公开(公告)号：US3988458A

公开(公告)日：1976-10-26

申请号：US532458

申请日：1974-12-13

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： A61K31/395 ,  A61K31/44 ,  C07D455/02 ,  C07D471/04 ,  A61K31/505

CPC分类号： C07D471/04 ,  A61K31/395 ,  A61K31/44 ,  C07D455/02

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。

公开(公告)号：US3987176A

公开(公告)日：1976-10-19

申请号：US531906

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： A61K31/455 ,  C07D401/04 ,  C07D409/04

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' 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 substituents 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.

公开(公告)号：US3966767A

公开(公告)日：1976-06-29

申请号：US526800

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： A61K31/35 ,  C07D309/22 ,  C07D409/04 ,  C07D333/24

CPC分类号： C07D309/22 ,  A61K31/35 ,  C07D409/04 ,  Y10S514/929

摘要： 2-Amino-4 H-pyrane derivatives of the formula ##SPC1##WhereinR.sup.1 and R.sup.2 are the same or different and each is hydrogen or straight- or branched-chain alkyl;R.sup.3 is straight- or branched-chain alkyl, phenyl or --COOR' wherein R' is a straight, branched or cyclic saturated or unsaturated aliphatic hydrocarbon;R.sup.4 is straight, branched or cyclic alkyl or alkenyl, aryl unsubstituted or substituted by 1, 2 or 3 of the same or different substituents 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, orR.sup.4 is naphthyl, quinolyl, pyridyl, thienyl or furyl unsubstituted or substituted by alkyl, alkoxy or halogen;R.sup.5 is straight, branched or cyclic alkyl or --OR" wherein R" is a straight, branched or cyclic hydrocarbon or said hydrocarbon interrupted by 1 or 2 oxygen atoms; andR.sup.6 is hydrogen or alkyl;Are useful for their strong coronary action and as anti-hypertensive agents.

摘要翻译： 式WHEREIN R1和R2的2-氨基-4H-吡喃衍生物相同或不同，各自为氢或直链或支链烷基; R3是直链或支链烷基，苯基或-COOR'，其中R'是直链，支链或环状的饱和或不饱和脂族烃; R4是直链，支链或环状的烷基或链烯基，未被取代或被1,2或3个相同或不同的选自烷基，烷氧基，卤素，硝基，氰基，三氟甲基，烷氧羰基和-SOn 烷基，其中n为0,1或2，或R4为萘基，喹啉基，吡啶基，噻吩基或呋喃基，未取代或被烷基，烷氧基或卤素取代; R5是直链，支链或环状烷基或-OR“，其中R”是直链，支链或环状烃或被1或2个氧原子间断的所述烃; R6为氢或烷基; 有用于其强大的冠状动脉和抗高血压药物。

公开(公告)号：US3959474A

公开(公告)日：1976-05-25

申请号：US523357

申请日：1974-11-13

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： 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。

公开(公告)号：US3951992A

公开(公告)日：1976-04-20

申请号：US531525

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 ,  C07D213/70

CPC分类号： C07D401/04 ,  A61K31/455 ,  C07D409/04

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 substituents 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个相同或不同的选自烷基，烷氧基，卤素，硝基，氰基，三氟甲基，碳烷氧基和SO- 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。

公开(公告)号：US3951990A

公开(公告)日：1976-04-20

申请号：US531999

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： A61K31/455 ,  C07D401/04 ,  C07D409/04 ,  C07D213/70

CPC分类号： C07D401/04 ,  A61K31/455 ,  C07D409/04 ,  Y10S514/929 ,  Y10S514/96

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 substituents 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个相同或不同的选自烷基，烷氧基，卤素，硝基，氰基，三氟甲基，碳烷氧基和SO- 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。

公开(公告)号：US3951988A

公开(公告)日：1976-04-20

申请号：US468664

申请日：1974-05-10

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 ,  C07D213/55

CPC分类号： C07D471/04 ,  A61K31/395 ,  A61K31/44 ,  C07D455/02 ,  Y10S514/929

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：US3935220A

公开(公告)日：1976-01-27

申请号：US468741

申请日：1974-05-10

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 ,  C07D213/46

CPC分类号： C07D471/04 ,  A61K31/395 ,  A61K31/44 ,  C07D455/02 ,  Y10S514/929

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：US4675329A

公开(公告)日：1987-06-23

申请号：US750561

申请日：1985-06-27

申请人： Egbert Wehinger ,  Andreas Knorr ,  Kurt Stoepel ,  Arend Heise

发明人： Egbert Wehinger ,  Andreas Knorr ,  Kurt Stoepel ,  Arend Heise

IPC分类号： A61K31/455 ,  A61P9/08 ,  C07D211/90

CPC分类号： C07D211/90

摘要： ##STR1## is a vaso-dilator effective in combating hypertension and circulatory disorders.

摘要翻译： 是一种有效抗击高血压和循环系统疾病的血管扩张剂。

公开(公告)号：US3985886A

公开(公告)日：1976-10-12

申请号：US453930

申请日：1974-03-22

申请人： Horst Meyer ,  Freidrich Bossert ,  Wulf Vater ,  Kurt Stoepel

发明人： Horst Meyer ,  Freidrich Bossert ,  Wulf Vater ,  Kurt Stoepel

IPC分类号： C07D211/90 ,  C07D401/04 ,  C07D405/04 ,  A61K31/455

CPC分类号： C07D401/04 ,  C07D211/90 ,  C07D405/04 ,  Y10S514/929

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。