, wherein the active compound is 1,4-dihydro-2,6-dimethyl-4-(3'-nitrophenyl)-pyridine-3-(.beta.-methoxyethyl ester)-5-(isopropyl ester). Also included in the invention are methods for the use of said compositions and medicaments.
摘要翻译：本发明提供可用于治疗脑疾病的药物组合物和药物，其中活性化合物是1,4-二氢-2,6-二甲基-4-（3'-硝基苯基） - 吡啶-3-（β-甲氧基乙基酯）-5-（异丙酯）。本发明还包括使用所述组合物和药物的方法。

22. 发明授权

US4136187A Antihypertensive 2-amino-4,5-dihydropyridine derivatives 失效
标题翻译：抗坏血酸2-氨基-4,5-二氢吡啶衍生物
公开(公告)号：US4136187A
公开(公告)日：1979-01-23
申请号：US518283
申请日：1974-10-29
申请人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
发明人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
IPC分类号： C07D211/90 , A61K31/455
CPC分类号： C07D211/90 , Y10S514/929
摘要： 4,5-Dihydropyridines bearing an N,N-disubstituted amino group in the 2-position, carbonyl functions in the 3- and 5-positions and being optionally substituted in the 6-position by lower alkyl or phenyl and, in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group, are antihypertensive agents and coronary vessel dilators. The compounds, of which 2-pyrrolidino-6-methyl-4-(3-nitrophenyl)-4,5-dihydropyridine-3,5-dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an ylideneacetoacetic acid ester and a substituted 3,3-diaminoacrylate.

23. 发明授权

US3989708A 2-Amino-1,4-dihydropyridine derivatives 失效
标题翻译： 2-氨基-1,4-二氢吡啶衍生物
公开(公告)号：US3989708A
公开(公告)日：1976-11-02
申请号：US526510
申请日：1974-11-25
申请人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
发明人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
IPC分类号： C07D239/20 , C07D211/90 , C07D213/55 , C07D215/14
CPC分类号： C07D211/90 , Y10S514/929
摘要： 2-Amino-1,4-dihydropyridines bearing an ester carbonyl function in the 3-position, being optionally substituted by lower alkyl in the 5-position, and being substituted in the 4- and 6-positions by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2-amino-6-methyl-4-(3-chlorophenyl)-1,4-dihydropyridine-3 carboxylic acid ethyl ester is a representative embodiment, are prepared through condensation of an .alpha.-B-unsaturated ketone and an amidine.
摘要翻译： 3-位上具有酯羰基官能团的2-氨基-1,4-二氢吡啶，任选被5-位的低级烷基取代，并在4-和6-位被低级烷基，苯基，取代的苯基或杂环基是抗高血压剂和冠状血管扩张剂。其中2-氨基-6-甲基-4-（3-氯苯基）-1,4-二氢吡啶-3-羧酸乙酯的代表性实施方案是通过α-β-不饱和酮和脒

24. 发明授权

US3957998A Use of 2,6-diamino-4-substituted-1,4-dihydropyridine-3,5-dicarboxylic acid esters for effecting coronary vessel dilation and treating hypertension 失效
标题翻译：使用2,6-二氨基-4-取代-1,4-二氢吡啶-3,5-二羧酸酯来实现冠状动脉血管扩张和治疗高血压
公开(公告)号：US3957998A
公开(公告)日：1976-05-18
申请号：US455258
申请日：1974-03-27
申请人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
发明人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
IPC分类号： A61K31/455 , C07D211/90 , C07D401/04 , C07D405/04
CPC分类号： C07D401/04 , A61K31/455 , C07D211/90 , C07D405/04 , Y10S514/929
摘要： 2,6-Diamino-1,4-dihydropyridines bearing carbonyl functions in the 3- and 5-positions and being substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2,6-diamino-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an amidine with either an aldehyde or an ylidenecyanoacetoacetic acid ester.
摘要翻译：在3-和5-位上具有羰基官能团的2,6-二氨基-1,4-二氢吡啶是低级烷基，苯基，取代的苯基或杂环基在4-位上被取代的是抗高血压剂和冠状血管扩张剂。其中2,6-二氨基-4-（3-硝基苯基）-1,4-二氢吡啶-3,5-二羧酸3,5-二乙酯是一个代表性的实施方案，通过脒与醛或亚基甲酰乙酰乙酸酯。

