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52 条记录 (耗时 0.037 秒)

    2-Azabicyclo(2.2.2)octane derivatives and their use as immunosuppressive agents
    5.
    发明授权
    2-Azabicyclo(2.2.2)octane derivatives and their use as immunosuppressive agents 失效
    2-氨基双环（2.2.2）辛烷衍生物及其作为免疫抑制剂的用途

    公开(公告)号：US4563464A

    公开(公告)日：1986-01-07

    申请号：US625069

    申请日：1984-06-27

    申请人： Elemer Ezer ,  Laszlo Szporny ,  Gyorgy Hajos ,  Csaba Szantay ,  Tibor Keve ,  Gyorgy Fekete ,  Gabor Megyeri ,  Tibor Acs ,  Hedvig Bolcskei

    发明人： Elemer Ezer ,  Laszlo Szporny ,  Gyorgy Hajos ,  Csaba Szantay ,  Tibor Keve ,  Gyorgy Fekete ,  Gabor Megyeri ,  Tibor Acs ,  Hedvig Bolcskei

    IPC分类号： A61K31/435 ,  A61P1/04 ,  A61P9/08 ,  A61P25/08 ,  A61P37/06 ,  C07D211/82 ,  C07D453/06 ,  C07D491/18 ,  A61K31/445 ,  C07D221/22

    CPC分类号： C07D211/82 ,  C07D453/06

    摘要： The invention relates to new 2-azabicyclo[2.2.2]octane derivatives of the formula (I), ##STR1## wherein A is hydrogen, alkoxycarbonyl having from one to 4 carbon atoms in the alkoxy group, phenylalkoxycarbonyl having from one to 4 carbon atoms in the alkoxy moiety, alkyl having from one to 6 carbon atoms, aralkyl containing from one to 4 carbon atoms in the alkyl moiety or substituted acyl,R.sub.1 is hydrogen or alkyl having from one to 4 carbon atoms,Z is hydrogen or halogen,X is hydrogen or halogen,Y is hydrogen, orX and Y together represent a C--C bond,W is alkoxycarbonyl having from one to 4 carbon atoms in the alkoxy moiety, cyano, carboxamido or haloformyl, orif X stands for halogen, X and Y together represent a ##STR2## group. According to another aspect of the invention there is provided a process for the preparation of the above compounds, which are pharmaceutically active, in particular, possess valuable anticonvulsive, vasodilating or gastric acid secretion inhibiting properties. Pharmaceutical compositions containing compounds of the formula (I) are also within the scope of the invention.

    摘要翻译： 本发明涉及式（I）的新的2-氮杂双环[2.2.2]辛烷衍生物，其中A是氢，烷氧基中具有1至4个碳原子的烷氧基羰基，具有1个 在烷氧基部分中具有4个碳原子，具有1至6个碳原子的烷基，在烷基部分含有1至4个碳原子的芳烷基或取代的酰基，R 1是氢或具有1至4个碳原子的烷基，Z是氢 或卤素，X是氢或卤素，Y是氢，或X和Y一起代表CC键，W是在烷氧基部分具有1至4个碳原子的烷氧基羰基，氰基，甲酰氨基或卤代甲酰基，或者如果X代表卤素 ，X和Y一起表示组。 根据本发明的另一方面，提供了一种制备上述化合物的方法，其具有药学活性，特别是具有有价值的抗惊厥，血管舒张或胃酸分泌抑制性质。 含有式（I）化合物的药物组合物也在本发明的范围内。

    2,3-Dihydro-7-chlorothiazolo[3,2-a]benzimidazole and salt
    8.
    发明授权
    2,3-Dihydro-7-chlorothiazolo[3,2-a]benzimidazole and salt 失效
    2,3-二氢-7-氯噻唑并[8 3,2-a {9苯并咪唑和盐

