Benzazepine and benzothiazepine derivatives
    3.
    发明授权
    Benzazepine and benzothiazepine derivatives 失效
    苯并氮杂和苯并硫氮杂衍生物

    公开(公告)号:US4946840A

    公开(公告)日:1990-08-07

    申请号:US334025

    申请日:1989-04-06

    摘要: Vasodilating activity is exhibited by compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein X is --CH.sub.2 -- or --S--;R.sub.1 is ##STR2## or --O--Y.sub.3 ; R.sub.2 is heterocyclo or heteroaryl;R.sub.3 and R.sub.4 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, arylalkyl, cyano, hydroxy, alkanoyloxy, ##STR3## fluoro-substituted alkoxy, fluoro-substituted alkyl, (cycloalkyl)alkoxy, --NO.sub.2, --NY.sub.10 Y.sub.11, --S(O).sub.k alkyl, --S(O).sub.k aryl ##STR4## n is 0, 1, 2 or 3; m is 0, 1, 2 or 3;k is 0, 1 or 2;Y.sub.1 and Y.sub.2 are each independently hydrogen or alkyl; or Y.sub.1 is hydrogen and Y.sub.2 is alkenyl, alkynyl, aryl, heteroaryl, or cycloalkyl; or Y.sub.1 and Y.sub.2, together with the carbon atom to which they are attached, are cycloalkyl;Y.sub.3 is hydrogen, alkyl, alkanoyl, alkenyl, arylcarbonyl, heteroarylcarbonyl, or ##STR5## Y.sub.8 and Y.sub.9 are each independently hydrogen, alkyl, aryl, or heteroaryl; or Y.sub.8 and Y.sub.9, together with the nitrogen atom to which they are attached, are pyrrolidinyl, piperidinyl or morpholinyl;Y.sub.10 and Y.sub.11 are each independently hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl, or ##STR6## Y.sub.12 is hydroxy, alkoxy, aryloxy, amino, alkylamino, or dialkylamino; andY.sub.13 is alkyl, alkoxy or aryloxy.

    Amino substituted benzenepropanols
    5.
    发明授权
    Amino substituted benzenepropanols 失效
    氨基取代苯丙酰醇

    公开(公告)号:US4788010A

    公开(公告)日:1988-11-29

    申请号:US726549

    申请日:1985-04-24

    IPC分类号: C07C91/16 C07C93/08

    摘要: Hypotensive activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is hydrogen or alkyl;R.sub.2 and R.sub.3 are each independently phenyl, substituted phenyl, cycloalkyl, or R.sub.2 is hydrogen and R.sub.3 is heteroaryl;R.sub.4 and R.sub.5 are the same or different and each is hydrogen, hydroxy, alkoxy, alkanoyl or alkyl;R.sub.6 is hydrogen or alkyl; andn is 1, 2, 3 or 4; with the proviso that if R.sub.2 and R.sub.3 are each phenyl, at least one of R.sub.1, R.sub.4, R.sub.5 and R.sub.6 is other than hydrogen.

    摘要翻译: 低分子活性由具有式“IMAGE”的化合物及其药学上可接受的盐显示,其中R 1是氢或烷基; R2和R3各自独立地是苯基,取代的苯基,环烷基,或者R2是氢,R3是杂芳基; R 4和R 5相同或不同,各自为氢,羟基,烷氧基,烷酰基或烷基; R6是氢或烷基; n为1,2,3或4; 条件是如果R 2和R 3各自为苯基,则R 1,R 4,R 5和R 6中的至少一个不是氢。

    Dihydropyrimidine macrocyclic lactones useful as calcium antagonists and
agonists
    6.
    发明授权
    Dihydropyrimidine macrocyclic lactones useful as calcium antagonists and agonists 失效
    可用作钙拮抗剂和激动剂的二氢嘧啶大环内酯

    公开(公告)号:US5143915A

    公开(公告)日:1992-09-01

    申请号:US558266

    申请日:1990-07-25

    IPC分类号: C07D497/04

    CPC分类号: C07D497/04

    摘要: A compound of the formula ##STR1## (symbols defined in the specification), its 3,4-dihydropyrimidine tautomer form and pharmaceutically acceptable salts thereof have calcium entry blocking activity. A process of preparation, pharmaceutical composition and method of using the compound to reduce blood pressure are also provided.

    摘要翻译: 式(IMAGE)化合物(说明书中定义的符号),其3,4-二氢嘧啶互变异构体形式及其药学上可接受的盐具有钙进入阻断活性。 还提供了一种制备方法,药物组合物和使用该化合物降低血压的方法。