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150 条记录 (耗时 0.026 秒)

    2,3-thiomorpholinedione-2-oxime derivatives and pharmaceutical compositions containing them
    111.
    发明授权
    2,3-thiomorpholinedione-2-oxime derivatives and pharmaceutical compositions containing them 失效
    2,3-苯硫酚-2-氧化物衍生物和含有它们的药物组合物

    公开(公告)号：US5106846A

    公开(公告)日：1992-04-21

    申请号：US477999

    申请日：1990-07-10

    申请人： Istvan Szabadkai ,  Kalman Harsanyi ,  Agnes Lampert ,  Gyorgy Domany ,  Bela Hegedus ,  Elemer Ezer ,  Judit Matuz ,  Katalin Saghy ,  Laszlo Szporny ,  Gyorgy Hajos ,  Krisztina Szekely

    发明人： Istvan Szabadkai ,  Kalman Harsanyi ,  Agnes Lampert ,  Gyorgy Domany ,  Bela Hegedus ,  Elemer Ezer ,  Judit Matuz ,  Katalin Saghy ,  Laszlo Szporny ,  Gyorgy Hajos ,  Krisztina Szekely

    IPC分类号： A61K31/54 ,  A61P1/04 ,  C07D279/12

    CPC分类号： C07D279/12

    摘要： The present invention relates to compounds of the general formula (I), ##STR1## wherein R.sub.1 stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or nitro group;R.sub.2 means a C.sub.1-7 alkyl group optionally substituted by: a hydroxyl or oxo group; or an ester group containing 1 to 4 carbon atoms in the alkoxy moiety; or a C.sub.1-4 alkoxy, cyano, amino, C.sub.1-4 alkylamino, or dialkylamino group; or an acyl group containing 1 to 7 carbon atoms in the alkyl moiety; orR.sub.2 means an aryl-C.sub.1-7 alkyl group optionally bearing the substituents defined above for R.sub.2 in the alkyl chain and optionally substituted by halogen, nitro, C.sub.1-4 alkyl or alkoxy group in the benzene ring; orR.sub.2 represents an allyl, phenylallyl or phenylsulfonyl group, both latter groups optionally being substituted by halogen or a C.sub.1-4 alkyl group in the benzene ring; orR.sub.2 stands for a carbamoyl group substituted by one or two C.sub.1-4 alkyl group(s) or phenyl group on the nitrogen atom.The compounds according to the invention show a cytoprotective and acid secretion-inhibiting action and are effective against gastric and duodenal ulcers.

    摘要翻译： PCT No.PCT / HU88 / 00080 Sec。 371日期1990年7月10日 102（e）日期1990年7月10日PCT提交1988年12月13日PCT公布。 出版物WO89 / 05805 日本时间1989年6月29日。本发明涉及通式（I），其中R1代表氢，卤素，C1-4烷基，C1-4烷氧基或硝基的通式（I）的化合物。 R 2表示任选被羟基或氧代基取代的C 1-7烷基; 或在烷氧基部分含有1至4个碳原子的酯基; 或C 1-4烷氧基，氰基，氨基，C 1-4烷基氨基或二烷基氨基; 或在烷基部分含有1至7个碳原子的酰基; 或R 2表示任选具有上述对烷基链中的R 2定义并且任选被苯环中的卤素，硝基，C 1-4烷基或烷氧基取代的取代基的芳基-C 1-7烷基; 或R 2表示烯丙基，苯基烯丙基或苯基磺酰基，后两个基团任选被苯环中的卤素或C 1-4烷基取代; 或R 2表示被一个或两个C 1-4烷基或氮原子上的苯基取代的氨基甲酰基。 根据本发明的化合物显示出细胞保护和酸分泌抑制作用，并且对胃和十二指肠溃疡有效。

    3,7-Diazabicyclo [3.3.1] nonanes having anti-arrhythmic activity
    114.
    发明授权
    3,7-Diazabicyclo [3.3.1] nonanes having anti-arrhythmic activity 失效
    具有抗心律不齐活性的3,7-二氮杂双环[3.3.1]壬烷

    公开(公告)号：US4451473A

    公开(公告)日：1984-05-29

    申请号：US398801

    申请日：1982-07-16

    申请人： Karoly Nador ,  Gabor Kraiss ,  Katalin Sinko ,  Margit Paroczai ,  Egon Karpati ,  Laszlo Szporny

    发明人： Karoly Nador ,  Gabor Kraiss ,  Katalin Sinko ,  Margit Paroczai ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： A61K31/395 ,  A61K31/435 ,  A61K31/48 ,  A61K31/4995 ,  A61P9/06 ,  C07D451/14 ,  C07D471/08 ,  A61K31/44

    CPC分类号： C07D471/08 ,  Y10S514/821

    摘要： New bicyclic compounds of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent a C.sub.1-6 alkyl group, andR.sup.3 is an etherified hydroxy group of the formula --CR.sup.4, wherein R.sup.4 is benzyl group, benzhydryl group or a phenyl group bearing optionally a phenyl or a trihalomethyl substituent or one or more halogen substituent(s), orR.sup.3 is an esterified hydroxy group of the formula --OCO--R.sup.5, which representsa phenyl-(C.sub.1-5 alkyl)-carbonyloxy group,a cinnamoyloxy group having optionally a halogen or one or more C.sub.1-4 alkoxy substituent(s),a benzoyloxy group having optionally a C.sub.1-4 alkyl, phenyl or trihalomethyl substituent or one or more C.sub.1-4 alkoxy substituent(s), one or more halo substituent(s) and/or nitro substituent,a benzyloyloxy group,a xanthene-9-carbonyloxy group,an optionally substituted naphthoyloxy group, oran acyloxy group derived from a five- or six-membered heterocyclic carboxylic acid bearing optionally a halo substituent on the ring,are prepared by etherifying or esterifying a bicyclic compound of the general formula (II), ##STR2## wherein R.sup.1 and R.sup.2 are as defined above. The new compounds according to the invention possess anti-arrhythmic effects and can be applied to advantage in the therapy of cardiac rhythm disorders.

    摘要翻译： 通式（I）的新的双环化合物，其中R 1和R 2各自表示C 1-6烷基，R 3是式-CR 4的醚化羟基，其中R 4是苄基，二苯甲基 基团或任选带有苯基或三卤甲基取代基或一个或多个卤素取代基的苯基，或R3是式-OCO-R5的酯化羟基，其代表苯基 - （C 1-5烷基） - 具有任选卤素或一个或多个C 1-4烷氧基取代基的肉桂酰氧基，任选具有C 1-4烷基的苯甲酰氧基，苯基或三卤甲基取代基或一个或多个C 1-4烷氧基取代基， ，一个或多个卤素取代基和/或硝基取代基，苯甲酰氧基，呫吨-9-羰氧基，任选取代的萘氧基或衍生自五元或六元杂环羧酸的酰氧基 任选地，环上的卤素取代基通过醚化制备 或酯化通式（II）的双环化合物，其中R 1和R 2如上所定义。 根据本发明的新化合物具有抗心律失常作用，可用于治疗心律失常的优点。

    Nitrogen-containing polycyclic compounds and a process for the preparation thereof
    118.
    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。