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69 条记录 (耗时 0.022 秒)

    Indolo[2,3-a]quinolizines
    21.
    发明授权
    Indolo[2,3-a]quinolizines 失效
    吲哚并[8-2,3-a {9 quinolizines

    公开(公告)号：US4057551A

    公开(公告)日：1977-11-08

    申请号：US614240

    申请日：1975-09-17

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

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

    IPC分类号： C07D471/04 ,  A61K31/437 ,  C07D471/14 ,  C07D471/02 ,  C07D455/02

    CPC分类号： C07D471/14 ,  Y10S514/929

    摘要： New compounds of the general formula (I) ##STR1## wherein R stands for an alkyl group, have been prepared by reducing a compound of the general formula (II) ##STR2## wherein R stands for alkyl, B stands for H.sub.2 O or an X.sup.- anion derived from an acid, and if B is an X.sup.- anion, A represents hydrogen, whereas if B is H.sub.2 O, A represents an electron pair. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.

    摘要翻译： 通式（I）的新化合物其中R代表烷基的化合物是通过还原通式（II）的化合物（II）制备的，其中R代表烷基，B 代表H 2 O或衍生自酸的X阴离子，如果B是X-阴离子，则A表示氢，而如果B是H 2 O，则A表示电子对。 如果需要，可以拆分通式（I）的外消旋化合物，得到相应的旋光异构体。 通式（I）的游离碱可以转化为其药学上可接受的盐，或者盐可以用碱剂处理以产生游离碱。

    Nitrogen-containing polycyclic compounds
    22.
    发明授权
    Nitrogen-containing polycyclic compounds 失效
    含氮多环化合物

    公开(公告)号：US4057550A

    公开(公告)日：1977-11-08

    申请号：US614239

    申请日：1975-09-17

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

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

    IPC分类号： C07D471/06 ,  A61K31/435 ,  A61K31/4375 ,  A61K31/439 ,  A61P9/08 ,  C07D461/00 ,  C07D471/02 ,  C07D455/02

    CPC分类号： C07D461/00 ,  Y10S514/929

    摘要： New compounds of the general formula (I) ##STR1## wherein R.sub.1 stands for alkyl and R.sub.2 stands for carboxy, a functional carboxy derivative or a group convertible into carboxy group or a functional derivative thereof, have been prepared by reducing a compound of the general formula ##STR2## wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- represents an anion derived from an acid, and optionally subjecting the obtained compound to hydrolysis. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.

    摘要翻译： 通式（I）的新化合物其中R1代表烷基，R2代表羧基，官能羧基衍生物或可转化成羧基的基团或其官能衍生物，通过还原化合物 通式（II）其中R 1和R 2各自具有与上述相同的含义，并且X代表由酸衍生的阴离子，并且任选地使得到的化合物进行水解。 如果需要，可以拆分通式（I）的外消旋化合物，得到相应的旋光异构体。 通式（I）的游离碱可以转化为其药学上可接受的盐，或者盐可以用碱剂处理以产生游离碱。

    E-Homo-eburnane derivatives, process for their preparation, and pharmaceutical compositions containing these compounds
    25.
    发明授权
    E-Homo-eburnane derivatives, process for their preparation, and pharmaceutical compositions containing these compounds 失效
    E-Homo-eburnane衍生物，其制备方法和含有这些化合物的药物组合物

    公开(公告)号：US4481204A

    公开(公告)日：1984-11-06

    申请号：US509150

    申请日：1983-06-29

    申请人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Janos Sapi ,  Eva Palosi ,  Egon Karpati ,  Laszlo Szporny

    发明人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Janos Sapi ,  Eva Palosi ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： C07D471/22 ,  A61K31/395 ,  C07D459/00 ,  C07D461/00

    CPC分类号： C07D471/22

    摘要： The invention relates to racemic or optically active E-homo-eburnane derivatives of the formula /I/, ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and acid addition salts thereof.The new compounds are pharmaceutically active, for example their certain representatives, in particular from the cis-series, show antidepressive activity, while others, especially the compounds of the trans-series, are potent anthypoxial agents. The compounds of the formula /I/ and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions.

    摘要翻译： 本发明涉及式/ I /，其中R 1和R 2独立地表示具有1至6个碳原子的烷基的式/ I /，/ IMAGE / I / C的外消旋或光学活性的E-均 - burn烷衍生物及其酸加成盐。 新化合物是药学上活性的，例如它们的特定代表，特别是顺式的化合物显示出抗抑郁活性，而其它代表，特别是反式系列的化合物是有效的抗氧化剂。 因此，式/ I /的化合物及其药学上可接受的酸加成盐可用作药物组合物的活性成分。

    Hexahydroindoloquinolizinium and octahydroindoloquinolizine esters, and method of increasing blood flow in an animal with hydroxyamino-eburnane derivatives
    27.
    发明授权
    Hexahydroindoloquinolizinium and octahydroindoloquinolizine esters, and method of increasing blood flow in an animal with hydroxyamino-eburnane derivatives 失效
    六氢吲哚喹啉鎓和八氢二吲哚喹啉酯，以及用羟基氨基 - 伊本恩衍生物增加动物血流量的方法

