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    1,2,3,6-Tetrahydropyridine derivatives
    3.
    发明公开
    1,2,3,6-Tetrahydropyridine derivatives 失效
    1,2,3,6-四氢吡啶衍生物

    公开(公告)号：EP0490560A1

    公开(公告)日：1992-06-17

    申请号：EP91311257.9

    申请日：1991-12-03

    申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

    发明人： Gizur, Tibor ,  Harsányi, Kálmán ,  Csehi, Attila ,  Demeter, Anikó ,  Trischler, Ferenc ,  Vajda, Eva ,  Szporny, László ,  Kiss, Béla ,  Kárpáti, Egon ,  Pálosi, Eva ,  Szombathelyi, Zsolt ,  Sarkadi, Adám ,  Gere, Anikó ,  Bodó, Mihály ,  Csomor, Katalin ,  Laszy, Judit Nagykovacsi ,  Szentirmai, Zsolt ,  Lapis, Erzsébet ,  Szabó, Sándor

    IPC分类号： C07D211/70 ,  A61K31/44

    CPC分类号： C07D211/70

    摘要： The present invention relates to novel 1,2,3,6-tetrahydropyridine derivatives of the general formula (I)
    - wherein
    R stands for hydrogen or an alkyl group,
    X stands for an unsubstituted phenyl or benzyl group or for a phenyl or benzyl group substituted with a halogen atom,
    Y stands for hydrogen or halogen or a trifluoro-methyl group -
    as well as enantiomers acid addition salts thereof.
    The invention further extends to pharmaceutical compositions containing said compounds as active ingredient mainly for improving cerebral blood circulation and antihypoxic activity. The 1,2,3,6-tetrahydropyridine derivatives of the general formula (I) are prepared by treating an oxo derivative of the general formula (II)
    wherein R, X and Y are as given above in an organic solvent by a reducing agent and reacting the obtained 1,2,3,6-tetrahydropyridine derivative of the general formula (I), wherein R, X and Y are as given above, with a mineral or organic acid and converting the same, if desired, to an acid addition salt.

    摘要翻译： 本发明涉及通式（I）的新的1,2,3,6-四氢吡啶衍生物 - 其中R代表氢或烷基，X代表未取代的苯基或苄基或苯基或苄基 Y代表氢或卤素或三氟甲基 - 以及其对映体酸加成盐。 本发明进一步扩展到含有所述化合物作为活性成分的药物组合物，主要用于改善脑血液循环和抗缺氧活性。 通式（I）的1,2,3,6-四氢吡啶衍生物是通过将通式（II）的氧代衍生物（其中R，X和Y如上所述）在有机溶剂中用还原剂 并将得到的通式（I）的1,2,3,6-四氢吡啶衍生物（其中R，X和Y如上所述）与矿物酸或有机酸反应，并且如果需要将其转化为酸 加成盐。

    Diamino-androstane derivatives
    6.
    发明公开
    Diamino-androstane derivatives 失效
    二氨基 - 雄甾烷衍生物

    公开(公告)号：EP0208497A2

    公开(公告)日：1987-01-14

    申请号：EP86305079.5

    申请日：1986-07-01

    申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

    发明人： Tuba, Zoltán ,  Horváth, Judit ,  Lovas, Mária ,  Riesz, Miklos ,  Szporny, László ,  Kárpáti, Egon

    IPC分类号： C07J43/00 ,  A61K31/58 ,  C07J13/00 ,  C07J71/00

    CPC分类号： C07J43/003 ,  C07J13/005 ,  C07J41/0005 ,  C07J71/001

    摘要： The invention relates to new 6, 16-diamino-androstane derviatives of formula (I)
    wherein

    Y is hydrogen or an OAc group,
    Ac is an alkylcarbonyl group having from 1 to 4 carbon atoms in the alkyl moiety,
    A is methylene or a group of formula N-R 1 (wherein
    R 1 is alkyl having from 1 to 4 carbon atoms).
    B is methylene, or a group N-R 1 or N-R 2 , in which R 1 is as defined above and
    R 2 is a -CH 2 -CH 2 -COOR 1 , and
    n is 1 or 2,
    m is 1, 2 or 3,
    and physiologically acceptable diquaternary and monoquaternary salts thereof with C 1-4 alkyl or alkenyl groups.