25. 发明授权

US3951993A 2-Amino-4,5-dihydropyridine derivatives and process for their preparation 失效
公开(公告)号：US3951993A
公开(公告)日：1976-04-20
申请号：US453863
申请日：1974-03-22
申请人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
发明人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
IPC分类号： C07D211/90 , C07D405/04 , C07D213/32
CPC分类号： C07D405/04 , C07D211/90
摘要： 2-Amino-4,5-dihydropyridines-3,5-dicarboxylates substituted by lower alkoxy or lower alkylthio in the 6-position and optionally substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2-amino-4-(3-nitrophenyl)-6-ethoxy-4,5-dihydropyridine-3,5-dicarboxylic acid diethyl ester is a representative embodiment, are prepared through condensation of an aldehyde and a 3-aminoacrylate bearing an alkoxy or alkylthio group in the 3-position.

26. 发明授权

US3951991A 4-Aryl-6-amino-3,4-dihydropyrid-2-one-3,5-dicarboxylic acid ester 失效
标题翻译： 4-芳基-6-氨基-3,4-二氢吡啶-2-酮-3,5-二羧酸酯
公开(公告)号：US3951991A
公开(公告)日：1976-04-20
申请号：US531599
申请日：1974-12-11
申请人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
发明人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
IPC分类号： A61K31/455 , C07D401/04 , C07D409/04 , C07D213/71
CPC分类号： C07D401/04 , A61K31/455 , C07D409/04 , Y10S514/929
摘要： 3,4-Dihydropyridones of the formula ##SPC1##Wherein R.sup.1 is hydrogen, straight or branched chain alkyl, or --COOR' wherein R' is a straight, branched or cyclic, saturated or unsaturated hydrocarbon or said hydrocarbon interrupted by 1 or 2 oxygen atoms; R.sup.2 is a straight, branched or cyclic, saturated or unsaturated hydrocarbon, aryl unsubstituted or substituted by 1 to 3 of the same or different substitutents selected from the group consisting of alkyl, alkoxy, halogen, nitro, cyano, trifluoromethyl, carbalkoxy and SO.sub.n --alkyl wherein n is 0, 1 or 2, or naphthyl, quinolyl, isoquinolyl, pyridyl, pyrimidyl, thenyl, furyl or pyrryl unsubstituted or substituted by 1 or more substituents selected from the group consisting of alkyl, alkoxy and halogen; and R.sup.3 is a straight or branched chain hydrocarbon or said hydrocarbon interrupted by 1 or 2 oxygen atoms, are produced by reacting an .alpha.,.beta.-unsaturated carboxylic acid ester of the formula ##EQU1## wherein R is alkyl, alkenyl or alkynyl, and R.sup.1 and R.sup.2 are as above defined, with an amidine of the formula ##EQU2## wherein R.sup.3 is as above defined. These compounds are useful as coronary agents and as anti-hypertensive agents.
摘要翻译：式WHEREIN R 1是氢，直链或支链烷基或-COOR'的3,4-二氢吡啶酮，其中R'是直链，支链或环状，饱和或不饱和烃或被1或2个氧原子间断的烃; R2是直链，支链或环状的饱和或不饱和的烃，未取代或被1至3个选自烷基，烷氧基，卤素，硝基，氰基，三氟甲基，碳烷氧基和SO n- 烷基，其中n为0,1或2，或萘基，喹啉基，异喹啉基，吡啶基，嘧啶基，噻吩基，呋喃基或吡啶基，未取代或被一个或多个选自烷基，烷氧基和卤素的取代基取代; 并且R3是直链或支链烃或被1或2个氧原子间断的所述烃通过使式R 1 R 2 -CH = C ANGLE COOR的α，β-不饱和羧酸酯反应制备，其中R是烷基，烯基或炔基，并且R 1和R 2如上所定义，与式H 2 N AN CLE C-CH 2 COOR 3 HN的脒反应，其中R 3如上所定义。这些化合物可用作冠状动脉剂和抗高血压剂。

27. 发明授权

US3935223A 2-Amino-1,4-dihydropyridine derivatives 失效
公开(公告)号：US3935223A
公开(公告)日：1976-01-27
申请号：US455305
申请日：1974-03-27
申请人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
发明人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
IPC分类号： C07D401/04 , C07D405/04 , C07D409/04 , C07D213/55
CPC分类号： C07D401/04 , C07D405/04 , C07D409/04 , Y10S514/929
摘要： 2-Amino-1,4-dihydropyridines bearing a carbonyl function in the 5-position and being optionally substituted by lower alkyl or phenyl in the 6-position, and the corresponding 2-amino-1,4,5,6,7,8-hexahydro-5-oxoquinolines, which derivatives are further substituted by a carbonyl group in the 3-position and optionally substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are anti-hypertensive agents and coronary vessel dilators. The compounds, of which 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an ylideneacetoacetic acid ester and an amidine.

