公开(公告)号：US4849433A

公开(公告)日：1989-07-18

申请号：US12515

申请日：1987-02-09

申请人： Egbert Wehinger ,  Horst Meyer ,  Friedrich Bossert ,  Wulf Vater ,  Robertson Towart ,  Kurt Stoepel ,  Stanislav Kazda

发明人： Egbert Wehinger ,  Horst Meyer ,  Friedrich Bossert ,  Wulf Vater ,  Robertson Towart ,  Kurt Stoepel ,  Stanislav Kazda

IPC分类号： A61K31/4422 ,  A61K31/455 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D211/90

CPC分类号： C07D211/90

摘要： The invention relates to optically active 1,4-dihydropyridine compounds of Formulas Ia and Ib as defined hereinabove which are effective for influencing circulation. Also included in the invention are compositions containing said optically active compounds and methods for the use of said compounds and compositions.

摘要翻译： 本发明涉及有效影响循环的如上所定义的式Ia和Ib的光学活性的1,4-二氢吡啶化合物。 本发明还包括含有所述光学活性化合物的组合物和使用所述化合物和组合物的方法。

公开(公告)号：US4510310A

公开(公告)日：1985-04-09

申请号：US429732

申请日：1982-09-30

申请人： Egbert Wehinger ,  Horst Meyer ,  Friedrich Bossert ,  Wulf Vater ,  Robertson Towart ,  Kurt Stoepel ,  Stanislay Kazda

发明人： Egbert Wehinger ,  Horst Meyer ,  Friedrich Bossert ,  Wulf Vater ,  Robertson Towart ,  Kurt Stoepel ,  Stanislay Kazda

IPC分类号： A61K31/4422 ,  A61K31/455 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D211/90 ,  C07D213/55 ,  A61K31/44

CPC分类号： C07D211/90

摘要： The invention relates to optically active 1,4-dihydropyridine compounds of Formulas Ia and Ib as defined hereinabove which are effective for influencing circulation. Also included in the invention are compositions containing said optically active compounds and methods for the use of said compounds and compositions.

摘要翻译： 本发明涉及有效影响循环的如上所定义的式Ia和Ib的光学活性的1,4-二氢吡啶化合物。 本发明还包括含有所述光学活性化合物的组合物和使用所述化合物和组合物的方法。

公开(公告)号：US4146627A

公开(公告)日：1979-03-27

申请号：US828136

申请日：1977-08-26

申请人： Egbert Wehinger ,  Friedrich Bossert ,  Horst Meyer ,  Wulf Vater ,  Arend Heise ,  Stanislav Kaada ,  Kurt Stoepel

发明人： Egbert Wehinger ,  Friedrich Bossert ,  Horst Meyer ,  Wulf Vater ,  Arend Heise ,  Stanislav Kaada ,  Kurt Stoepel

IPC分类号： A61K31/4427 ,  A61K31/455 ,  A61K31/55 ,  A61P1/00 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  C07D211/90 ,  C07D401/12 ,  C07D213/55

CPC分类号： C07D401/12 ,  C07D211/90

摘要： The circulation provides new aminoalkylidene-amino-1,4-dihydropyridines which influence the circulatory system and are useful, for instance, as antihypertensive agents. Also included in the invention are methods for the preparation of said dihydropyridines, compositions containing them and methods for their use.

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。

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.

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。

公开(公告)号：US3933834A

公开(公告)日：1976-01-20

申请号：US496972

申请日：1974-08-13

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 ,  C07D213/55

CPC分类号： C07D405/04 ,  Y10S514/929

摘要： Unsymmetrical esters of N-substituted 4-substituted-1,4-dihydropyridine 3,5-dicarboxylic acid substituted in the 4-position by pyridyl, thienyl, furyl and pyrryl and optionally substituted in the 2- and 6-positions by lower alkyl. The products can be prepared (A) through condensation of an ylidene-.beta.-ketocarboxylic acid ester, with a .beta.-ketocarboxylic acid ester and an amine or salt thereof, or with an enamino carboxylic acid ester or (B) through condensation of an aldehyde, an enamino carboxylic acid ester and a .beta.-ketocarboxylic acid ester. The said products have utility as cardiovascular agents.

摘要翻译： 在4-位被吡啶基，噻吩基，呋喃基和吡咯基取代的N-取代的4-取代-1,4-二氢吡啶3,5-二羧酸的非对称酯，并且在2-和6-位被低级烷基取代。 可以通过将亚基-β-酮羧酸酯与β-酮羧酸酯与其胺或其盐或与氨基羧酸酯缩合制备（A），或（B）通过缩醛 ，烯氨基羧酸酯和β-酮羧酸酯。 所述产品具有作为心血管药物的作用。

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.

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

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。