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150 条记录 (耗时 0.026 秒)

    2-Azabicyclo(2.2.2)octane derivatives and their use as immunosuppressive agents
    142.
    发明授权
    2-Azabicyclo(2.2.2)octane derivatives and their use as immunosuppressive agents 失效
    2-氨基双环（2.2.2）辛烷衍生物及其作为免疫抑制剂的用途

    公开(公告)号：US4563464A

    公开(公告)日：1986-01-07

    申请号：US625069

    申请日：1984-06-27

    申请人： Elemer Ezer ,  Laszlo Szporny ,  Gyorgy Hajos ,  Csaba Szantay ,  Tibor Keve ,  Gyorgy Fekete ,  Gabor Megyeri ,  Tibor Acs ,  Hedvig Bolcskei

    发明人： Elemer Ezer ,  Laszlo Szporny ,  Gyorgy Hajos ,  Csaba Szantay ,  Tibor Keve ,  Gyorgy Fekete ,  Gabor Megyeri ,  Tibor Acs ,  Hedvig Bolcskei

    IPC分类号： A61K31/435 ,  A61P1/04 ,  A61P9/08 ,  A61P25/08 ,  A61P37/06 ,  C07D211/82 ,  C07D453/06 ,  C07D491/18 ,  A61K31/445 ,  C07D221/22

    CPC分类号： C07D211/82 ,  C07D453/06

    摘要： The invention relates to new 2-azabicyclo[2.2.2]octane derivatives of the formula (I), ##STR1## wherein A is hydrogen, alkoxycarbonyl having from one to 4 carbon atoms in the alkoxy group, phenylalkoxycarbonyl having from one to 4 carbon atoms in the alkoxy moiety, alkyl having from one to 6 carbon atoms, aralkyl containing from one to 4 carbon atoms in the alkyl moiety or substituted acyl,R.sub.1 is hydrogen or alkyl having from one to 4 carbon atoms,Z is hydrogen or halogen,X is hydrogen or halogen,Y is hydrogen, orX and Y together represent a C--C bond,W is alkoxycarbonyl having from one to 4 carbon atoms in the alkoxy moiety, cyano, carboxamido or haloformyl, orif X stands for halogen, X and Y together represent a ##STR2## group. According to another aspect of the invention there is provided a process for the preparation of the above compounds, which are pharmaceutically active, in particular, possess valuable anticonvulsive, vasodilating or gastric acid secretion inhibiting properties. Pharmaceutical compositions containing compounds of the formula (I) are also within the scope of the invention.

    摘要翻译： 本发明涉及式（I）的新的2-氮杂双环[2.2.2]辛烷衍生物，其中A是氢，烷氧基中具有1至4个碳原子的烷氧基羰基，具有1个 在烷氧基部分中具有4个碳原子，具有1至6个碳原子的烷基，在烷基部分含有1至4个碳原子的芳烷基或取代的酰基，R 1是氢或具有1至4个碳原子的烷基，Z是氢 或卤素，X是氢或卤素，Y是氢，或X和Y一起代表CC键，W是在烷氧基部分具有1至4个碳原子的烷氧基羰基，氰基，甲酰氨基或卤代甲酰基，或者如果X代表卤素 ，X和Y一起表示组。 根据本发明的另一方面，提供了一种制备上述化合物的方法，其具有药学活性，特别是具有有价值的抗惊厥，血管舒张或胃酸分泌抑制性质。 含有式（I）化合物的药物组合物也在本发明的范围内。

    Process for the preparation of 11-bromo-vincaminic acid ester derivatives and their use in protecting animals against cerebral hypoxy
    146.
    发明授权
    Process for the preparation of 11-bromo-vincaminic acid ester derivatives and their use in protecting animals against cerebral hypoxy 失效
    制备11-溴 - 长春胺酸酯衍生物的方法及其在保护动物免受脑缺氧的作用

    公开(公告)号：US4283401A

    公开(公告)日：1981-08-11

    申请号：US56647

    申请日：1979-07-11

    申请人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Egon Karpati ,  Laszlo Szporny

    发明人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： C07D461/00 ,  C07D471/22 ,  A61K31/55 ,  C07D459/00

    CPC分类号： C07D461/00

    摘要： A novel process for preparing 11-bromo-vincaminic acid esters of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand independently from each other for a C.sub.1-6 alkyl group, comprising the steps of treating a 1-alkyl-1-alkoxycarbonylethyl-octahydroindolo-quinolisine of the general formula ##STR2## wherein R.sup.2 is as defined above and R.sup.3 stands for a C.sub.1-6 alkyl group, with a brominating agent and treating the resulting isomeric mixture of the bromo-derivatives with an alkaline agent or treating the corresponding 14-oxo-E-homo-eburnane being unsubstituted in ring A with a brominating agent and nitrosating the resulting 11-bromo-14-oxo-E-homo-eburnane of the general formula ##STR3## wherein R.sup.2 is as defined above, then subjecting the resulting 11-bromo-14-oxo-15-hydroxyimino-E-homoeburnanes to deoxyimination and treating the 14,15-dioxo-derivatives obtained with a base in an alcohol of the general formula R.sup.1 OH, wherein R.sup.1 is as defined above.All the intermediate products are novel and exhibit a therapeutical protecting effect against cerebral hypoxy.

    摘要翻译： 一种用于制备通式为“IMAGE”的11-溴 - 长春胺酸酯的新方法，其中R 1和R 2各自独立地为C 1-6烷基独立地包括如下步骤：将1-烷基-1-烷氧基羰基乙基 其中R 2如上所定义，R 3表示C 1-6烷基，与溴化剂反应，并用碱处理所得到的溴代衍生物的异构体混合物或处理 环A中未取代的相应的14-氧代-E-均 - 异丁苯与溴化剂并亚硝化所得的通式为“IMAGE”的11-溴-14-氧代-E-均 - 胡烷，其中R2如上定义， 然后将所得的11-溴代-14-氧代-15-羟基亚氨基-E-高硼烷进行脱氧亚胺化处理，并用在通式为R 1 OH的醇中用碱获得的14,15-二氧代衍生物进行脱氧，其中R1如上定义 。 所有的中间产物都是新颖的，并且对脑缺氧具有治疗保护作用。