    Processes for preparing the compounds of formula (I) and compositions containing them are also disclosed. The compounds are potentially valuable as muscle relaxants.

    摘要翻译： 本发明涉及式（I）的新的6,16-二氨基 - 雄甾烷衍生物，其中Y是氢或OAc基团，Ac是烷基部分中具有1至4个碳原子的烷基羰基，A是亚甲基或基团 的式N-R 1（其中R 1是具有1至4个碳原子的烷基）。 B是亚甲基或基团NR 1或NR 2，其中R 1如上所定义且R 2是-CH 2 -CH 2 -COOR 1，且n是1或2，m是1,2或3，并且生理学上 其可接受的具有C 1-4烷基或链烯基的二季和单季盐。 还公开了制备式（I）化合物和含有它们的组合物的方法。 该化合物作为肌肉松弛剂可能是有价值的。

    1,12b-Disubstituted octahydroindolo [2,3-a]-Quinolizine derivatives
    7.
    发明公开
    1,12b-Disubstituted octahydroindolo [2,3-a]-Quinolizine derivatives 失效
    1,12b-二取代的八氢吲哚并[2,3-a] - 奎因嗪衍生物

    公开(公告)号：EP0202774A2

    公开(公告)日：1986-11-26

    申请号：EP86302934.4

    申请日：1986-04-18

    申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

    发明人： Szántay, Csabe ,  Sóti, Ferenc ,  Incze, Maria ,  Balogh, Zsuzsanna ,  Szombathelyi, Zsolt ,  Kárpáti, Egon ,  Kiss, Béla ,  Csomor, Katalin ,  Laszlovszky, Istvan ,  Lapis, Erzsébet ,  Forgács, Lilla ,  Kuthi, Csaba ,  Szporny, László

    IPC分类号： C07D471/14 ,  A61K31/44

    CPC分类号： C07D401/06 ,  C07D209/16 ,  C07D471/14

    摘要： The invention relates to new racemic and optically active 1,12b-disubstituted octahydroindolo[2,3- alquinolizine derivatives of formula (I)
    wherein

    R 1 and R 2 are the same or different and represent hydrogen, halogen, nitro, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or hydroxyl,
    R" and R 5 are the same or different and represent hydrogen, alkyl having from to 6 carbon atoms or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety,
    R 4 is alkyl having from 1 to 6 carbon atoms, aryl or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, and
    R 6 is an electron attracting substituent, and cis and trans isomers and acid addition salts thereof.

    The compounds are pharmaceutically active, in particular they show an outstanding cardiovascular, e.g. selective peripheral vasodilating activity. Some of these compounds are valuable intermediates in the preparation of other, pharmaceutically active compounds.

    摘要翻译： 本发明涉及式（I）的新的外消旋和旋光活性的1,12b-二取代的八氢吲哚并[2,3-喹喔啉衍生物，其中R 1和R 2相同或不同且代表氢，卤素，硝基，具有1至6 碳原子，具有1至6个碳原子的烷氧基或羟基，R“和R5相同或不同，代表氢，烷基部分具有6至6个碳原子的烷基或具有1至6个碳原子的芳烷基，R4是 具有1至6个碳原子的烷基，在烷基部分具有1至6个碳原子的芳基或芳烷基，并且R 6是吸电子取代基，以及其顺式和反式异构体及其酸加成盐。 特别是它们表现出优异的心血管功能，例如选择性的外周血管舒张活性。这些化合物中的一些是制备其它药物活性化合物的有价值的中间体。