Cardioselective aryloxy- and arylthio- hydroxypropylene-piperazinyl
acetanilides which affect calcium entry
    8.
    发明授权
    Cardioselective aryloxy- and arylthio- hydroxypropylene-piperazinyl acetanilides which affect calcium entry 失效
    影响钙进入的心脏选择性芳氧基和芳硫基 - 羟丙基 - 哌嗪基乙酰苯胺

    公开(公告)号:US4567264A

    公开(公告)日:1986-01-28

    申请号:US495904

    申请日:1983-05-18

    摘要: Novel compounds of the general formula ##STR1## and the pharmaceutically acceptable esters and acid addition salts thereof, wherein:R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently hydrogen, lower alkyl, lower alkoxy, cyano, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, N-optionally substituted alkylamido, except that when R.sup.1 is methyl, R.sup.4 is not methyl; orR.sup.2 and R.sup.3 together form --OCH.sub.2 O--;R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are each independently hydrogen, lower acyl, aminocarbonylmethyl, cyano, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, di-lower alkyl amino; orR.sup.6 and R.sup.7 together form --CH.dbd.CH--CH.dbd.CH--;R.sup.7 and R.sup.8 together form --OCH.sub.2 O--;R.sup.11 and R.sup.12 are each independently hydrogen or lower alkyl; andW is oxygen or sulfur.These cardioselective compounds have calcium entry blockade properties and therefore are useful in therapy in the treatment of cardiovascular diseases, including arrhythmias, variant and exercise induced angina and myocardial infarction.

    摘要翻译: 新颖的通式(I)化合物及其药学上可接受的酯和酸加成盐,其中:R 1,R 2,R 3,R 4和R 5各自独立地为氢,低级烷基,低级烷氧基,氰基,三氟甲基,卤素 ,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,N-任选取代的烷基酰胺基,除了当R 1为甲基时,R 4不是甲基; 或R 2和R 3一起形成-OCH 2 O-; R6,R7,R8,R9和R10各自独立地为氢,低级酰基,氨基羰基甲基,氰基,低级烷基,低级烷氧基,三氟甲基,卤素,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,二低级烷基氨基; 或R6和R7一起形成-CH = CH-CH = CH-; R7和R8一起形成-OCH 2 O-; R 11和R 12各自独立地为氢或低级烷基; W是氧或硫。 这些心脏选择性化合物具有钙进入阻断性质,因此可用于治疗心血管疾病,包括心律失常,变异和运动诱发的心绞痛和心肌梗塞。

    2-(1,4-Benzodioxan-2-ylalkyl)imidazoles
    10.
    发明授权
    2-(1,4-Benzodioxan-2-ylalkyl)imidazoles 失效
    2-(1,4-苯并二恶烷-2-基烷基)咪唑

    公开(公告)号:US4315021A

    公开(公告)日:1982-02-09

    申请号:US212288

    申请日:1980-12-03

    CPC分类号: C07D319/20

    摘要: 2-(1,4-Benzodioxan-2-ylalkyl)imidazoles having the general formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, alkyl, optionally substituted phenyl, and optionally substituted phenyl lower alkyl;R.sup.3 is hydrogen, alkyl, or optionally substituted phenyl lower alkyl;n is an integer equal to 0, 1 or 2;with the proviso that R.sup.1, R.sup.2 and R.sup.3 cannot all be hydrogen and/or alkyl; and the pharmaceutically acceptable acid addition salts thereof, are useful as antidepressants.

    摘要翻译: 具有通式(I)的2-(1,4-苯并二恶烷-2-基烷基)咪唑,其中R 1和R 2各自独立地选自氢,烷基,任选取代的苯基和任选取代的苯基低级 烷基; R3是氢,烷基或任选取代的苯基低级烷基; n是等于0,1或2的整数; 条件是R1,R2和R3不能全部为氢和/或烷基; 及其药学上可接受的酸加成盐可用作抗抑郁药。