28. 发明授权

US4004015A Bicyclic derivatives of 1,4-dihydropyridine as antihypertensive agents and coronary vessel dilators 失效
标题翻译： 1,4-二氢吡啶的双环衍生物作为抗高血压药和冠状血管扩张剂
公开(公告)号：US4004015A
公开(公告)日：1977-01-18
申请号：US604604
申请日：1975-08-14
申请人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
发明人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
IPC分类号： A61K31/395 , A61K31/44 , C07D455/02 , C07D471/04 , A61K31/455
CPC分类号： C07D471/04 , A61K31/395 , A61K31/44 , C07D455/02
摘要： 1,4-Dihydropyridines bearing carbonyl functions in the 3- and 5-positions, being optionally substituted by lower alkyl in the 6-position, being substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group, and being fused through the 1- and 2-positions to a five, six or seven membered cycloalkyl ring, one methylene group of which can be replaced by sulfur, oxygen imino or alkylimino, are antihypertensive agents and coronary vessel dilators. The compounds, of which 6-methyl-4-(3-nitrophenyl)-1,2-pentamethylene-1,4-dihydropyridine-3,5-dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an ylideneacetoacetic acid ester and a cyclic enamino carbonyl derivative.
摘要翻译：在3-位和5-位具有羰基官能团的1,4-二氢吡啶，任选被6位的低级烷基取代，在4-位被低级烷基，苯基，取代的苯基或杂环基取代，和通过1-和2-位融合成五，六或七元环烷基环，其中一个亚甲基可以被硫，氧亚氨基或烷基亚氨基取代，是抗高血压剂和冠状血管扩张剂。其中6-甲基-4-（3-硝基苯基）-1,2-戊烯-1,4-二氢吡啶-3,5-二羧酸3,5-二乙酯的代表性实施例是通过缩合的亚乙酰乙酸酯和环状氨基羰基衍生物。

29. 发明授权

US4001252A 2-Amino-3,4-dihydropyridines 失效
标题翻译： 2-氨基-3,4-二氢吡啶
公开(公告)号：US4001252A
公开(公告)日：1977-01-04
申请号：US445166
申请日：1974-02-25
申请人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
发明人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
IPC分类号： C07D211/90
CPC分类号： C07D211/90 , Y10S514/929
摘要： 2-Amino-3,4-dihydropyridine-3-carboxylic acid ester derivatives are produced by reacting 2-amino-1,4-dihydropyridine-3-carboxylic acid ester derivatives with an alkylating agent in the presence of an inert organic solvent at a temperature of from 20.degree. to 200.degree. C. and exhibit antihypertensive and coronary dilating properties.

30. 发明授权

US3992545A 2-Amino-4,5-dihydropyridine derivatives in pharmaceutical compositions 失效
标题翻译：药物组合物中的2-氨基-4,5-二氢吡啶衍生物
公开(公告)号：US3992545A
公开(公告)日：1976-11-16
申请号：US531919
申请日：1974-12-12
申请人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
发明人： Horst Meyer , Friedrich Bossert , Wulf Vater , Kurt Stoepel
IPC分类号： C07D405/04 , A61K31/455
CPC分类号： C07D405/04
摘要： 2-Amino-4,5-dihydropyridines-3,5-dicarboxylates substituted by lower alkoxy or lower alkylthio in the 6-position and optionally substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2-amino-4-(3-nitrophenyl)-6-ethoxy-4,5-dihydropyridine-3,5-dicarboxylic acid diethyl ester is a representative embodiment, are prepared through condensation of an aldehyde and a 3-aminoacrylate bearing an alkoxy or alkylthio group in the 3-position.
摘要翻译： 6-位被低级烷氧基或低级烷硫基取代的2-氨基-4,5-二氢吡啶-3,5-二羧酸酯，低级烷基，苯基，取代苯基或杂环基任选被4-位取代为抗高血压剂和冠状血管扩张器。 2-氨基-4-（3-硝基苯基）-6-乙氧基-4,5-二氢吡啶-3,5-二羧酸二乙酯的化合物是代表性的实施方案，通过醛和3 - 氨基丙烯酸酯在3-位上带有烷氧基或烷硫基。

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