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11. 发明授权

US4940794A Quinoline carboxylic acid boric acid anhydrides 失效
标题翻译：喹啉羧酸硼酸酐
公开(公告)号：US4940794A
公开(公告)日：1990-07-10
申请号：US290167
申请日：1988-12-02
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Halogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Halogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
IPC分类号： C07D215/56 , A61K31/47 , A61P31/04 , C07D215/16 , C07D215/54 , C07F5/00 , C07F5/02 , C07F5/04
CPC分类号： C07F5/04
摘要： The invention relates to new quinoline-3-carboxylic acid anhydride intermediates of the Formula I ##STR1## wherein R stands for cyclopropyl, a group of the Formula --CH.sub.2 CR.sup.5 R.sup.6 R.sup.7 wherein R.sup.5, R.sup.6 and R.sup.7 stand for hydrogen or halogen, or phenyl optionally substituted by 1 or 2 halogen,R.sup.1 and R.sup.2 stand for halogen, or an aliphatic acyloxy group containing 2 to 6 carbon atoms optionally substituted by halogen, or an aromatic acyloxy group containing 7 to 11 carbon atoms,R.sup.3 stands for chlorine or fluorine andR.sup.4 stands for hydrogen or fluorine. The compounds of the Formula I are new intermediates for the preparation of known quinoline-3-carbocxylic acids showing antibacterial activity.
摘要翻译： PCT No.PCT / HU88 / 00018 Sec。 371日期：1988年12月2日 102（e）日期1988年12月2日PCT提交1988年4月8日PCT公布。出版物WO88 / 07998 日本公开号为1988年10月20日。本发明涉及式I（I）的新型喹啉-3-羧酸酐中间体，其中R代表环丙基，式-CH 2 CR 5 R 6 R 7基团，其中R5，R6和R7表示对于氢或卤素，或任选被1或2个卤素取代的苯基，R 1和R 2代表卤素，或任选被卤素取代的含2至6个碳原子的脂族酰氧基或含有7至11个碳原子的芳族酰氧基， R3代表氯或氟，R4代表氢或氟。式I化合物是制备显示抗菌活性的已知喹啉-3-羧酸的新中间体。

12. 发明授权

US4670440A Medicinal norfloxacin salts 失效
标题翻译：药用诺氟沙星盐
公开(公告)号：US4670440A
公开(公告)日：1987-06-02
申请号：US854395
申请日：1986-04-21
申请人： Tamas Szuts , Peter Szentmiklosi , Jozsef Lengyel , Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Geza Kerszturi , Gabor Kovacs , Gabor Horvath , Katalin Marmarosi nee Kellner
发明人： Tamas Szuts , Peter Szentmiklosi , Jozsef Lengyel , Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Geza Kerszturi , Gabor Kovacs , Gabor Horvath , Katalin Marmarosi nee Kellner
IPC分类号： A23K1/16 , A61K31/4709 , A61K31/495 , A61K31/496 , A61P31/04 , C07C67/00 , C07C213/00 , C07C215/40 , C07D215/56 , C07D401/10 , C07D401/04
CPC分类号： C07D215/56
摘要： N,N,N-trimethyl-2-hydroxyethyl-ammonium-[1-ethyl-6-fluoro-4-oxo-7-(1-piperazinyl)-1,4-dihydro-quinolizine-3-carboxylate] of the formula I ##STR1## as a norfloxacin antimicrobial salt capable of enteral administration.
摘要翻译： N，N，N-三甲基-2-羟乙基 - 铵 - [1-乙基-6-氟-4-氧代-7-（1-对异哌嗪基）-1,4-二氢 - 喹嗪-3-羧酸酯] 配方I 作为能够肠内给药的诺氟沙星抗微生物盐。

13. 发明授权

US4666912A Treating process 失效
标题翻译：治疗过程
公开(公告)号：US4666912A
公开(公告)日：1987-05-19
申请号：US715190
申请日：1985-03-22
申请人： Zoltan Meszaros , Jozse Knoll , Istvan Hurmecz , Peter Szentmiklosi , Agnes Horvath , Lelle Vasvari nee Debreczy , Gabor Kovacs , Klara Gyires , Sandor Virag
发明人： Zoltan Meszaros , Jozse Knoll , Istvan Hurmecz , Peter Szentmiklosi , Agnes Horvath , Lelle Vasvari nee Debreczy , Gabor Kovacs , Klara Gyires , Sandor Virag
IPC分类号： C07D471/04 , A61K31/505 , A61P1/04
CPC分类号： A61K31/505 , Y10S514/926 , Y10S514/927
摘要： The invention relates to a process for the restoration and prevention of gastrointestinal injuries, which comprises treating a patient with an effective dose of racemic or optically active 1,6-dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrimido[1,2-a]pyrimidine-3-carboxamide.
摘要翻译：本发明涉及一种恢复和预防胃肠道损伤的方法，其包括用有效剂量的外消旋或光学活性的1,6-二甲基-4-氧代-1,6,7,8,9,9a - 六氢-4H-嘧啶并[1,2-a]嘧啶-3-甲酰胺。

