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    Organosilane derivatives, pharmaceutical compositions containing them and process for preparing same
    52.
    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。

    Anti-arrhythmic azabicyclic compounds
    53.
    发明授权
    Anti-arrhythmic azabicyclic compounds 失效
    抗心律不齐的氮杂双环化合物

    公开(公告)号：US4769373A

    公开(公告)日：1988-09-06

    申请号：US674773

    申请日：1984-11-26

    申请人： Karoly Nador ,  Gabor Kraiss ,  Margit Paroczay ,  Egon Karpati ,  Laszlo Szporny

    发明人： Karoly Nador ,  Gabor Kraiss ,  Margit Paroczay ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： A61K31/435 ,  A61P9/06 ,  A61P25/02 ,  C07D211/72 ,  C07D221/22 ,  C07D405/12 ,  C07D409/12 ,  A61K31/44

    CPC分类号： C07D221/22 ,  C07D211/72 ,  C07D405/12 ,  C07D409/12

    摘要： The invention relates to new anti-arrythmic azabicyclo[3.3.1]nonanes of the general formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are C.sub.1-4 alkyl groups which are the same or different, or one of them is a benzyl group and the others are C.sub.1-4 alkyl groups, andR.sup.4 is a hydroxy group, or an etherified hydroxy group of the formula --OR.sup.5, or an esterified hydroxy group of the formula --OOCR.sup.6, in which the esterifying groupR.sup.5 is a phenyl or benzyl group which optionally each can have a trihalomethyl substituent or one or more halogen or C.sub.1-4 substituents, or is a diphenyl or benzhydryl group, and the esterifying groupR.sup.6 is a C.sub.1-8 alkyl or a C.sub.3-6 cycloalkyl group, or a phenyl or benzyl group which optionally each can have a halo-substituent or one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro or phenyl substituents, or is an optionally halogenated or hydrogenated naphthyl group, or a cinnamyl group optionally substituted by a halogen atom or C.sub.1-4 alkoxy groups, or is a benzhydryl or 1,1-diphenyl-hydroxymethyl group, or is a heterocyclic substituent selected from the group consisting of thenyl, 9-xanthenyl or 3-indolyl-(C.sub.1-3 alkyl) groups,as well as the stereoisomers and pharmaceutically acceptable acid addition salts thereof.The invention also provides a process for the preparation of the new compounds of the general formula (I), in which new intermediates of the general formula (IV), ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, are utilized.

    摘要翻译： 本发明涉及通式（I）的新的抗焦虑氮杂二氮杂双环[3.3.1]壬烷，其中R1，R2和R3是相同或不同的C1-4烷基，或其中之一 它们是苄基，其它是C 1-4烷基，R4是羟基，或式-OR5的醚化羟基或式-OOCR6的酯化羟基，其中酯化基团R5 是任选地可以具有三卤代甲基取代基或一个或多个卤素或C 1-4取代基的苯基或苄基，或者是二苯基或二苯甲基，酯化基团R6是C 1-8烷基或C 3-6环烷基 基团或苯基或苄基，其任选地各自可以具有卤素取代基或一个或多个C 1-4烷基，C 1-4烷氧基，硝基或苯基取代基，或者是任选卤代或氢化的萘基或肉桂基 任选被卤素原子或C 1-4烷氧基取代，或者是二苯甲基或1,1-二苯基 - 氢 或者是选自草酰基，9-呫吨基或3-吲哚基 - （C 1-3烷基）基团的杂环取代基，以及它们的立体异构体和药学上可接受的酸加成盐。 本发明还提供了制备通式（I）的新化合物的方法，其中通式（IV）的新中间体，其中R 1，R 2和R 3如上所定义， 被利用。

    14-Substituted vincanes
    57.
    发明授权
    14-Substituted vincanes 失效
    14取代的维根素

    公开(公告)号：US4120858A

    公开(公告)日：1978-10-17

    申请号：US719066

    申请日：1976-08-30

    申请人： Otto Clauder ,  Jozsef Kokosi ,  Laszlo Szporny ,  Egon Karpati

    发明人： Otto Clauder ,  Jozsef Kokosi ,  Laszlo Szporny ,  Egon Karpati

    IPC分类号： A61K31/435 ,  A61P9/08 ,  A61P9/12 ,  A61P25/02 ,  A61P43/00 ,  C07D461/00 ,  C07D519/04

    CPC分类号： C07D461/00 ,  Y10S514/824

    摘要： A compound of the formula (I) ##STR1## wherein X stands for a hydrogen atom, an optionally substituted aliphatic or aromatic sulfonyloxy group, a thiocyanato group, an azido group or an amino group optionally mono- or disubstituted by aliphatic, cycloaliphatic, aromatic or araliphatic hydrocarbon groups, acyl, alkyloxycarbonyl, cycloalkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl, aminocarboimido groups or the substituents of the said amino group may form with the nitrogen atom thereof a five-, six- or seven-membered saturated or unsaturated heterocyclic ring optionally containing a further nitrogen, oxygen or sulfur hetero atom, and a quaternary salt or acid addition salt thereof. The compounds are useful in the treatment of arteriosclerosis and high blood pressure.

    摘要翻译： 式（I）的化合物其中X代表氢原子，任选取代的脂族或芳族磺酰氧基，硫氰酸酯基，叠氮基或氨基，任选被脂族，脂环族，芳族 或芳脂族烃基，酰基，烷氧基羰基，环烷氧基羰基，芳氧基羰基，芳烷氧基羰基，氨基羧基亚氨基或所述氨基的取代基可以与其氮原子一起形成五元，六元或七元饱和或不饱和杂环，任选地含有 进一步的氮，氧或硫杂原子，及其季盐或酸加成盐。 该化合物可用于治疗动脉硬化和高血压。