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15 条记录 (耗时 0.019 秒)

    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

    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。

    Benzenesulfon YL-semicarbazides for lowering blood sugar levels
    9.
    发明授权
    Benzenesulfon YL-semicarbazides for lowering blood sugar levels 失效
    用于降低血糖水平的苯磺酸YL-氨基脲

    公开(公告)号：US3939269A

    公开(公告)日：1976-02-17

    申请号：US324836

    申请日：1973-01-18

    申请人： Walter Aumuller ,  Rudi Weyer ,  Ruth Heerdt

    发明人： Walter Aumuller ,  Rudi Weyer ,  Ruth Heerdt

    IPC分类号： A61K31/47 ,  A61K27/00

    CPC分类号： A61K31/47 ,  Y10S514/866 ,  Y10S514/884

    摘要： Hypoglycemically active benzenesulfonyl-semicarbazides of the formula ##SPC1##Wherein X is hydrogen, chlorine, bromine, methyl or methoxy, Y is --CH(CH.sub.3)-CH.sub.2 --, preferably --CH.sub.2 --CH.sub.2 --, Z is hydrogen or a hydrocarbon radical of 1 or 2 carbon atoms, which forms together with Y a 5- or 6-membered ring, R is alkylene-imino of 3 to 7 carbon atoms in the ring which may be unsaturated or substituted by 1 or 2 methyl or lower alkyl or methoxy, pentamethylene-imino substituted by endoalkylene of 1 to 3 carbon atoms, hexamethylene-imino substituted by endoethylene in .beta.- .epsilon.-position, tetrahydro-iso-indoline, 4,7-endoalkylenehexahydro- or -tetrahydro-iso-indoline, the endoalkylene containing 1 or 2 carbon atoms and the double bond of the tetrahydro compound being in 5,6-position, and the salts thereof as pharmaceutical preparations for oral administration and lowering of blood sugar level in the treatment of diabetes mellitus and the process for lowering the blood sugar level in the treatment of diabetes mellitus.

    摘要翻译： 式WHEREIN X的低分子活性苯磺酰基 - 氨基脲是氢，氯，溴，甲基或甲氧基，Y是-CH（CH 3）-CH 2 - ，优选-CH 2 -CH 2 - ，Z是氢或1或2的烃基 碳原子，其与Y一起形成5-或6-元环，R是环中具有3-7个碳原子的亚烷基亚氨基，其可以是不饱和的或被1或2个甲基或低级烷基或甲氧基，五亚甲基 - 四氢异吲哚啉，4,7-内亚烷基六氢或四氢异吲哚啉，含有1〜3个碳原子的亚烷基亚氨基，含有1〜3个碳原子的亚烷基亚烷基， 碳原子，四氢化合物的双键为5,6位，其盐作为用于口服给药的药物制剂和降低糖尿病治疗中的血糖水平以及降低血糖水平的方法 直接治疗 。。

    1-Aziridine carboxylic acid derivatives with immunostimulant activity
    10.
    发明授权
    1-Aziridine carboxylic acid derivatives with immunostimulant activity 失效
    具有免疫刺激活性的1-氮杂环丁烷羧酸衍生物

    公开(公告)号：US4376731A

    公开(公告)日：1983-03-15

    申请号：US859633

    申请日：1978-01-31

    申请人： Elmar Bosies ,  Ruth Heerdt ,  Rudi Gall ,  Uwe Bicker ,  Anna E. Ziegler

    发明人： Elmar Bosies ,  Ruth Heerdt ,  Rudi Gall ,  Uwe Bicker ,  Anna E. Ziegler

    IPC分类号： C07D203/20 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/395

    CPC分类号： C07D403/12 ,  C07D203/20 ,  C07D405/12 ,  C07D409/12

    摘要： 2-Substituted-1-aziridine-carboxylic acid esters exhibiting immuno-stimulant activity and of the formula ##STR1## wherein X is a carbamoyl or alkoxycarbonyl radical, andR.sup.1 is an aliphatic hydrocarbon radical optionally substituted by halogen, alkoxy, amino, carbamoyloxy, cycloalkyl, hydroxyl, an imido or heterocyclic radical, cycloalkyl; or aryl, aralkyl, aryloxyalkyl or arylthioalkyl wherein the aryl moiety is optionally substituted by halogen, alkyl, alkoxy, hydroxyl, amino, nitro, cyano, acyl, carbalkoxy, thioalkyl, alkylsulphonyl, phenyl or trifluoromethyl. Counterparts where X is --CN and R.sup.1 is as above, except for ethyl, are also new.

    摘要翻译： 2-取代的1-氮丙啶 - 羧酸酯，其具有免疫刺激活性，并且具有下式：其中X是氨基甲酰基或烷氧基羰基，R1是任选被卤素，烷氧基，氨基，氨基甲酰氧基取代的脂族烃基， 环烷基，羟基，亚氨基或杂环基，环烷基; 芳基，芳烷基，芳氧基烷基或芳硫基烷基，其中芳基部分任选被卤素，烷基，烷氧基，羟基，氨基，硝基，氰基，酰基，烷氧基，硫代烷基，烷基磺酰基，苯基或三氟甲基取代。 对应物，其中X为-CN和R1如上所述，除乙基以外，也是新的。