14. 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。

15. 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。

16. 发明授权

US4456752A 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
标题翻译：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。

17. 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。

18. 发明授权

US4209622A 3-(Ethoxycarbonyl-methyl)-6-methyl-4-oxo-6,7,8,9-tet rahydro-4H-pyrido[1,2-a]pyrimidine 失效
标题翻译： 3-（乙氧基羰基 - 甲基）-6-甲基-4-氧代-6,7,8,9-四氢-4H-吡啶并[1,2-a]嘧啶
公开(公告)号：US4209622A
公开(公告)日：1980-06-24
申请号：US559916
申请日：1975-03-19
申请人： Zoltan Meszaros , Jozsef Knoll , Istvan Hermecz , Lelle Vasvari , Agnes Horvath
发明人： Zoltan Meszaros , Jozsef Knoll , Istvan Hermecz , Lelle Vasvari , Agnes Horvath
IPC分类号： C07D471/04 , A61K31/505 , C07D487/04
CPC分类号： C07D471/04 , Y10S514/916
摘要： Pyrida-(1,2A)-pyrimidine-derivatives and a process for preparing these compounds are disclosed. These compounds possess analgesic, anti-inflammatory, and anti-pyretic properties as well as the ability to depress the central nervous system.
摘要翻译：公开了吡啶并（1,2A） - 嘧啶衍生物及其制备方法。这些化合物具有镇痛，抗炎和抗热解性能以及抑制中枢神经系统的能力。

19. 发明授权

US5387588A Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：吡啶并嘧啶衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5387588A
公开(公告)日：1995-02-07
申请号：US80402
申请日：1993-06-21
申请人： Istvan Hermecz , Jozsef Knoll , Lelle Vasvari nee Debreczy , Klara Gyires , Judit Sipos , Agnes Horvath , Laszlo Tardos , Maria Blaogh
发明人： Istvan Hermecz , Jozsef Knoll , Lelle Vasvari nee Debreczy , Klara Gyires , Judit Sipos , Agnes Horvath , Laszlo Tardos , Maria Blaogh
IPC分类号： C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 represents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.
摘要翻译：本发明涉及通式（I）的新型4-氧代-4H-吡啶并[1,2-a]嘧啶-3-甲酰胺衍生物及其酸加成盐，含有它们的药物组合物及其制备方法。在通式（I）中，R 1表示任选被C 1-4烷氧基羰基取代的C 1-12烷基; C3-9环烷基，金刚烷基或任选取代的苯基; R1表示氢或C1-4烷基; 或R和R 1一起形成 - （CH 2）n - 链，其中n为4,5或6; R2代表氢，C1-4烷基或卤素; R3表示氢或C1-4烷基; m为0或1.通式（I）的化合物具有胃保护作用，可用于预防和治疗胃和小肠溃疡。

20. 发明授权

US4981966A Process for the preparation of quinoline carboxylic acids 失效
标题翻译：制备喹啉羧酸的方法
公开(公告)号：US4981966A
公开(公告)日：1991-01-01
申请号：US295439
申请日：1989-01-10
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari nee Debreczy , Agnes Horvath , Maria Balogh , Gabor Kovacs , Tamas Szuts , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D401/10 , A61K31/47 , A61P31/04 , C07D215/56 , C07D295/067 , C07D295/155 , C07F5/02 , C07F5/04
CPC分类号： C07D215/56 , C07F5/022 , C07F5/04
摘要： The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.The advantage of the process of the present invention is that it makes the desired compounds of the Formula I available in a simple manner, with high yields and in a short reaction time.
摘要翻译：本发明涉及制备式I化合物（I）（其中R代表氢或甲基）及其药学上可接受的盐的新方法，其包括使式V化合物（V ）（其中R 1和R 2表示包含2-6个碳原子并且任选被卤素取代的脂族酰氧基或对于包含7-11个碳原子的芳族酰氧基）与式VI的胺VI，（其中R具有与上述相同的含义）或其盐，并且如此获得的式VII（VII）化合物（其中R，R 1和R 2如上所述）在分离之后或在不分离之前进行水解，以及如果需要将由此获得的式I的化合物转化成其盐或使其与其盐相同。式I的化合物是已知的抗菌剂。本发明方法的优点在于使得所需的式I化合物可以简单的方式得到，产率高，反应时间短。

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