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1. 发明授权

US4260612A Antiallergic nitrogen bridge-head compounds 失效
标题翻译：抗过敏氮桥头化合物
公开(公告)号：US4260612A
公开(公告)日：1981-04-07
申请号：US967957
申请日：1978-12-11
申请人： Istvan Hermecz , Zoltan Meszaros , Tibor Breining , Sandor Virag , Lelle Vasvari nee Debreczi , Agnes Horvath , Gabor Nagy , Attila Mandi , Tamas Szuts , Istvan Bitteer , Gyula Sebestyen
发明人： Istvan Hermecz , Zoltan Meszaros , Tibor Breining , Sandor Virag , Lelle Vasvari nee Debreczi , Agnes Horvath , Gabor Nagy , Attila Mandi , Tamas Szuts , Istvan Bitteer , Gyula Sebestyen
IPC分类号： A61K31/505 , A61K31/519 , A61P1/04 , A61P7/02 , A61P9/08 , A61P9/10 , A61P25/04 , A61P25/08 , A61P29/00 , A61P31/04 , A61P37/08 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： Antiallergic and antiasthmatic compounds of the formula ##STR1## of which 9-phenylamino-6-methyl-4-oxo-6,7-dihydro-4H-pyrido(1,2-a)pyrimidine-3-carboxylic acid and optically active antipodes and salts thereof are examples.
摘要翻译：其中9-苯氨基-6-甲基-4-氧代-6,7-二氢-4H-吡啶并（1,2-a）嘧啶-3-羧酸和光学活性的抗过敏和抗哮喘化合物对映体和盐是实例。

2. 发明授权

US4461769A Nitrogen bridgehead compounds having anti-allergic effect 失效
标题翻译：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。

3. 发明授权

US4234586A Nitrogen bridgehead compounds having anti-allergic effect 失效
标题翻译：具有抗过敏作用的氮桥头头合成物
公开(公告)号：US4234586A
公开(公告)日：1980-11-18
申请号：US967958
申请日：1978-12-11
申请人： Istvan Hermecz , Zoltan Meszaros , Tibor Breining , Sandor Virag , Lelle V. 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 V. 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： Antiallergic and particularly antiasthmatic compounds of the formula: ##STR1## of which 9-phenylhydrazono-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2-a)pyrimidine-3-carboxylic acid is an especially significant example.
摘要翻译：抗过敏和特别是下列化学式的抗哮喘化合物：其中9-苯基亚肼基-6-甲基-4-氧代-6,7,8,9-四氢-4H-吡啶并（1,2-a）吡啶啶-3 - 羧酸是特别重要的实例。

4. 发明授权

US4472399A Indolo[2',3';3,4]pyrido[2,1-b]quinazoline-5-ones, a process for the preparation thereof, and diuretic compositions and methods using them 失效
标题翻译：吲哚并[2'，3'; 3,4]吡啶并[2,1-b]喹唑啉-5-酮，其制备方法和使用它们的利尿剂组合物和方法
公开(公告)号：US4472399A
公开(公告)日：1984-09-18
申请号：US308037
申请日：1981-10-02
申请人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari, nee Debreczy , Gyorgy Szasz , Agnes Horvath , Tibor Breining , Tamas Szuts , Gyula Sebestyen
发明人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari, nee Debreczy , Gyorgy Szasz , Agnes Horvath , Tibor Breining , Tamas Szuts , Gyula Sebestyen
IPC分类号： C07D471/14 , A61K31/505 , C07D487/14
CPC分类号： C07D471/14 , Y10S514/869
摘要： New Rutecarpine analogs are disclosed having Rutecarpine-like activity, especially diuretic activity. Also a novel process for the preparation of the Rutecarpine analogs is disclosed.
摘要翻译：公开了具有罗特金属样活性，特别是利尿活性的新的罗特金属类似物。还公开了用于制备罗非鱼类似物的新方法。