    公开(公告)号：US4446139A

    公开(公告)日：1984-05-01

    申请号：US351506

    申请日：1982-02-23

    申请人： Csaba Szantay ,  Lajos Szbao ,  Gyorgy Kalaus ,  Janos Sapi ,  Lajos Dancsi ,  Tibor Keve

    发明人： Csaba Szantay ,  Lajos Szbao ,  Gyorgy Kalaus ,  Janos Sapi ,  Lajos Dancsi ,  Tibor Keve

    IPC分类号： C07D461/00 ,  C07D471/14 ,  A61K31/435 ,  C07D455/00

    CPC分类号： C07D471/14 ,  C07D461/00

    摘要： The invention relates to new hydroxyamino-eburnane derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group, as well as to pharmaceutically acceptable acid addition salts and optically active isomers of these compounds.These new compounds can be applied as peripheral vasodilatating agents or can be converted into other compounds, e.g. vincamine and apovincamine derivatives, of valuable therapeutical effects.The compounds of the general formula (I) are prepared according to the invention by reacting a hexahydro-indoloquinolisinium derivative of the general formula (II), ##STR2## wherein R.sup.2 is as defined above and X stands for an acid residue, with a methylenemalonic acid diester derivative of the general formula (III), ##STR3## wherein R.sup.1 is as defined above, subjecting the resulting product to catalytic hydrogenation, treating the resulting product with an alkali, and reacting the resulting octahydroindoloquinolisine monoester derivative with a nitrosating agent in an acidic medium.

    摘要翻译： 本发明涉及通式（I）的新型羟基氨基 - 伊本烷衍生物，其中R1和R2各自表示C1-6烷基，以及药学上可接受的酸加成盐和旋光异构体 的这些化合物。 这些新化合物可以作为外周血管舒张剂使用，也可以转化为其它化合物，例如 长春胺和氨肽素衍生物，具有宝贵的疗效。 通式（I）的化合物根据本发明通过使通式（II）的六氢 - 吲哚并喹啉鎓衍生物，其中R 2如上定义，X​​代表酸残基， 与通式（III）的亚甲基丙二酸二酯衍生物，其中R1如上所定义，使所得产物进行催化氢化，用碱处理所得产物，并使所得八氢二吲哚并喹啉酮单酯衍生物 在酸性介质中使用亚硝化剂。

    Process for preparation of cytostatic compounds
    28.
    发明授权
    Process for preparation of cytostatic compounds 失效
    细胞生长抑制化合物的制备方法

    公开(公告)号：US4410459A

    公开(公告)日：1983-10-18

    申请号：US293611

    申请日：1981-08-17

    申请人： Lajos Dancsi ,  Tibor Keve ,  Lajos Szabo ,  Katalin Honty ,  Sandor Eckhardt ,  Ivan Hindi ,  Sandor Kerpel-Fronius ,  Gyorgy Fekete ,  Eszter Dezseri ,  Sandor Gorog ,  Tibor Acs ,  Csaba Szantay ,  Zsuzsanna Relle nee Somfai ,  Janos Sugar

    发明人： Lajos Dancsi ,  Tibor Keve ,  Lajos Szabo ,  Katalin Honty ,  Sandor Eckhardt ,  Ivan Hindi ,  Sandor Kerpel-Fronius ,  Gyorgy Fekete ,  Eszter Dezseri ,  Sandor Gorog ,  Tibor Acs ,  Csaba Szantay ,  Zsuzsanna Relle nee Somfai ,  Janos Sugar

    IPC分类号： A61K31/475 ,  A61P35/00 ,  C07D519/04

    CPC分类号： C07D519/04 ,  Y10S514/908

    摘要： The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a -CH.sub.2 -O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl,provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl, R.sup.4 is other than ethyl.These compounds and N-desmethyl-N- ethoxy- methyl -vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula ##STR2## with a large excess of alcohols of the general formulaR"--OH (III)Pharmaceutical compositions containing compounds of the general formula /I/ as active ingredients are also within the scope of invention.

    摘要翻译： 本发明涉及新的细胞生长抑制化合物，其制备方法和含有它们的药物组合物。 更具体地，提供了通式为（I）的新化合物，其中R 4是β-羟基并且R 3是α-乙基; 或R4是氢，R3是β-乙基; R“是具有1至10个碳原子的直链烷基或具有3至10个碳原子的支链烷基，其中与> Na-CH 2 -O-基团连接的碳原子具有伯或 二级构型或具有3至6个碳原子的烯基或炔基，或在烷基部分具有1至3个碳原子的芳烷基; R1是甲氧基，R2是乙酰基，条件是如果R3是α-乙基和R4β-羟基，R4不是乙基。 这些化合物和N-去甲基-N-乙氧基 - 甲基 - 长春花碱可以根据本发明通过将通式为“IMAGE”（II）的化合物的化合物与大量过量的通式R' '-OH（III）含有通式I I化合物作为活性成分的药物组合物也在本发明的范围内。

