Pharmacologically active novel O-substituted pyruvic acid oximes
    2.
    发明授权
    Pharmacologically active novel O-substituted pyruvic acid oximes 失效
    药理活性新型O-取代丙酮酸肟

    公开(公告)号:US4425360A

    公开(公告)日:1984-01-10

    申请号:US300076

    申请日:1981-09-08

    CPC分类号: C07D295/185 Y10S514/866

    摘要: The present invention provides pyruvic acid oximes of the general formula: ##STR1## wherein R is a hydrogen atom, a C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, cinnamyloxy, phenylamino, phenyl-N-alkylamino or phenylthio radical or an aryl or aryloxy radical, the aryl moiety of which can be substituted one or more times by C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen, hydroxyl, trifluoromethyl, amino, acetylamino, nitrile, nitro or methylenedioxy, A is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon chain containing up to 10 carbon atoms, which can be substituted one or more times by halogen or hydroxyl, and R.sub.1 is a C.sub.1 -C.sub.8 alkyl radical, which can be substituted one or more times by halogen, hydroxyl, nitrile, phenyl or carboxyl, or is a nitrile or formyl group, with the proviso that when R--A-- is a methyl or ethyl radical, R.sub.1 is not a methyl radical or a nitrile group and when R--A-- is a benzyl radical, R.sub.1 is not a methyl or benzyl radical; and the physiologically acceptable salts, carboxylic acid esters and amides thereof. The invention also provides processes for the preparation of these compounds pharmaceutical compositions containing them, and their use in combating hypoglycaemia.

    摘要翻译: 本发明提供以下通式的丙酮酸肟:其中R为氢原子,C 3 -C 8环烷基,C 1 -C 6烷氧基,肉桂氧基,苯基氨基,苯基-N-烷基氨基或苯硫基或 芳基或芳氧基,其芳基部分可以被C 1 -C 6烷基,C 1 -C 6烷氧基,卤素,羟基,三氟甲基,氨基,乙酰氨基,腈,硝基或亚甲二氧基取代一次或多次,A是直链 或含有至多10个碳原子的支链,饱和或不饱和脂族烃链,其可以被卤素或羟基取代一次或多次,并且R 1是可被卤素取代一次或多次的C 1 -C 8烷基, 羟基,腈,苯基或羧基,或者是腈或甲酰基,条件是当RA-是甲基或乙基时,R 1不是甲基或腈基,当RA-是苄基时,R 1 不是甲基或苄基; 和其生理上可接受的盐,羧酸酯和酰胺。 本发明还提供了制备这些化合物的方法,含有它们的药物组合物及其在抗低血糖中的应用。

    Piperazine-substituted aryl and aralkyl carboxylic acids useful for
treating infirmaties caused by excess lipids or thrombocyte
    7.
    发明授权
    Piperazine-substituted aryl and aralkyl carboxylic acids useful for treating infirmaties caused by excess lipids or thrombocyte 失效
    哌嗪取代的芳基和芳烷基羧酸,可用于治疗由过量脂质或血小板细胞引起的体温

    公开(公告)号:US4616086A

    公开(公告)日:1986-10-07

    申请号:US657032

    申请日:1984-10-01

    摘要: The present invention is concerned with new carboxylic acid derivatives, with processes for the preparation thereof and with pharmaceutical compositions for lipid depression and thrombocyte aggregation, containing them, and to methods for treating infirmaties caused by excess lipids or thrombocyte aggregation.The new carboxylic acid derivatives according to the present invention are compounds of the general formula: ##STR1## wherein A is a valency bond or a lower alkylene chain, B is a valency bond or a saturated or unsaturated lower alkylene chain, R is hydrogen, an alkyl group which can be substituted by hydroxyl, carboxyl, sulphonic acid or optionally substituted phenoxy group, or R is an aralkyl radical, the aryl moiety of which can be substituted and the alkyl moiety of which is optionally unsaturated and can contain up to 4 carbon atoms, or R is a phenacyl radical, the phenyl moiety optionally substituted, or R is an acyl radical derived from aliphatic, araliphatic or aromatic carboxylic or sulphonic acid, or R is an aryl radical optionally substituted with the proviso that when A is a valency bond, R cannot be hydrogen, methyl, ethyl, hydroxyethyl, benzyl or phenyl, and the physiologically acceptable salts, esters and amides thereof.

    摘要翻译: 本发明涉及新的羧酸衍生物,其制备方法和含有它们的脂质抑制和血小板聚集的药物组合物,以及用于治疗由过量脂质或凝血细胞聚集引起的不孕症的方法。 根据本发明的新的羧酸衍生物是下列通式的化合物:其中A是价键或低级亚烷基链,B是价键或饱和或不饱和的低级亚烷基链,R 是氢,可以被羟基,羧基,磺酸或任选取代的苯氧基取代的烷基,或R是芳烷基,其芳基部分可以被取代,并且其烷基部分任选是不饱和的并且可以含有 最多4个碳原子,或R是苯甲酰基,苯基部分任选被取代,或R是衍生自脂族,芳脂族或芳族羧酸或磺酸的酰基,或R是任选被取代的芳基,条件是当 A是价键,R不能是氢,甲基,乙基,羟乙基,苄基或苯基,以及它们的生理上可接受的盐,酯和酰胺。