5. 发明授权

US4123533A Fused pyrimidine derivatives and compositions for treating atherosclerosis containing them 失效
标题翻译：融合的嘧啶衍生物和用于治疗含有它们的动脉粥样硬化的组合物
公开(公告)号：US4123533A
公开(公告)日：1978-10-31
申请号：US765595
申请日：1977-02-04
申请人： Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Knoll , Gyula Sebestyen , Agoston David
发明人： Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Knoll , Gyula Sebestyen , Agoston David
IPC分类号： C07D487/04 , A61K31/505 , A61K31/519 , A61P3/06 , A61P9/10 , A61P25/28 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/824 , Y10S514/826 , Y10S514/893 , Y10S514/916 , Y10S514/924
摘要： Compounds of the formula: ##STR1## or pharmaceutically acceptable salts thereof are disclosed wherein R is hydrogen or C.sub.1 to C.sub.6 alkyl;R.sup.2 and R.sup.3 are each hydrogen or together form a valency bond;R.sup.6 is carboxy or C.sub.1 to C.sub.6 alkoxycarbonyl;R.sup.7 and R.sup.8 are each hydrogen or together form a valency bond;R.sup.10 is carboxy or C.sub.1 to C.sub.6 alkoxycarbonyl and the dotted line represents two hydrogen atoms or a valency bond. The compounds are useful in the treatment of atherosclerosis.
摘要翻译：公开了下式的化合物：其中R是氢或C1-C6烷基; R2和R3各自为氢或一起形成价键; R6是羧基或C1-C6烷氧基羰基; R7和R8各自为氢或一起形成价键; R 10是羧基或C 1至C 6烷氧基羰基，虚线表示两个氢原子或价键。该化合物可用于治疗动脉粥样硬化。

6. 发明授权

US4252807A Fused pyrimidine derivatives and antiatherosclerotic methods of treatment with them 失效
标题翻译：融合嘧啶衍生物和抗动脉粥样硬化治疗方法
公开(公告)号：US4252807A
公开(公告)日：1981-02-24
申请号：US931908
申请日：1978-08-08
申请人： Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari , Agnes Horvath , Jozsef Knoll , Gyula Sebestyen , Agoston David
发明人： Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari , Agnes Horvath , Jozsef Knoll , Gyula Sebestyen , Agoston David
IPC分类号： C07D487/04 , A61K31/505 , A61K31/519 , A61P3/06 , A61P9/10 , A61P25/28 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/824 , Y10S514/826 , Y10S514/893 , Y10S514/916 , Y10S514/924
摘要： An optically active or racemic fused pyrimidine derivative of the formula I ##STR1## has pharmaceutical activity in decreasing serum lipids, cholesterol deposits and, in general, against atherosclerosis.
摘要翻译：式I（I）的光学活性或外消旋的稠合嘧啶衍生物具有降低血清脂质，胆固醇沉积物和一般抗动脉粥样硬化的药物活性。

7. 发明授权

US4588526A Bronchodilatory azepino(1,2-A)pyrimidine derivatives and acid addition salts thereof and bronchodilating pharmaceutical compositions containing same 失效
标题翻译：支气管佐剂（1,2-A）嘧啶衍生物及其酸加成盐和含有其的支气管扩张药物组合物
公开(公告)号：US4588526A
公开(公告)日：1986-05-13
申请号：US550937
申请日：1983-11-10
申请人： Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi , Sandor Virag , Tibor Breining
发明人： Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi , Sandor Virag , Tibor Breining
IPC分类号： A61K31/519 , A61K31/55 , A61P11/08 , C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： The invention relates to new azepino[1,2-a]pyrimidine derivatives--of the general formula ##STR1## wherein p=1, 2 and acid addition salts thereof which can be prepared by(a) reacting a compound of the formula ##STR2## with a compound of the general formula ##STR3## wherein p is as defined above and R.sup.7 is alkoxycarbonyl containing 2 to 5 carbon atoms or carboxamido or(b) reacting a compound of the general formula ##STR4## wherein R.sup.8 is alkyl containing 1 to 4 carbon atoms with a compound of the general formula ##STR5## wherein R.sup.7 is as defined above and if desired converting a compound of the general formula I to acid addition salt thereof or setting it free from the salt thereof.The new compounds show bronchodilatory activity.
摘要翻译：本发明涉及通式为其中p = 1,2及其酸加成盐的通式为其中的氮杂[1,2-a]嘧啶衍生物及其酸加成盐，其可通过（a）使式图像II与具有通式III的化合物，其中p如上所定义，R 7是含有2至5个碳原子的烷氧基羰基或甲酰胺基，或（b）使通式为IV的化合物其中R8为含有1至4个碳原子的烷基与通式为其中R 7如上所定义的化合物反应，如果需要，将通式I的化合物转化为其酸加成盐或使其不含盐。新化合物显示支气管扩张活性。

