Alkanolamine derivatives and pharmaceutical compositions and uses thereof
    32.
    发明授权
    Alkanolamine derivatives and pharmaceutical compositions and uses thereof 失效
    烷醇胺衍生物及其药物组合物及其用途

    公开(公告)号:US4167581A

    公开(公告)日:1979-09-11

    申请号:US956986

    申请日:1978-11-01

    申请人: Leslie H. Smith

    发明人: Leslie H. Smith

    摘要: 1-Aryloxy-3-aminoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. The compounds possess .beta.-adrenergic blocking activity and some of them additionally possess cardiac stimulant activity. Representative of the compounds disclosed is 1-(2-cyanophenoxy)-3-.beta.(4-hydroxyphenylacetamido)ethylamino-2-propanol.

    摘要翻译: 1-芳氧基-3-氨基烷基氨基-2-丙醇衍生物,其制备方法,含有它们的药物组合物和使用它们治疗心脏病的方法。 该化合物具有β-肾上腺素能阻滞活性,其中一些另外具有心脏兴奋剂活性。 所公开的化合物的代表是1-(2-氰基苯氧基)-3-β(4-羟基苯基乙酰氨基)乙基氨基-2-丙醇。

    Derivatives of 3-benzoyl-2-({62 -hydroxyphenethylamino)-propionitrile
    35.
    发明授权
    Derivatives of 3-benzoyl-2-({62 -hydroxyphenethylamino)-propionitrile 失效
    3-苯甲酰基-2 - ({62-羟基苯甲酰氨基) - 丙酸酯的衍生物

    公开(公告)号:US3846470A

    公开(公告)日:1974-11-05

    申请号:US23935972

    申请日:1972-03-29

    摘要: The present invention relates to new pharmacologically valuable ketone derivatives exhibiting a distinct dilatory action on the cerebral vessels and which have the general formula

    AND THEIR PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS, WHEREIN R1 stands for a member selected from the group consisting of CN, -CONH2, -COOH, -COONa and -COOK, R2 stands for a member selected from the group consisting of

    X stands for alkylene having 1 to 4 carbon atoms, Y stands for a member selected from the group consisting of -OCO- and -CO-NH-, R3 and R4 each stand for a member selected from the group consisting of hydrogen and alkyl having 1 to 6 carbon atoms, R5 stands for a member selected from the group consisting of hydrogen and -OH, the nucleus I may have 1 to 3 alkoxy, halogen, alkyl or nitro substituents, THE NUCLEUS II may have 1 to 3 alkoxy, halogen or alkyl substituents, THE NUCLEUS III may be substituted by 1 to 3 methoxy groups and to processes for producing said ketone derivatives.

    摘要翻译: 本发明涉及对脑血管表现出明显的缓解作用的新的药理学有价值的酮衍生物,其具有通式及其药物可接受酸的添加剂,其中R1代表选自-CN,-CONH 2 ,-COOH,-COONa和-COOK,R2代表选自X代表具有1至4个碳原子的亚烷基的成员,Y代表选自-O- CO-和 - CO-NH-,R3和R4各自表示选自氢和具有1至6个碳原子的烷基的成员,R5代表选自氢和-OH的成员,核可以具有 1至3个烷氧基,卤素,烷基或硝基取代基,核酸II可具有1至3个烷氧基,卤素或烷基取代基,核酸III可被1至3个甲氧基取代,以及制备所述酮衍生物的方法。

    .alpha., .omega.-dicarboxylic acids and medicaments which contain these
compounds
    39.
    发明授权
    .alpha., .omega.-dicarboxylic acids and medicaments which contain these compounds 失效
    α,ω-二羧酸和含有这些化合物的药物

    公开(公告)号:US4711896A

    公开(公告)日:1987-12-08

    申请号:US840563

    申请日:1986-02-21

    摘要: ##STR1## α, ω-dicarboxylic acids having the general formula (I') in which: R
    1 and R
    2 , which may be different or the same, represent a lower alkyl group which can be substituted by hydroxy, lower alkoxy, halogen or phenyl, the phenyl being capable of substitution one or several times by hydroxy, lower alkoxy, lower alkyl or halogen; a lower alkenyl or alkinyl group; a C
    3 -C
    7 -cyclo-alkyl group or a phenyl group possibly substituted by hydroxy, halogen, lower alkyl or lower alkoxy, and X and Y, which may be different or the same, represent hydrogen, lower alkyl, lower alkoxy, hydroxy, cyano, halogen, carboxyl, lower alkoxycarbonyl or carbamoyl, and Q represents non-ramified, saturated or unsaturated alkyl chain with 8-14 C atoms, which can be substituted, interrupted by hetero-atoms, and form part of a cyclic system, as well as their carboxylic acid derivatives in vivo, provided that when Q represents an unramified, saturated alkyl chain with 8-14 C atoms, and R
    1 and R
    2 represent methyl and Y represents hydrogen, X may not represent hydrogen, ethoxy-carbonyl, bromine, cyano or methyl, and if R
    1 and R
    2 represent methyl and X and Y hydrogen, then Q may not represent any formula (II) group. Process for their preparation and medicines containing these compounds, which have an anti-diabetic action and lower the level of lipids.

    摘要翻译: PCT No.PCT / EP85 / 00288 Sec。 371日期1986年2月21日 102(e)日期1986年2月21日PCT归档1985年6月15日PCT公布。 公开号WO86 / 00298 日本1月16日,1986年1月16日,具有通式(I')的α,ω-二羧酸,其中:R1和R2可以不同或相同,表示 可被羟基,低级烷氧基,卤素或苯基取代的低级烷基,苯基能够被羟基,低级烷氧基,低级烷基或卤素取代一次或几次; 低级烯基或炔基; 可以被羟基,卤素,低级烷基或低级烷氧基取代的C 3 -C 7 - 环烷基或苯基,X和Y可以不同或相同,表示氢,低级烷基,低级烷氧基,羟基, 氰基,卤素,羧基,低级烷氧基羰基或氨基甲酰基,Q表示具有8-14个C原子的非分支,饱和或不饱和的烷基链,其可被取代,被杂原子间隔并形成环系的一部分,如 以及它们的体内羧酸衍生物,条件是当Q表示具有8-14个C原子的未饱和的饱和烷基链时,R 1和R 2表示甲基且Y表示氢,X可以不表示氢,乙氧羰基,溴, 氰基或甲基,并且如果R 1和R 2表示甲基且X和Y氢,则Q可以不表示任何式(II)基团。 其制备方法和含有这些化合物的药物,其具有抗糖尿病作用并降低脂质水平。