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    Organosilane derivatives, pharmaceutical compositions containing them and process for preparing same
    1.
    发明授权
    Organosilane derivatives, pharmaceutical compositions containing them and process for preparing same 失效
    有机硅烷衍生物，含有它们的药物组合物及其制备方法

    公开(公告)号：US5340823A

    公开(公告)日：1994-08-23

    申请号：US993139

    申请日：1992-12-18

    申请人： Sandor Farkas ,  Sandor Foldeak ,  Egon Karpati ,  Peter Hegyes ,  Janos Kreidl ,  Laszlo Szporny ,  Laszlo Czibula ,  Szilvia Petofi-Vass

    发明人： Sandor Farkas ,  Sandor Foldeak ,  Egon Karpati ,  Peter Hegyes ,  Janos Kreidl ,  Laszlo Szporny ,  Laszlo Czibula ,  Szilvia Petofi-Vass

    IPC分类号： A61K31/695 ,  C07F7/08 ,  C07F7/10 ,  A61K31/445 ,  C07D7/10

    CPC分类号： C07F7/0812 ,  C07F7/0818

    摘要： A method of treating a mammalian subject for Parkinson's disease or to provide a central muscle relaxant effect, which comprises the step of administering to the mammalian subject in need of the treatment, a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein m is 1,2 or 3;R.sub.1 and R.sub.2 each independently stand for hydrogen, C.sub.1 to C.sub.4 straight or branched chain alkyl, C.sub.1 to C.sub.4 alkoxy, C.sub.5 to C.sub.7 cycloalkyl, or halogen; andB is a 5- or 6-membered saturated or unsaturated heterocyclic group containing a nitrogen heteroatom, the heterocyclic group being bound through its heterocyclic nitrogen atom to the remainder of the compound, and which can contain one or two additional heteroatoms selected from the group consisting of an oxygen heteroatom, a sulfur heteroatom, and one or two additional nitrogen heteroatoms, which may be as an .dbd.N--, --NH-- or --NR-- group, where R is a C.sub.1 to C.sub.5 alkyl or C.sub.1 to C.sub.5 alkycarbonyl group, the nitrogen-containing heterocyclic group is unsubstituted or substituted on one of its carbon atoms by C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxycarbonyl; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 一种治疗哺乳动物受试者帕金森病或提供中枢肌肉松弛作用的方法，其包括向需要治疗的哺乳动物受试者施用治疗有效量的式（I）化合物的步骤（I）其中m是1,2或3; R1和R2各自独立代表氢，C1至C4直链或支链烷基，C1至C4烷氧基，C5至C7环烷基或卤素; 并且B是含有氮杂原子的5或6元饱和或不饱和杂环基，杂环基通过其杂环氮原子与化合物的其余部分结合，并且其可以含有一个或两个另外的杂原子， 由氧杂原子，硫杂原子和一个或两个另外的氮杂原子组成，其可以是= N，-NH-或-NR-基，其中R是C1-C5烷基或C1-C5烷羰基 ，所述含氮杂环基是未取代的或在其碳原子之一被C1-C4烷基或C1-C4烷氧基羰基取代; 或其药学上可接受的盐。

    Novel apovincaminic acid derivatives
    3.
    发明授权
    Novel apovincaminic acid derivatives 失效
    新型氨基丁酸衍生物

    公开(公告)号：US4614824A

    公开(公告)日：1986-09-30

    申请号：US754671

    申请日：1985-07-11

    申请人： Janos Kreidl ,  Laszlo Czibula ,  Gyorgy Visky ,  Maria Farkas nee Kirjak ,  Judit Meszaros nee Brill ,  Dora Groo ,  Eva Palosi ,  Egon Karpati ,  Laszlo Szporny

    发明人： Janos Kreidl ,  Laszlo Czibula ,  Gyorgy Visky ,  Maria Farkas nee Kirjak ,  Judit Meszaros nee Brill ,  Dora Groo ,  Eva Palosi ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： A61K31/435 ,  A61P9/00 ,  C07D461/00

    CPC分类号： C07D461/00

    摘要： The invention relates to new racemic and optically active apovincaminic acid derivatives of the general formula (I) ##STR1## wherein A is hydroxyl, halogen or a group --O--(CH.sub.2).sub.n --OR.sup.1 or --OMe, in whichR.sup.1 is alkyl having from one to 6 carbon atoms,n is an integer between 2 and 6,Me is an alkali metal,R.sup.2 stands for an alkyl group having from one to 6 carbon atoms, which may be identical with or different from R.sup.1,and the hydrogen in the 3-position and the R.sup.2 group have an .alpha.,.alpha.- and/or .beta.,.beta.- or .alpha.,.beta.- and/or .beta.,.alpha.-configuration, and pharmaceutically acceptable acid addition salts thereof, which are pharmaceutically active, e.g. show antihypoxial activity or are potent peripheral vasodilators. Their preparation and pharmaceutical composition containing them are also within the scope of the invention.

    摘要翻译： 本发明涉及通式（I）的新的外消旋和光学活性氨基丁酸衍生物，其中A是羟基，卤素或-O-（CH2）n-OR1或-OMe基团，其中R1 是具有1至6个碳原子的烷基，n是2和6之间的整数，Me是碱金属，R 2表示具有1至6个碳原子的烷基，其可以与R 1相同或不同， 3-位和R2基团中的氢具有药学活性的α，α - 和/或β，β-或α，β-和/或β，α-构型及其药学上可接受的酸加成盐 ，例如 显示抗低氧活性或是有效的外周血管扩张剂。 它们的制备和含有它们的药物组合物也在本发明的范围内。