Bicyclic derivatives of 1,4-dihydropyridine as antihypertensive agents
and coronary vessel dilators
    4.
    发明授权
    Bicyclic derivatives of 1,4-dihydropyridine as antihypertensive agents and coronary vessel dilators 失效
    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

    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。

    2-Amino-4,5-dihydropyridine derivatives in pharmaceutical compositions
    6.
    发明授权
    2-Amino-4,5-dihydropyridine derivatives in pharmaceutical compositions 失效
    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

    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。

    Unsymmetrical esters of N-substituted 1,4-dihydropyridine
3,5-dicarboxylic acid
    7.
    发明授权
    Unsymmetrical esters of N-substituted 1,4-dihydropyridine 3,5-dicarboxylic acid 失效
    N-取代的1,4-二氢吡啶3,5-二羧酸的不对称酯

    公开(公告)号:US3933834A

    公开(公告)日:1976-01-20

    申请号:US496972

    申请日:1974-08-13

    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。

    Compositions and methods employing tetrahydroindolizine derivatives
    9.
    发明授权
    Compositions and methods employing tetrahydroindolizine derivatives 失效
    使用四氢吲哚啉衍生物的组合物和方法

    公开(公告)号:US4024261A

    公开(公告)日:1977-05-17

    申请号:US604257

    申请日:1975-08-13

    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 anti-hypertensive 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-位和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。

    2-Amino-6-dialkylaminodihydropyridines, their production, pharmaceutical
compositions and methods of use thereof
    10.
    发明授权
    2-Amino-6-dialkylaminodihydropyridines, their production, pharmaceutical compositions and methods of use thereof 失效
    2-氨基-6-二烷基氨基二氢吡啶,它们的制备,药物组合物及其使用方法

    公开(公告)号:US4004014A

    公开(公告)日:1977-01-18

    申请号:US545202

    申请日:1975-01-29

    CPC分类号: C07D211/90

    摘要: 2-Amino-6-dialkylaminodihydropyridines exist in tautomeric form and are represented by the formulae ##STR1## WHEREIN R.sub.1 and R.sub.3 are the same or different and each is straight, branched or cyclic alkyl, alkenyl or alkynyl or said alkyl, alkenyl or alkynyl interrupted by 1 or 2 oxygen atoms;R.sub.2 is a saturated, partially unsaturated or unsaturated straight, branched or cyclic hydrocarbon; aryl unsubstituted or substituted by 1, 2 or 3 of the same or different substituents selected from the group consisting of alkyl, alkoxy, azido, halo, cyano, nitro, trifluoromethyl, carbalkoxy and SO.sub.n -alkyl wherein n is 0, 1 or 2; naphthyl; quinolyl; isoquinolyl; pyridyl; pyrimidyl; thenyl; or furyl; andR.sub.4 and R.sub.5 are each lower alkyl; benzyl; or, together with the nitrogen atom to which they are attached, a 4- to 7-membered ring. These compounds are useful for their coronary-vessel-dilating effect, their antihypertensive effect, their anti-fibrillation effect, their vascular-spasmolytic effect and their muscular-spasmolytic effect.

    摘要翻译: 2-氨基-6-二烷基氨基二氢吡啶以互变异构形式存在并由下式表示:其中R 1和R 3相同或不同,并且各自为直链,支链或环状烷基,烯基或炔基或所述 被1或2个氧原子间隔的烷基,烯基或炔基; R2是饱和的,部分不饱和的或不饱和的直链,支链或环状烃; 未取代的或被1,2或3个相同或不同的选自烷基,烷氧基,叠氮基,卤素,氰基,硝基,三氟甲基,烷氧基和其中n为0,1或2的烷基的取代基取代的芳基; 萘基; 喹啉基 异喹啉基 吡啶基 嘧啶基 茶碱 或呋喃基; 且R 4和R 5各自为低级烷基; 苄基; 或者与它们所连接的氮原子一起形成4-至7-元环。 这些化合物可用于其冠状血管扩张作用,其抗高血压作用,其抗纤维化作用,其血管解痉作用及其肌肉 - 解痉作用。