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    Antiphlogistic and anticoagulant condensed pyrimidine derivatives
    5.
    发明授权
    Antiphlogistic and anticoagulant condensed pyrimidine derivatives 失效
    消炎和抗凝血嘧啶衍生物

    公开(公告)号：US4460771A

    公开(公告)日：1984-07-17

    申请号：US742464

    申请日：1976-11-17

    申请人： Zoltan Meszaros ,  Jozsef Knoll ,  Peter Szentmiklosi ,  Istvan Hermes ,  Agnes Horvath ,  Sandor Virag ,  Lelle Vasvari nee Debreczy ,  Agoston David

    发明人： Zoltan Meszaros ,  Jozsef Knoll ,  Peter Szentmiklosi ,  Istvan Hermes ,  Agnes Horvath ,  Sandor Virag ,  Lelle Vasvari nee Debreczy ,  Agoston David

    IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P7/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： New optionally racemic or optically active pyrimido(1,2a) heterocyclic compounds of the formula ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is an alkyl group containing one to six carbon atoms,R.sup.1 is hydrogen, alkyl containing one to six carbon atoms,R.sup.2 is hydrogen, alkyl containing one to six carbon atoms, optionally substituted amino, optionally substituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sup.1 and R.sup.2 together form a --(CH.dbd.CH).sub.2 -- group attached to the two adjacent carbon atoms of the ring A and the broken line represents a chemical bond,R.sup.3 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl or optionally substituted hydroxy,R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl orR.sup.3 and R.sup.4 together with the nitrogen can form an optionally substituted five-, six- or seven-membered ring, which can contain a further heteroatom or heteroatoms,R.sup.5 is oxygen or an optionally substituted imino group are disclosed as well as a process for the preparation thereof.

    摘要翻译： 新的任选的外消旋或光学活性嘧啶（1,2a）杂环化合物，其中m为0,1或2，n为0,1或2，R为含有1至6个碳原子的烷基，R 1为 是氢，含有1至6个碳原子的烷基，R 2是氢，含1至6个碳原子的烷基，任选取代的氨基，任选取代的羟基，羧基或衍生自羧酸的基团或R 1和R 2一起形成 - （CH = CH）连接到环A的两个相邻碳原子上的2-基团，虚线表示化学键，R 3是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基， 任选取代的酰基或任选取代的羟基，R 4是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基，选择 可以将氮取代的酰基或R3和R4与氮一起形成任选取代的五元，六元或七元环，其可以含有另外的杂原子或杂原子，R5是氧或任选取代的亚氨基， 其制备方法。

    Nitrogen bridgehead compounds having anti-allergic effect
    6.
    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。

    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。