8. 发明授权

US4219649A Pyrido[1,2-a]pyrimidine derivatives 失效
标题翻译：吡啶并[1,2-a]嘧啶衍生物
公开(公告)号：US4219649A
公开(公告)日：1980-08-26
申请号：US934801
申请日：1978-08-17
申请人： Josef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
发明人： Josef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
IPC分类号： A61K31/505 , A61K31/519 , A61P25/04 , A61P29/00 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04
摘要： Compounds of the formula: ##STR1## or pharmaceutically acceptable acid addition or quaternary ammonium salts thereofwhereinR.sup.2 is C.sub.1 to C.sub.6 alkyl:R.sup.3 is C.sub.1 to C.sub.6 alkyl;R.sup.4 is a single electron pair, hydrogen or lower alkyl; and the dotted lines indicate saturated or unsaturated bonds, are disclosed with analgesic properties.
摘要翻译：下式的化合物或其药学上可接受的酸加成盐或季铵盐，其中R 2为C 1至C 6烷基：R 3为C 1至C 6烷基; R4是单电子对，氢或低级烷基; 虚线表示饱和或不饱和键，具有镇痛特性。

9. 发明授权

US4495189A Condensed pyrimidines 失效
标题翻译：浓缩嘧啶
公开(公告)号：US4495189A
公开(公告)日：1985-01-22
申请号：US364753
申请日：1982-04-02
申请人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermecz , Agnes Horvath , Sandor Virag , Lelle Vasvari , Agoston David
发明人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermecz , Agnes Horvath , Sandor Virag , Lelle Vasvari , Agoston David
IPC分类号： C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： New compounds of the following formula are disclosed:1,6-dimethyl-3-carbamoyl-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)-pyrimidine;1,6-dimethyl-3-(N-tertiary-butyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-(N-2-phenethyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-[N-(3,3-diphenyl-propyl)-carbamoyl]-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-(N-phenyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine; and1,6-dimethyl-3-(N-methyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine, as well as pharmaceutical compositions containing these compounds and a method of inhibiting thrombocyte aggregation in mammals employing a pharmaceutically effective amount of at least one of these compounds.
摘要翻译：公开了下式的新化合物：1,6-二甲基-3-氨基甲酰基-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a） - 吡啶亚胺; 1,6-二甲基-3-（N-叔丁基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶; 1,1-二甲基-3-（N-2-苯乙基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-哒嗪（1,2-a）嘧啶; 1,6-二甲基-3- [N-（3,3-二苯基 - 丙基） - 氨基甲酰基] -4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶 ; 1,6-二甲基-3-（N-苯基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶; 和1,6-二甲基-3-（N-甲基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶，以及含有这些的药物组合物化合物和使用药学上有效量的这些化合物中的至少一种来抑制哺乳动物血小板聚集的方法。

10. 发明授权

US4291036A Pyrido[1,2-A]pyrimidine derivatives and method of analgesic treatment 失效
标题翻译：吡啶并[1,2-A]嘧啶衍生物和镇痛治疗方法
公开(公告)号：US4291036A
公开(公告)日：1981-09-22
申请号：US130371
申请日：1980-03-14
申请人： Jozsef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
发明人： Jozsef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
IPC分类号： A61K31/505 , A61K31/519 , A61P25/04 , A61P29/00 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04
摘要： Compounds of the formula ##STR1## or pharmaceutically acceptable acid-addition or quaternart ammonium salts thereofwhereinR is hydroxy, carboxy, lower alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, carbamoyl, N-loweralkyl-carbamoyl, N,N-dilower-alkyl-carbamoyl, carboazido, carbohydrazido or cyano;R.sup.2 is C.sub.1 to C.sub.6 alkyl;R.sup.3 is C.sub.1 to C.sub.6 alkyl or benzyl; andR.sup.4 is a single electron pair, hydrogen or lower alkyl; and the dotted lines represent saturated or unsaturated bonds, are disclosed with analgesic properties.
摘要翻译：其中R是羟基，羧基，低级烷氧基羰基，苄氧基羰基，苯氧基羰基，氨基甲酰基，N-低级烷基 - 氨基甲酰基，N，N-二 - 低级烷基 - 氨基甲酰基，碳氮杂，碳酰肼基或氰基; R2是C1-C6烷基; R3是C1-C6烷基或苄基; R4是单电子对，氢或低级烷基; 并且虚线表示饱和或不饱和键，其具有镇痛特性。

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