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。

    Analgesic 1-acetonyl-2-(phenylimino)-imidazolidines and salts thereof
    3.
    发明授权
    Analgesic 1-acetonyl-2-(phenylimino)-imidazolidines and salts thereof 失效
    止痛性1-丙酰基-2-(苯基亚氨基) - 咪唑烷及其盐

    公开(公告)号:US4588736A

    公开(公告)日:1986-05-13

    申请号:US612340

    申请日:1984-05-21

    CPC分类号: C07D405/12 C07D233/50

    摘要: Compounds of the formula ##STR1## wherein X, Y and Z are each independently hydrogen, halogen, lower alkyl, halo(lower alkyl), lower alkoxy, halo(lower alkoxy), (lower alkyl)thio or halo(lower alkyl)thio, orY and Z, together with each other, are lower alkylenedioxy;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as analgesics.

    摘要翻译: 其中X,Y和Z各自独立地为氢,卤素,低级烷基,卤代(低级烷基),低级烷氧基,卤代(低级烷氧基),(低级烷基)硫代或卤代(低级烷基)硫基 ,或Y和Z彼此一起是低亚烷基二氧基; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用作镇痛药。

    Pharmaceutical compositions containing a
1-phenoxy-2-hydroxy-3-alkynylamino-propane and method of use

    公开(公告)号:US4084002A

    公开(公告)日:1978-04-11

    申请号:US742639

    申请日:1976-11-17

    IPC分类号: C07C275/34 A61K31/135

    CPC分类号: C07C275/34

    摘要: Pharmaceutical dosage unit compositions containing as an active ingredient a 1-aryloxy-2-hydroxy-3-alkynylamino-propane selected from the group consisting of racemic or optically active compounds of the formula ##STR1## wherein R.sub.1 is a member selected from the group consisting of hydrogen; halogen; nitro; alkyl having from 1 to 5 carbon atoms; alkoxy having from 1 to 4 carbon atoms; alkenyl having from 2 to 5 carbon atoms; alkynyl having from 2 to 5 carbon atoms; alkylamino having from 1 to 5 carbon atoms; dialkylamino having from 1 to 5 carbon atoms in each alkyl; alkoxyalkyl having from 2 to 6 carbon atoms; alkylaminoalkyl having from 2 to 6 carbon atoms; dialkylaminoalkyl having from 3 to 12 carbon atoms; --(CH.sub.2).sub.x -NH.sub.2 or --(CH.sub.2).sub.x -OH, where x is an integer from 0 to 3; alkynyloxy having from 3 to 6 carbon atoms; alkenyloxy having from 3 to 6 carbon atoms; --CO-R.sub.9, where R.sub.9 is a member selected from the group consisting of alkyl having 1 to 6 carbon atoms, phenylalkyl having 7 to 10 carbon atoms and phenyl; cycloalkyl having from 3 to 7 carbon atoms; phenyl; phenyl substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and nitro; phenoxy; and phenoxy substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and nitro;R.sub.2 is a member selected from the group consisting of hydrogen, halogen, alkyl having from 1 to 4 carbon atoms, alkoxy having from 1 to 4 carbon atoms, alkanoyl having from 2 to 4 carbon atoms, alkenyl having from 2 to 4 carbon atoms, amino and nitro;R.sub.3 is a member selected from the group consisting of hydrogen, halogen, alkyl having from 1 to 4 carbon atoms, alkoxy having from 1 to 4 carbon atoms and, together with R.sub.2 in the ortho-position, --CH.dbd.CH-CH.dbd.CH- or --(CH.sub.2).sub.n --, where n is an integer from 3 to 5;R.sub.4 is a member selected from the group consisting of hydrogen and alkyl having from 1 to 3 carbon atoms; andR.sub.5 is a member selected from the group consisting of alkyl having from 1 to 3 carbon atoms, and, together with R.sub.4, --(CH.sub.2).sub.p --, where p is an integer from 4 to 6;And physiologically compatible acid addition salts thereof; and a method of using the same as adrenolytics and hypotensives.

    Pharmaceutical compositions containing a
1-(cyano-phenoxy)-2-hydroxy-3-hydroxyalkylamino-propane and method of
use
    9.
    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。