Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions
    2.
    发明授权
    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions 失效
    (4) - 氧丙醇胺化合物和治疗组合物

    公开(公告)号:US4503067A

    公开(公告)日:1985-03-05

    申请号:US479921

    申请日:1983-04-04

    CPC分类号: C07D209/88 C07D317/64

    摘要: Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen or lower alkyl, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2 --, oxygen or sulfur;Ar is mono- or bicyclic aryl or pyridyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl;R.sub.5 and R.sub.6 together can represent methylenedioxy;and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.

    摘要翻译: 式(I)的羧基 - (4) - 氧丙醇胺化合物,其中R 1是氢,低级烷酰基或芳酰基; R2是氢,低级烷基或芳基烷基; R3是氢或低级烷基; R4是氢或低级烷基,或者当X是氧时,R4与R5一起可以代表-CH2-O-; X是价键,-CH 2 - ,氧或硫; Ar是单环或双环芳基或吡啶基; R5和R6分别选自氢,卤素,羟基,低级烷基,氨基羰基,低级烷氧基,芳烷氧基,低级烷硫基,低级烷基亚磺酰基或低级烷基磺酰基; R5和R6一起可以代表亚甲二氧基; 并且其与生理上可接受的酸的盐在治疗和预防循环和心脏疾病例如高血压和心绞痛方面是显着的。

    Indazole compounds
    7.
    发明授权
    Indazole compounds 失效
    吲唑化合物

    公开(公告)号:US4171446A

    公开(公告)日:1979-10-16

    申请号:US790646

    申请日:1977-04-25

    CPC分类号: C07D231/56

    摘要: Indazole compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl,R' is hydrogen or acyl, e.g., alkanoyl, andR.sub.2 is benzyl or a radical of the general formula ##STR2## in which X is a reactive residue and Y is hydroxyl or X and Y together represent oxygen and, when R' is an acyl radical, R.sub.2 can also be hydrogen:Are valuable intermediates for the preparation of pharmacologically active compounds, e.g., adrenergic .beta.-receptor active 3-indazolyl-(4)-oxy-propan-2-ol-amines.

    摘要翻译: 式(I)的吲唑化合物,其中R 1是氢或低级烷基,R'是氢或酰基,例如烷酰基,R 2是苄基或通式为“IMAGE”的基团,其中X是反应性 残基,Y是羟基或X和Y一起代表氧,当R'是酰基时,R 2也可以是氢:

    Heterocyclic oxypropanolamine compounds and pharmaceutical compositions

    公开(公告)号:US4346093A

    公开(公告)日:1982-08-24

    申请号:US117190

    申请日:1980-01-31

    摘要: The present invention provides heterocyclic oxypropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl, aralkyl or lower alkanoyl radical, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen atoms or lower alkyl, hydroxyalkyl, alkoxycarbonyl or alkanoyloxyalkyl radicals or together represent an alkylene radical, R.sub.4 is a hydrogen atom or a lower alkanoyl radical or an aroyl radical, R.sub.5 is a hydrogen atom or a lower alkyl radical or an aralkyl radical, R.sub.6 is a hydrogen atom or a lower alkyl radical, R.sub.7 is a hydrogen atom, a hydroxyl group or a lower alkyl radical, Z is a valency bond, a methylene radical or an oxygen or sulphur atom, Ar is a carbocyclic aryl radical or a pyridyl radical, R.sub.8, R.sub.9 and R.sub.10, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, lower alkyl radicals, lower alkenyl radicals, lower alkoxy radicals, aralkoxy radicals, allyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or lower alkanoylamino radicals or R.sub.8 and R.sub.9 together represent a lower alkylenedioxy radical or R.sub.7 and R.sub.8 together represent a --CH.sub.2 --O-- radical and A is --X.sub.1 --Y.sub.1, in which X.sub.1 is a methylene or --NR.sub.11 -- radical, R.sub.11 being a hydrogen atom or a lower alkyl radical, and Y.sub.1 is a methylene radical or .dbd.C.dbd.Q, Q being an oxygen or sulphur atom; or A is --X.sub.2 .dbd.Y.sub.2 --, in which X.sub.2 and Y.sub.2, which can be the same or different and signify nitrogen atoms or .dbd.C(R.sub.12)-- groups, R.sub.12 being a hydrogen atom or a lower alkyl or an alkoxycarbonyl radical, and when --X.sub.2 .dbd.Y.sub.2 -- represents a --CH.dbd.N-- group and R.sub.1 is an alkyl or aralkyl radical, because of the ability of indazole to tautomerise, this can also be localized on the nitrogen atom represented by Y.sub.2, with the proviso that Y.sub.1 or Y.sub.2 is joined to .dbd.N--R.sub.1 in general formula (I), and, when Q is an oxygen atom or --X.sub.2 .dbd.Y.sub.2 -- represents --CR.sub.12 .dbd.CR.sub.12 -- and Z is a valency bond or when --X.sub.1 --Y.sub.1 -- represents ##STR2## and Z is an oxygen atom or a valency bond, either the two symbols R.sub.2 and R.sub.3 do not simultaneously represent hydrogen atoms or R.sub.7 and R.sub.8 together must form a --CH.sub.2 --O-- radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.Furthermore, the present invention is concerned with the use of these compounds for the treatment of cardiac and circulatory diseases.