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    Nitrogen bridgehead compounds having anti-allergic effect
    2.
    发明授权
    Nitrogen bridgehead compounds having anti-allergic effect 失效
    具有抗过敏作用的氮桥头头合成物

    公开(公告)号：US4461769A

    公开(公告)日：1984-07-24

    申请号：US76811

    申请日：1979-09-19

    申请人： Istvan Hermecz ,  Zoltan Meszaros ,  Tibor Breining ,  Sandor Virag ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Gabor Nagy ,  Attila Mandi ,  Tamas Szucs ,  Istvan Bitter ,  Gyula Sebestyen

    发明人： Istvan Hermecz ,  Zoltan Meszaros ,  Tibor Breining ,  Sandor Virag ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Gabor Nagy ,  Attila Mandi ,  Tamas Szucs ,  Istvan Bitter ,  Gyula Sebestyen

    IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  A61P29/00 ,  A61P31/04 ,  A61P37/08 ,  A61P43/00 ,  C07D471/04

    CPC分类号： C07D471/04 ,  Y10S514/826

    摘要： Compounds of the formula I ##STR1## or pharmaceutically acceptable salts, hydrates, stereoisomers, optically active isomers, geometrical isomers or tautomeric forms thereof are disclosedwhereinR is hydrogen or lower alkylR.sup.1 is hydrogen, lower alkyl, styryl, or a carboxylic acid; orR and R.sup.1 together form a group of the formula --(CH.dbd.CH).sub.2 -- and in this case the broken line represents a further C--C bond, while in all other cases there is a single bond between positions 6 and 7;R.sup.2 is hydrogen, lower alkyl or hydroxy;R.sup.3 is hydrogen, lower alkyl, aryl, lower alkanoyl, carboxyl or a carboxyl acid derivative or a group of the formula --(CH.sub.2)m--COOH or a derivative thereof formed in the carboxylic group;n=1-3;R.sup.4 is hydrogen, lower alkyl which can be substituted by hydroxy or carboxy; trifluoromethyl, substituted or unsubstituted aryl, phenyl-lower alkyl or substituted or an unsubstituted heterocyclic group;R.sup.5 is hydrogen, lower alkanoyl, substituted or unsubstituted benzoyl or heteroaryl; orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidino, pyrrolidino or morpholino ring; orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a group of the formula ##STR2## wherein R.sup.6 is hydrogen and R.sup.7 is substituted or unsubstituted phenyl; andZ is oxygen. The new compounds are useful for treating asthma.

    摘要翻译： 公开了式I的化合物或其药学上可接受的盐，水合物，立体异构体，光学活性异构体，几何异构体或互变异构体，其中R是氢或低级烷基R 1是氢，低级烷基，苯乙烯基或羧酸; 或R和R 1一起形成式 - （CH = CH）2 - 的基团，在这种情况下，虚线代表另外的C-C键，而在所有其它情况下，位置6和7之间存在单键; R2是氢，低级烷基或羟基; R3是在羧基中形成的氢，低级烷基，芳基，低级烷酰基，羧基或羧基酸衍生物或式 - （CH2）m-COOH或其衍生物的基团; n = 1-3; R4是氢，可被羟基或羧基取代的低级烷基; 三氟甲基，取代或未取代的芳基，苯基 - 低级烷基或取代或未取代的杂环基; R5是氢，低级烷酰基，取代或未取代的苯甲酰基或杂芳基; 或R4和R5与相邻的氮原子一起形成哌啶子基，吡咯烷子基或吗啉代环; 或R 4和R 5与相邻的氮原子一起形成下式的基团：其中R6是氢，R7是取代或未取代的苯基; Z是氧。 新化合物可用于治疗哮喘。

    Process for the preparation of substituted acyl ureas
    5.
    发明授权
    Process for the preparation of substituted acyl ureas 失效
    制备取代酰基脲的方法

    公开(公告)号：US4355178A

    公开(公告)日：1982-10-19

    申请号：US198050

    申请日：1980-10-17

    申请人： Laszio Toke ,  Istvan Bitter ,  Eva Karpati nee Adam ,  Todor Pfliegel

    发明人： Laszio Toke ,  Istvan Bitter ,  Eva Karpati nee Adam ,  Todor Pfliegel

    IPC分类号： A01N47/34 ,  C07C273/18 ,  C07C275/54 ,  C07C127/22

    CPC分类号： C07C273/1854 ,  A01N47/34

    摘要： The invention relates to a process for the preparation of acyl ureas of formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same of different and each is halogen atom, preferably fluorine or chlorine atom, andR.sub.3 is a substituted aryl group.The compounds of the invention can be prepared by reacting an urea of formula (II):R.sub.3 NHCONH.sub.2 (II)wherein R.sub.3 is as defined above, with an acid chloride of formula (III): ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, in an inert organic solvent at a temperature of from 20.degree. C. to 100.degree. C.

    摘要翻译： 本发明涉及一种制备式（I）的酰基脲的方法，其中R 1和R 2相同，各自为卤素原子，优选氟或氯原子，R 3为取代的芳基 组。 本发明的化合物可以通过使式（II）的脲：R3NHCONH2（II）（其中R3如上定义）与式（III）的酰氯反应制备：其中R1和R2是 如上所述，在惰性有机溶剂中，温度为20℃至100℃。

    Process for the preparation of polyhalogenphenyl carbamates
    8.
    发明授权
    Process for the preparation of polyhalogenphenyl carbamates 失效
    制备多卤代苯基氨基甲酸酯的方法

    公开(公告)号：US4347377A

    公开(公告)日：1982-08-31

    申请号：US188966

    申请日：1980-09-19

    申请人： Istvan Bitter ,  Rudolf Soos ,  Geza Toth ,  Laszlo Toke ,  Gabor Szabo

    发明人： Istvan Bitter ,  Rudolf Soos ,  Geza Toth ,  Laszlo Toke ,  Gabor Szabo

    IPC分类号： C07C271/08 ,  C07C67/00 ,  C07C239/00 ,  C07C257/08 ,  C07C271/06 ,  C07C125/067

    CPC分类号： C07C271/06

    摘要： The invention concerns a new process for the preparation of polyhalogenphenyl carbamates of the formula (I)R.sup.2 -OCONHR.sup.1 (I)whereinR.sup.1 is alkyl, aralkyl or aryl, where the aromatic rings may optionally be substituted; andR.sup.2 is phenyl substituted with three, four or five halogens, through intermediates of the formula (IV)(R.sup.2 --O).sub.2 C.dbd.NR.sup.1 (IV)wherein R.sup.1 and R.sup.2 are as defined above.The compounds of the formula (I) are valuable acylating agents. The intermediates of the formula (IV) are new compounds, which are also encompassed by the invention.

    摘要翻译： 本发明涉及一种制备式（I）的多卤代苯基氨基甲酸酯的新方法，其中R 1为烷基，芳烷基或芳基，其中芳环可任选被取代; R2为通过式（IV）中间体（R2-O）2C = NR1（Ⅳ）取代的苯基，其中R1和R2如上定义。 式（I）的化合物是有价值的酰化剂。 式（IV）的中间体是新化合物，其也包括在本发明中。