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    Pharmacologically active novel O-substituted pyruvic acid oximes
    1.
    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

    申请人： Hans P. Wolff ,  Ruth Heerdt ,  Manfred Hubner, deceased ,  Hans Kuhnle ,  Felix H. Schmidt

    发明人： Hans P. Wolff ,  Ruth Heerdt ,  Manfred Hubner, deceased ,  Hans Kuhnle ,  Felix H. Schmidt

    IPC分类号： A61K31/15 ,  A61K31/19 ,  A61K31/195 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  C07C249/08 ,  C07C251/32 ,  C07C251/36 ,  C07C251/50 ,  C07C251/52 ,  C07C251/54 ,  C07C251/60 ,  C07C253/30 ,  C07C255/50 ,  C07D295/185 ,  C07C131/00

    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。

    Hypoglycaemically and hypolipidaemically active derivatives of phenyl-alkane-carboxylic acids
    4.
    发明授权
    Hypoglycaemically and hypolipidaemically active derivatives of phenyl-alkane-carboxylic acids 失效
    苯基 - 烷烃 - 羧酸的低血糖和降血糖活性衍生物

    公开(公告)号：US4238506A

    公开(公告)日：1980-12-09

    申请号：US920508

    申请日：1978-06-29

    申请人： Kurt Stach, deceased ,  Elmar Bosies ,  Ruth Heerdt ,  Hans-Frieder Kuhnle ,  Felix H. Schmidt

    发明人： Kurt Stach, deceased ,  Elmar Bosies ,  Ruth Heerdt ,  Hans-Frieder Kuhnle ,  Felix H. Schmidt

    IPC分类号： C07D213/82 ,  C07D241/24 ,  C07D307/79 ,  C07D311/66 ,  C07D333/38 ,  C07C101/42

    CPC分类号： C07D213/82 ,  C07D241/24 ,  C07D307/79 ,  C07D311/66 ,  C07D333/38 ,  C07C2103/18

    摘要： Phenyl-alkane-carboxylic acids of the formula ##STR1## wherein A is an aryl, aralkyl or arylvinyl radical optionally substituted by hydroxy, halogen, trifluoromethyl, alkyl, alkylthio, alkoxy, alkenyloxy, alkoxyalkoxy, alkyl-substituted amino, aryloxy or alkoxy-substituted aryloxy, or is an aryloxyalkyl or arylthioalkyl radical, or a heterocyclic ring system optionally substituted by halogen, alkyl or alkoxy,Y is a valency bond or an unbranched or branched lower alkylene radical containing up to 3 carbon atoms,X is a straight or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing 2 to 8 carbon atoms, there being at least 2 carbon atoms between the benzene ring and the carboxyl group, andR is a hydrogen atom or a lower alkyl radical, as well as physiologically compatible salts, esters and amides thereof, exhibit hypoglycaemic and hypolipidaemic activity.

    摘要翻译： 式（I）的苯基 - 烷烃 - 羧酸其中A是任选被羟基，卤素，三氟甲基，烷基，烷硫基，烷氧基，烯氧基，烷氧基烷氧基，烷基取代的氨基，芳氧基 或烷氧基取代的芳氧基，或是芳氧基烷基或芳硫基烷基，或任选被卤素，烷基或烷氧基取代的杂环体系，Y是价态键或含有至多3个碳原子的无支链或支链低级亚烷基，X是 含有2至8个碳原子的直链或支链，饱和或不饱和的二价脂族烃基，苯环和羧基之间至少有2个碳原子，R是氢原子或低级烷基，以及 其生理上相容的盐，酯和酰胺显示出低血糖和降血脂活性。