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    Process for the preparation of nitrogen-bridgehead condensed pyrimidine compounds, and pharmaceutical compositions containing them
    3.
    发明授权
    Process for the preparation of nitrogen-bridgehead condensed pyrimidine compounds, and pharmaceutical compositions containing them 失效
    氮桥头浓缩嘧啶化合物的制备方法和含有它们的药物组合物

    公开(公告)号：US4452982A

    公开(公告)日：1984-06-05

    申请号：US148238

    申请日：1980-05-09

    申请人： Istvan Hermecz ,  Tibor Breining ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Jozsef Kokosi

    发明人： Istvan Hermecz ,  Tibor Breining ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Jozsef Kokosi

    IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P11/00 ,  A61P37/08 ,  C07D471/04 ,  C07D239/70

    CPC分类号： C07D471/04

    摘要： A process is disclosed for the preparation of compounds of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or lower alkyl;R.sup.3 is carboxy, lower alkoxycarbonyl, carbamoyl, carbamoyl substituted by one or two lower alkyl groups, or cyano;R.sup.4 is hydrogen, lower alkyl, phenyl, naphthyl, phenyl or naphthyl substituted by at least one fluoro, chloro, bromo, iodo, lower alkyl, lower alkoxy, hydroxy, carboxy, or phenyl, pyridyl or tetrazolyl; andR.sup.5 is hydrogen or lower alkyl; or a pharmaceutically acceptable salt, hydrate, stereoisomer, optically active isomer, geometric isomer, or tautomer thereof, which comprises the step of aminating a racemic or optically active compound of the formula (II) ##STR2## wherein X is halogen with a compound of the formula (III) ##STR3## or a pharmaceutically acceptable acid addition salt thereof. The compound of formula (II) possess antiallergic, especially antiasthma, activity.

    摘要翻译： 公开了制备式（I）化合物的方法，其中R 1和R 2各自为氢或低级烷基; R3是羧基，低级烷氧基羰基，氨基甲酰基，被一个或两个低级烷基取代的氨基甲酰基，或氰基; R4是氢，低级烷基，苯基，萘基，苯基或被至少一个氟，氯，溴，碘，低级烷基，低级烷氧基，羟基，羧基或苯基，吡啶基或四唑基取代的萘基。 R5是氢或低级烷基; 或其药学上可接受的盐，水合物，立体异构体，旋光异构体，几何异构体或其互变异构体，其包括将式（II）的外消旋或旋光活性化合物胺化的步骤，其中X是卤素， 式（III）或其药学上可接受的酸加成盐。 式（II）化合物具有抗过敏，特别是抗哮喘作用。

    6-Hydrazono-pyrido[2,1-b] quinazoline-11 ones
    7.
    发明授权
    6-Hydrazono-pyrido[2,1-b] quinazoline-11 ones 失效
    6-肼基 - 吡啶并[2,1-b]喹唑啉-11

    公开(公告)号：US4395549A

    公开(公告)日：1983-07-26

    申请号：US308038

    申请日：1981-10-02

    申请人： Istvan Hermecz ,  Jozsef Kokosi ,  Agnes Horvath ,  Zoltan Meszaros ,  Gyorgy Szasz ,  Tibor Breining ,  Lelle Vasvari nee Debreczy

    发明人： Istvan Hermecz ,  Jozsef Kokosi ,  Agnes Horvath ,  Zoltan Meszaros ,  Gyorgy Szasz ,  Tibor Breining ,  Lelle Vasvari nee Debreczy

    IPC分类号： C07D487/04 ,  C07D487/14

    CPC分类号： C07D487/04

    摘要： Intermediates useful in the preparation of Rutecarpine and Rutecarpine derivatives are disclosed as well as a process for the preparation of said intermediates having the following formula: ##STR1## wherein R, R.sup.1 and R.sup.2 are the same or different and stand for hydrogen, halogen, nitro, carboxy, nitrile, alkoxy containing 1 to 4 carbon atoms, alkoxycarbonyl containing 1 to 4 carbon atoms in the alkoxy group, alkyl containing 1 to 4 carbon atoms, amino or hydroxy or R and R.sup.1 together stand for methylenedioxy, R.sup.2 stands for hydrogen, R.sup.3 represents hydrogen or alkyl containing 1 to 4 carbon atoms, R.sup.4 stands for phenyl, phenyl substituted by 1 to 3 same or different substituents selected from the group of halogen(s), alkyl, and alkoxy containing 1 to 4 carbon atoms, phenyloxy, hydroxy, nitro, amino, cyano, carboxy, alkoxycarbonyl having 1 to 4 carbon atoms, alkanoyl having 1 to 4 carbon atoms, methylenedioxy, trifluoromethyl, phenyl and dialkylamino having 1 to 4 carbon atoms in the alkyl part or naphthyl and the dotted line indicated an optional double bond. Also pharmaceutically acceptable acid addition and quaternary ammonium salts are disclosed.

