1-(Alkanoylamino-aryloxy)-2-hydroxy-3-(alkinyl-amino)-propanes and salts
thereof
    2.
    发明授权
    1-(Alkanoylamino-aryloxy)-2-hydroxy-3-(alkinyl-amino)-propanes and salts thereof 失效
    1-(烷酰基氨基 - 芳氧基)-2-羟基-3-(炔基 - 氨基) - 丙烷及其盐

    公开(公告)号:US4609672A

    公开(公告)日:1986-09-02

    申请号:US623960

    申请日:1984-06-25

    CPC分类号: C07C255/00 A61K31/505

    摘要: The invention relates to a compound of the formula ##STR1## wherein R.sub.1 is a linear or branched alkyl of 4 to 20 carbon atoms;R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or a bivalent radical --CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.n --, where n is an integer from 3 to 5, inclusive, and the free bonds of said bivalent radical are attached to adjacent carbon atoms of the phenyl ring; andR.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.4 is alkyl of 1 to 3 carbon atoms; orR.sub.3 and R.sub.4, together with each other, are --(CH.sub.2).sub.p --, where p is an integer from 4 to 6, inclusive,or a non-toxic, pharmacologically acceptable acid addition salt thereof. The compounds of formula I are useful for treatment and prophylaxis of diseases of the coronaries, for the treatment of hypertension, and for treatment of cardiac arrhythmia, particularly tachycardia.

    摘要翻译: 本发明涉及式IMA的化合物,其中R 1是4至20个碳原子的直链或支链烷基; R 2是氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基或2价基团-CH = CH-CH = CH-或 - (CH 2)n - ,其中n是从3到 5,其中所述二价基团的游离键连接到苯环的相邻碳原子上; 且R 3为氢或1至3个碳原子的烷基; R4是1〜3个碳原子的烷基; 或R 3和R 4彼此一起为 - (CH 2)p - ,其中p为4至6的整数,或其无毒的药学上可接受的酸加成盐。 式I化合物可用于治疗和预防冠状动脉疾病,治疗高血压和治疗心律失常,特别是心动过速。

    Hypertensive phenylalkylamines and salts thereof
    3.
    发明授权
    Hypertensive phenylalkylamines and salts thereof 失效
    高效苯丙氨酸及其盐

    公开(公告)号:US4146645A

    公开(公告)日:1979-03-27

    申请号:US761476

    申请日:1977-01-24

    CPC分类号: C07C275/40

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, --(CH.sub.2).sub.n --R.sub.4 or --CO--R.sub.5,where n is 1 or 2,R.sub.4 is hydrogen, cyano or benzoyl, andR.sub.5 is hydrogen, lower alkoxy, benzyloxy, --CH.sub.2 --NH.sub.2, --CH(CH.sub.3)--NH.sub.2, --CH.sub.2 --NH--CH.sub.2 --C.sub.6 H.sub.5 or --CH(CH.sub.3)--NH--CH.sub.2 --C.sub.6 H.sub.5,R.sub.2 is hydrogen or methyl, andR.sub.3 is amino, nitro, --NH--CO--R.sub.6 or --NH--A--R.sub.7,where R.sub.6 is hydrogen, methyl, methoxy, ethoxy, methylthio or ethylthio,R.sub.7 is amino, methylamino or dimethylamino, andA is --CO-- or --SO.sub.2 --,provided, however, that R.sub.1 and R.sub.4 are other than hydrogen and R.sub.2 is other than hydrogen or methyl when R.sub.6 is hydrogen or methyl, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as hypertensives.

    Pharmaceutical compositions containing a
1-(cyano-phenoxy)-2-hydroxy-3-hydroxyalkylamino-propane and method of
use
    4.
    发明授权
    Pharmaceutical compositions containing a 1-(cyano-phenoxy)-2-hydroxy-3-hydroxyalkylamino-propane and method of use 失效
    含有1-(氰基 - 苯氧基)-2-羟基-3-羟基烷基氨基丙烷的药物组合物及其使用方法

    公开(公告)号:US4025646A

    公开(公告)日:1977-05-24

    申请号:US652113

    申请日:1976-01-26

    IPC分类号: C07D317/64 A61K31/275

    CPC分类号: C07D317/64

    摘要: Pharmaceutical compositions containing as an active ingredient a racemic or optically active compound of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms, andR.sub.2 is straight or branched hydroxyalkyl of 3 to 6 carbon atoms,Or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as .beta.-adrenergic receptor blocking agents and hypotensives.

