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31 条记录 (耗时 0.011 秒)

    4-Aryl-6-amino-3,4-dihydropyrid-2-one-3,5-dicarboxylic acid ester
    1.
    发明授权
    4-Aryl-6-amino-3,4-dihydropyrid-2-one-3,5-dicarboxylic acid ester 失效
    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：US3925395A

    公开(公告)日：1975-12-09

    申请号：US39019373

    申请日：1973-08-21

    申请人： BAYER AG

    发明人： MEYER HORST ,  BOSSERT FRIEDRICH ,  VATER WULF ,  STOEPEL KURT

    IPC分类号： C07D215/14 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/455 ,  A61P1/00 ,  A61P3/06 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  C07D211/90 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D213/55

    CPC分类号： C07D401/04 ,  A61K31/455 ,  C07D211/90 ,  C07D409/04 ,  Y10S514/929

    摘要： 3,4-Dihydropyridones of the formula

    wherein R3 is as above defined. These compounds are useful as coronary agents and as anti-hypertensive agents.

    wherein R is alkyl, alkenyl or alkynyl, and R1 and R2 are as above defined, with an amidine of the formula

    WHEREIN R1 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; R2 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 SOn-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 R3 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

    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。

    Cyanophenyl-1,4-dihydropyridine derivatives
    3.
    发明授权
    Cyanophenyl-1,4-dihydropyridine derivatives 失效
    氰基-1,4-二氢吡啶衍生物

    公开(公告)号：US3691177A

    公开(公告)日：1972-09-12

    申请号：US3691177D

    申请日：1970-12-11

    申请人： BAYER AG

    发明人： BOSSERT FRIEDRICH ,  VATER WULF

    IPC分类号： C07D211/90 ,  C07D31/46

    CPC分类号： C07D211/90

    摘要： Cyanophenyl-1,4-dihydropyridine derivatives of the formula:

    WHEREIN R is hydrogen, saturated or unsaturated, straight, branched or cyclic alkyl of one to six carbon atoms, unsubstituted or substituted by hydroxyl or alkoxy of one to three carbon atoms, or benzyl or phenethyl unsubstituted or substituted in the aryl moiety by 1, 2 or 3 members selected from the group consisting of 1 to 3 alkoxy moieties of one to three carbon atoms, 1 or 2 alkyl moieties of one to three carbon atoms and 1 or 2 halogen atoms, R'' is straight or branched chain alkyl of one to four carbon atoms, R'''' is straight, branched, cyclic, saturated or unsaturated alkyl of one to six carbon atoms, said alkyl interrupted by 1 or 2 oxygen atoms or said alkyl substituted by hydroxyl, and R'''''' is aryl substituted by cyano or by cyano and 1 to 9 members selected from the group consisting of cyano, nitro, amino, acylamino of one to two carbon atoms, hydroxyl, acyloxy of one to two carbon atoms, 1 or 2 alkyl moieties of one to four carbon atoms, 1 or 2 alkoxy moieties of one to four carbon atoms, and 1 or 2 halogen atoms, ARE USEFUL FOR THEIR CORONARY DILATING EFFECT AND ANTIHYPERTENSIVE EFFECTS. Processes for the production of these compounds are set forth below.

    摘要翻译： 下式的氰基苯基-1,4-二氢吡啶衍生物：

    Pharmaceutical compositions utilizing 2-amino-1,4-dihydropyridine derivatives and method of effecting coronary vessel dilation and treating hypertension in humans and animals utilizing said compounds
    5.
    发明授权
    Pharmaceutical compositions utilizing 2-amino-1,4-dihydropyridine derivatives and method of effecting coronary vessel dilation and treating hypertension in humans and animals utilizing said compounds 失效
    利用2-氨基-1,4-二氢吡啶衍生物的药物组合物和使用所述化合物进行冠状动脉血管扩张和治疗人和动物高血压的方法

    公开(公告)号：US3911123A

    公开(公告)日：1975-10-07

    申请号：US43930574

    申请日：1974-02-04

    申请人： BAYER AG

    发明人： MEYER HORST ,  BOSSERT FRIEDRICH ,  VATER WULF ,  STOEPEL KURT

    IPC分类号： C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  A61K31/655 ,  A61K31/435

    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-amino1,4,5,6,7,8-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 heterocylic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an ylideneacetoacetic acid ester and an amidine.

    摘要翻译： 在5-位上具有羰基官能团的2-氨基-1,4-二氢吡啶并且任选被6位的低级烷基或苯基取代，并且相应的2-氨基-1,4,5,6,7， 8-六氢-5-氧代喹啉，其衍生物进一步被3-位上的羰基取代，并且任选被4-位被低级烷基，苯基，取代的苯基或杂环基取代的是抗高血压剂和冠状血管扩张剂。 其中2-氨基-6-甲基-4-（3-硝基苯基）-1,4-二氢吡啶-3,5-二羧酸3,5-二乙酯是其代表性实施方案的化合物是通过将 亚基乙酰乙酸酯和脒。

    Benzoquinolizine derivatives and process for their preparation and use
    6.
    发明授权
    Benzoquinolizine derivatives and process for their preparation and use 失效
    苯醌喹啉衍生物及其制备及使用方法