    N-Desmethyl-N-(allyloxymethyl)-vinblastine and antileukemic and antilymphomic compositions and method of treatment
    29.
    发明授权
    N-Desmethyl-N-(allyloxymethyl)-vinblastine and antileukemic and antilymphomic compositions and method of treatment 失效
    N-去甲基-N-（烯丙氧基甲基） - 长春花碱和抗白血病和抗病毒组合物和治疗方法

    公开(公告)号：US4490378A

    公开(公告)日：1984-12-25

    申请号：US503791

    申请日：1983-06-13

    申请人： Lajos Dancsi ,  Tibor Keve ,  Gyorgy Fekete ,  Eszter Dezseri ,  Sandor Gorog ,  Tibor cs ,  Csaba Szantay ,  Lajos Szabo ,  Katalin Honty ,  Sandor Eckhardt ,  Ivan Hindi ,  Sandor Kerpel-Fronius ,  Zsuzsanna Relle nee Somfa ,  Janos Sugar

    发明人： Lajos Dancsi ,  Tibor Keve ,  Gyorgy Fekete ,  Eszter Dezseri ,  Sandor Gorog ,  Tibor cs ,  Csaba Szantay ,  Lajos Szabo ,  Katalin Honty ,  Sandor Eckhardt ,  Ivan Hindi ,  Sandor Kerpel-Fronius ,  Zsuzsanna Relle nee Somfa ,  Janos Sugar

    IPC分类号： A61K31/475 ,  A61P35/00 ,  C07D519/04

    CPC分类号： C07D519/04 ,  Y10S514/908

    摘要： The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a --CH.sub.2 --O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl, provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl,R.sup.4 is other than ethyl.These compounds and N-desmethyl-N-(ethoxymethyl)-vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula ##STR2## with a large excess of alcohols of the general formulaR"--OH [III]Pharmaceutical compositions containing compounds of the general formula [I] as active ingredients are also within the scope of invention.

    摘要翻译： 本发明涉及新的细胞生长抑制化合物，其制备方法和含有它们的药物组合物。 更具体地，提供了通式为“IMAGE”/ I /的新化合物，其中R 4是β-羟基和R 3是α-乙基; 或R4是氢，R3是β-乙基; R“是具有1至10个碳原子的直链烷基或具有3至10个碳原子的支链烷基，其中与> Na-CH 2 -O-基团连接的碳原子具有伯或 二级构型或具有3至6个碳原子的烯基或炔基，或在烷基部分具有1至3个碳原子的芳烷基; R1是甲氧基，R2是乙酰基，条件是如果R3是α-乙基和R4β-羟基，R4不是乙基。 这些化合物和N-去甲基-N-（乙氧基甲基） - 长春花碱可以根据本发明通过将通式为“IMAGE”/ II /的化合物的化合物与大量过量的通式R' '-OH [III]含有通式[I]化合物作为活性成分的药物组合物也在本发明的范围内。

    Nitrogen-containing polycyclic compounds and a process for the preparation thereof
    30.
    发明授权
    Nitrogen-containing polycyclic compounds and a process for the preparation thereof 失效
    含氮多环化合物及其制备方法

    公开(公告)号：US4054571A

    公开(公告)日：1977-10-18

    申请号：US614151

    申请日：1975-09-17

    申请人： Csaba Szantay ,  Lajor Szabo ,  Gyorgy Kalaus ,  Egon Karpati ,  Laszlo Szporny

    发明人： Csaba Szantay ,  Lajor Szabo ,  Gyorgy Kalaus ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： C07D471/06 ,  A61K31/4375 ,  A61K31/4745 ,  C07D461/00 ,  C07D471/04

    CPC分类号： C07D461/00

    摘要： The invention relates to new eburnamenine derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for an alkyl group,R.sub.2 stands for a carboxy group, a functional carboxy derivative (preferably an ester group) or a group convertable into carboxy group or a functional derivative thereof (preferably cyano group), andX.sup.- is an anion derived from an acid,And the corresponding free bases.These compounds are valuable intermediates of the preparation of eburnamenine derivatives with advantageous therapeutical effects.The above compounds are prepared as follows: a compound of the general formula (II), ##STR2## wherein R.sub.1 has the same meanings as defined above, is reacted with a compound of the general formula (III), ##STR3## wherein R.sub.2 has the same meanings as defined above and Y is halogen, and, if desired, a thus-obtained compound of the general formula (I), wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- is a halide ion, is reacted with an acid, and/or, if desired, a compound of the general formula (I), wherein R.sub.1 and X.sup.- each have the same meanings as defined above and R.sub.2 is cyano or an ester group, is subjected to hydrolysis, and/or, if desired, a compound of the general formula (I), wherein R.sub.1, R.sub.2 and X.sup.- each have the same meanings as defined above, is treated with a base.

    摘要翻译： 本发明涉及通式（I），其中R1代表烷基，R2代表羧基，官能羧基衍生物（优选酯基）或可转化基团的新颖的本本母胺衍生物 羧基或其功能性衍生物（优选氰基），X是衍生自酸的阴离子，和相应的无碱基。