    摘要翻译: 含有下式的外消旋或旋光活性化合物作为活性成分的药物组合物,其中R 1是氢,卤素,1至4个碳原子的烷基或1至4个碳原子的烷氧基,R 2是直链或支链羟烷基 3至6个碳原子,或非毒性,药理学上可接受的酸添加盐; 以及将其用作β-受体阻断剂阻断剂和高血压药物的方法。

    1-Aryloxy-3-alkylamino-propan-2-ols
    7.
    发明授权
    1-Aryloxy-3-alkylamino-propan-2-ols 失效
    1-芳氧基-3-烷基氨基 - 丙-2-醇

    公开(公告)号:US4442120A

    公开(公告)日:1984-04-10

    申请号:US398577

    申请日:1982-07-15

    CPC分类号: C07C255/00 Y10S514/821

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is cycloalkyl of 3 to 10 carbon atoms; phenyl; mono- or poly-substituted phenyl, where the substituents are halogen, lower alkyl, lower alkoxy, lower alkenyl, lower alkinyl, lower alkinyloxy, lower cycloalkyl, acyl, acyloxy, lower alkoxycarbonyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl or the ring-forming groups (--CH.dbd.CH--).sub.2 or --O--CH.sub.2 --O-- attached to vicinal carbon atoms of the phenyl ring; aryloxy-lower alkyl; (mono- or poly-substituted aryl)-oxy-lower alkyl, where the substituents are halogen, lower alkyl, lower alkoxy, lower alkenyl, lower alkinyl, lower alkinyloxy, lower cycloalkyl, acyl, acyloxy, lower alkoxycarbonyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl or the ring-forming groups (--CH.dbd.CH--).sub.2 or --O--CH.sub.2 --O-- attached to vicinal carbon atoms of the phenyl ring;R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or the ring-forming group (--CH.dbd.CH).sub.2 or --(CH.sub.2).sub.n --, where n is an integer from 3 to 5, attached to vicinal carbon atoms of the phenyl ring; andR.sub.3 is straight or branched alkyl of 1 to 10 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful for the treatment of tachycardia, hypertension and coronary diseases.

    摘要翻译: 其中R 1是3至10个碳原子的环烷基的化合物< IMAGE> 苯基; 单取代或多取代的苯基,其中取代基为卤素,低级烷基,低级烷氧基,低级烯基,低级炔基,低级烷氧基,低级环烷基,酰基,酰氧基,低级烷氧基羰基,羟基 - 低级烷基,低级烷氧基 - 低级烷基或 连接到苯环的邻位碳原子上的成环基团(-CH = CH-)2或-O-CH2-O-; 芳氧基 - 低级烷基; (单或多取代芳基) - 氧基 - 低级烷基,其中取代基是卤素,低级烷基,低级烷氧基,低级烯基,低级炔基,低级烷氧基,低级环烷基,酰基,酰氧基,低级烷氧基羰基,羟基 - 低级烷基 ,低级烷氧基 - 低级烷基或连接到苯环的邻位碳原子上的成环基团(-CH = CH-)2或-O-CH2-O-; R 2是氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基或成环基团(-CH = CH)2或 - (CH 2)n - ,其中n是从3到 5,连接苯环的连位碳原子; 并且R 3是1至10个碳原子的直链或支链烷基; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用于治疗心动过速,高血压和冠状动脉疾病。

    1-(Alkanoylamino-aryloxy)-2-hydroxy-3-(alkinyl-amino)-propanes and salts
thereof
    8.
    发明授权
    1-(Alkanoylamino-aryloxy)-2-hydroxy-3-(alkinyl-amino)-propanes and salts thereof 失效
    1-(烷酰基氨基 - 芳氧基)-2-羟基-3-(炔基 - 氨基) - 丙烷及其盐

    公开(公告)号:US4344964A

    公开(公告)日:1982-08-17

    申请号:US241519

    申请日:1981-03-09

    CPC分类号: C07C255/00 A61K31/505

    摘要: This invention relates to a compound of the formula ##STR1## wherein R.sub.1 is ethyl or isopropyl;R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or a bivalent radical --CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.n --, where n is an integer from 3 to 5, inclusive, and the free bonds of said bivalent radical are attached to adjacent carbon atoms of the phenyl ring; andR.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.4 is alkyl of 1 to 3 carbon atoms; orR.sub.3 and R.sub.4, together with each other, are --(CH.sub.2).sub.p --, where p is an integer from 4 to 6, inclusive,or a non-toxic, pharmacologically acceptable acid addition salt thereof. The compounds of formula I are useful for treatment and prophylaxis of diseases of the coronaries, for treatment of hypertension, and for treatment of cardiac arrhythmia, particularly tachycardia.

    摘要翻译: 本发明涉及式(I)的化合物,其中R 1是乙基或异丙基; R 2是氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基或2价基团-CH = CH-CH = CH-或 - (CH 2)n - ,其中n是从3到 5,其中所述二价基团的游离键连接到苯环的相邻碳原子上; 且R 3为氢或1至3个碳原子的烷基; R4是1〜3个碳原子的烷基; 或R 3和R 4彼此一起为 - (CH 2)p - ,其中p为4至6的整数,或其无毒的药学上可接受的酸加成盐。 式I化合物可用于治疗和预防冠状动脉疾病,治疗高血压和治疗心律失常,特别是心动过速。