    公开(公告)号：US3907807A

    公开(公告)日：1975-09-23

    申请号：US33647673

    申请日：1973-02-28

    申请人： BAYER AG

    发明人： MEYER HORST ,  BOSSERT FRIEDRICH ,  VATER WULF ,  STOEPEL KURT

    IPC分类号： C07D221/06 ,  C07D455/04 ,  C07D215/20

    CPC分类号： C07D455/04 ,  Y10S514/929

    摘要： 6,7,7a,8,9,10-Hexahydro-1H,5H-benzo(i,j)quinolizines bearing a lower alkyl, phenyl, substituted phenyl or a heterocyclic group in the 1-position and a carbonyl function in the 2-position, and being optionally substituted by lower alkyl in the 3-position and by carbalkoxy in the 7a-position, are antihypertensive agents and coronary vessel dilators. The compounds of which 1-(3nitrophenyl)-3-methyl-10-oxo-6,7,7a,8,9,10-hexahydro-1H,5Hbenzo(i,j)quinolizine-2-carboxylic acid ethyl ester is a representative embodiment, are prepared through condensation of an ylideneacetoacetic acid ester and a 7-oxo-1,2,3,4,4a,5,6,7octahydroquinoline.

    摘要翻译： 在1位上具有低级烷基，苯基，取代的苯基或杂环基的6,7,7a，8,9,10-六氢-1H，5H-苯并[i，j]喹嗪在2位上具有羰基官能团 并且任选被3-位的低级烷基和7a位的烷氧基取代为抗高血压剂和冠状血管扩张剂。 其中1-（3-硝基苯基）-3-甲基-10-氧代-6,7,7a，8,9,10-六氢-1H，5H-苯并[i，j]喹嗪-2-羧酸 乙酯是代表性的实施方案，其通过亚基乙酰乙酸酯和7-氧代-1,2,3,4,4a，5,6,7-八氢喹啉的缩合制备。

    2-Amino-4 H-pyrane
    7.
    发明授权
    2-Amino-4 H-pyrane 失效
    2-氨基-4H-吡喃

    公开(公告)号：US3897462A

    公开(公告)日：1975-07-29

    申请号：US37580973

    申请日：1973-07-02

    申请人： BAYER AG

    发明人： MEYER HORST ,  BOSSERT FRIEDRICH ,  VATER WULF ,  STOEPEL KURT

    IPC分类号： A61K31/35 ,  A61K31/351 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D309/22 ,  C07D309/32 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D7/14

    CPC分类号： C07D309/22 ,  A61K31/35 ,  C07D309/32 ,  C07D409/04

    摘要： 2-Amino-4 H-pyrane derivatives of the formula

    WHEREIN R1 and R2 are the same or different and each is hydrogen or straight- or branched-chain alkyl; R3 is straight- or branched-chain alkyl, phenyl or -COOR'' wherein R'' is a straight, branched or cyclic saturated or unsaturated aliphatic hydrocarbon; R4 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 -SOn alkyl wherein n is 0, 1 or 2, or R4 is naphthyl, quinolyl, pyridyl, thenyl or furyl unsubstituted or substituted by alkyl, alkoxy or halogen; R5 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; and R6 is hydrogen or alkyl; ARE USEFUL FOR THEIR STRONG CORONARY ACTION AND AS ANTIHYPERTENSIVE 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R 4为萘基，喹啉基，吡啶基，噻吩基或未被取代或被烷基，烷氧基或卤素取代的呋喃基; 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精神病药。

    2-Amino-4,5-dihydropyridine derivatives
    9.
    发明授权
    2-Amino-4,5-dihydropyridine derivatives 失效
    2-氨基-4,5-二氢吡啶衍生物

    公开(公告)号：US3917619A

    公开(公告)日：1975-11-04

    申请号：US45325374

    申请日：1974-03-21

    申请人： BAYER AG

    发明人： MEYER HORST ,  BOSSERT FRIEDRICH ,  VATER WULF ,  STOEPEL KURT

    IPC分类号： C07D405/04 ,  C07D213/55

    CPC分类号： 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-(3nitrophenyl)-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。

    3,5,6-Tricarboxy- and 2,3,5,6-tetracarboxy-1,4-dihydropyridine derivatives
    10.
    发明授权
    3,5,6-Tricarboxy- and 2,3,5,6-tetracarboxy-1,4-dihydropyridine derivatives 失效
    3,5,6-三羧基和2,3,5,6-四羧基-1,4-二氢吡啶衍生物

    公开(公告)号：US3905983A

    公开(公告)日：1975-09-16

    申请号：US39985073

    申请日：1973-09-24

    申请人： BAYER AG

    发明人： BOSSERT FRIEDRICH ,  MEYER HORST ,  VATER WULF

    IPC分类号： A61K31/4427 ,  A61K31/455 ,  A61P3/06 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D211/90 ,  C07D401/04 ,  C07D213/80

    CPC分类号： C07D401/04 ,  C07D211/90

    摘要： 1,4-Dihydropyridines bearing carboxy functions in the 3-, 5- and 6- or 2-, 3-, 5- and 6-positions and being substituted in the 4position by phenyl, substituted phenyl, naphthyl, phenylalkyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2-methyl-4-(3nitrophenyl)-1,4-dihydropyridine-3,5,6-tricarboxylic acid triethylester is a representative embodiment, are prepared through condensation of an enamine with an ylidene acid ester, the latter being separately prepared or prepared in situ.

    摘要翻译： 在3-，5-和6-或2-，3-，5-和6-位具有羧基官能团的1,4-二氢吡啶并且在4-位被苯基，取代的苯基，萘基，苯基烷基或 杂环基是抗高血压药和冠状血管扩张剂。 其中2-甲基-4-（3-硝基苯基）-1,4-二氢吡啶-3,5,6-三羧酸三乙酯是其代表性实施方案的化合物，其通过将烯胺与亚乙酸酯缩合制备， 后者分别制备或原位制备。