    公开(公告)号：US4017507A

    公开(公告)日：1977-04-12

    申请号：US637978

    申请日：1975-12-05

    申请人： Kalman Hideg ,  Olga Hankovszky ,  Eva Palosi ,  Gyorgy Hajos ,  Laszlo Szporny

    发明人： Kalman Hideg ,  Olga Hankovszky ,  Eva Palosi ,  Gyorgy Hajos ,  Laszlo Szporny

    IPC分类号： C07D513/04

    CPC分类号： C07D513/04

    摘要： New tricyclic fused imidazole derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##STR2## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a=C-- group, orA stands for a group of the general formula (III), ##STR3## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##STR4## wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##STR5## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(ch.sub.2).sub.m --X VI.in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen. The reaction is carried out optionally in the presence of a base. The compounds of the general formula (I) can be converted into their acid addition salts.The compounds of the general formula (I) as well as their acid addition salts exert antipyretic and antiphlogistic activities, inhibit the reproduction of viruses, and exert a protecting effect against albumine shock.

    摘要翻译： 通式（I）的新型三环稠合咪唑衍生物，其中R1代表氢或羟基，N等于零或一，M等于零，一或二，A代表一个基团 的通式（II），其中R 2表示氢或羟基，R 3表示氢或氨基，或Q和Z各自代表氮或a = C-基团，或A表示一个 通式（III），其中R 4和R 5各自代表氢，甲基，氯或硝基，通过反应通用化合物（IV）化合物（IV）制备其中A和n各自 具有与上述定义相同的含有通式（Ⅴ）的化合物，其中X代表卤素，R6代表氢，R7代表通式（Ⅵ）的基团， （CH2）mX VI。

    Tricyclic imidazole derivatives
    9.
    发明授权
    Tricyclic imidazole derivatives 失效
    三环咪唑衍生物

    公开(公告)号：US3932395A

    公开(公告)日：1976-01-13

    申请号：US473184

    申请日：1974-05-24

    申请人： Kalman Hideg ,  Olga Hankovszky ,  Eva Palosi ,  Gyorgy Hajos ,  Laszlo Szporny

    发明人： Kalman Hideg ,  Olga Hankovszky ,  Eva Palosi ,  Gyorgy Hajos ,  Laszlo Szporny

    IPC分类号： C07D513/16 ,  C07D513/04 ,  C07D513/14 ,  C07D279/08 ,  C07D279/14

    CPC分类号： C07D513/04 ,  C07D513/14 ,  Y10S514/916

    摘要： New tricyclic fused imidazole derivatives of the general formula (I), ##SPC1##whereinR.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##EQU1## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a =C-- group, orA stands for a group of the general formula (III), ##EQU2## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##SPC2##wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##EQU3## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(CH.sub.2).sub.m --X (VI)in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen. The reaction is carried out optionally in the presence of a base. The compounds of the general formula (I) can be converted into their acid addition salts.The compounds of the general formula (I) as well as their acid addition salts exert antipyretic and antiphlogistic activities, inhibit the reproduction of viruses, and exert a protecting effect against albumine shock.

    摘要翻译： 新的通式（I）的三环稠合咪唑衍生物，其中R1代表氢或羟基，N等于零或一，M等于零，一或二，A代表通式（II ），-C = QC = Z- |（II）R2R3其中R2表示氢或羟基，R3表示氢或氨基，或Q和Z各自代表氮或a = C-基团，或A表示 通式（III）-CH = C-C = CH- |（III）R4R5其中R4和R5各自表示氢，甲基，氯或硝基，通过反应通用化合物（IV）的化合物制备， 其中A和n各自具有与上述相同的含义，与通式（V）的化合物，X-CH 2 -CH-CH 2 ||（V）R 6 R 7，其中X代表卤素，R6代表氢，R7 代表通式（VI）， - （CH 2）m X（VI）的基团，其中m和X各自具有与上述相同的含义，或者R6和R7一起代表氧。 任选地在碱的存在下进行反应。 通式（I）的化合物可以转化成它们的酸加成盐。