    摘要翻译： 公开了用于制备罗非鱼和芦丁类衍生物的中间体以及制备具有下式的所述中间体的方法：其中R，R 1和R 2相同或不同并代表氢， 卤素，硝基，羧基，腈，含有1至4个碳原子的烷氧基，烷氧基中含有1至4个碳原子的烷氧基羰基，含1至4个碳原子的烷基，氨基或羟基或R和R 1一起代表亚甲二氧基， 对于氢，R 3表示氢或含有1至4个碳原子的烷基，R 4代表苯基，被1至3个相同或不同的取代基取代的苯基，所述取代基选自含1至4个碳原子的卤素，烷基和烷氧基 ，苯氧基，羟基，硝基，氨基，氰基，羧基，具有1至4个碳原子的烷氧基羰基，具有1至4个碳原子的烷酰基，亚甲二氧基，三氟甲基，苯基和在烷基中具有1至4个碳原子的二烷基氨基 部分或萘基，虚线表示任选的双键。 还公开了药学上可接受的酸加成盐和季铵盐。

    Nitrogen bridgehead compounds having anti-allergic effect
    8.
    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 9-hydrazono-6,7,8,9-tetrahydro-4H-pyro[1,2-a]pyrimidine-4-one compounds, the salts and hydrates thereof
    9.
    发明授权
    Process for the preparation of 9-hydrazono-6,7,8,9-tetrahydro-4H-pyro[1,2-a]pyrimidine-4-one compounds, the salts and hydrates thereof 失效
    制备9-亚肼基-6,7,8,9-四氢-4H-焦[1,2-a]嘧啶-4-酮化合物的方法，其盐和水合物

    公开(公告)号：US4456752A

    公开(公告)日：1984-06-26

    申请号：US327689

    申请日：1981-12-04

    申请人： Istvan Hermecz ,  Tibor Breining ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Jozsef Kokosi

    发明人： Istvan Hermecz ,  Tibor Breining ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Jozsef Kokosi

    IPC分类号： A61K31/505 ,  A61P11/00 ,  A61P37/08 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： A process for the preparation of nitrogen bridgehead condensed pyrimidine compounds of the general formula ##STR1## [wherein R represents hydrogen or lower alkyl;R.sup.1 represents hydrogen, lower alkyl, carboxy or a derivative thereof or styryl;R.sup.2 represents hydrogen or optionally substituted lower alkyl;R.sup.3 represents hydrogen, optionally substituted lower alkyl, aryl, aralkyl, halogen, carboxy or a derivative thereof, the group --(CH.sub.2).sub.m --COOH (in which m is the integer 1, 2 or 3) or a carboxy derivative thereof, formyl, lower alkanoyl or a condensed thereof;R.sup.4 represents hydrogen, optionally substituted alkyl, aryl optionally substituted by one or more substituents, optionally substituted aralkyl, a heterocyclic group optionally substituted by one or more substituents, the group (CH.sub.2).sub.m --Het (in which m is the integer 1, 2 or 3; Het is an optionally substituted heterocyclic group);R.sup.5 represents hydrogen, C.sub.1-6 alkyl, aryl optionally substituted by one or more substituents, formyl, lower alkanoyl, optionally substituted aroyl or heteroaryl; orR.sup.4 and R.sup.5 together with the nitrogen therebetween represent an optionally substituted mono- or bicyclic heterocyclic ring optionally containing further heteroatom]and pharmaceutically acceptable salts, hydrates, stereoisomers, optically active isomers, geometrical isomers and tautomers thereof.

    摘要翻译： 制备通式为“IMAGE”I的氮桥头浓缩嘧啶化合物的方法[其中R表示氢或低级烷基; R1代表氢，低级烷基，羧基或其衍生物或苯乙烯基; R 2表示氢或任选取代的低级烷基; R 3表示氢，任选取代的低级烷基，芳基，芳烷基，卤素，羧基或其衍生物，基团 - （CH 2）m -COOH（其中m是整数1,2或3）或其羧基衍生物， ，低级烷酰基或其缩合物; R 4表示氢，任选取代的烷基，任选被一个或多个取代基取代的芳基，任选取代的芳烷基，任选被一个或多个取代基取代的杂环基，基团（CH 2）m -Het（其中m是整数1,2 或3; Het是任选取代的杂环基）; R 5表示氢，C 1-6烷基，任选被一个或多个取代基取代的芳基，甲酰基，低级烷酰基，任选取代的芳酰基或杂芳基; 或R4和R5以及它们之间的氮代表任选地被取代的单环或双环杂环，任选地含有另外的杂原子]及其药学上可接受的盐，水合物，立体异构体，光学活性异构体，几何异构体和互变异构体。