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11. 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。

12. 发明授权

US4089858A Heterocyclic-amino-acrylic acid derivatives 失效
标题翻译：杂环氨基 - 丙烯酸衍生物
公开(公告)号：US4089858A
公开(公告)日：1978-05-16
申请号：US614208
申请日：1975-09-17
申请人： Zoltan Meszaros , Jozsef Knoll , Istvan Hermecz , Piroska Simon , Peter Szentmiklosy , Lelle Vasvari , Agnes Horvath , Gabor Horvath , Peter Dvortsak
发明人： Zoltan Meszaros , Jozsef Knoll , Istvan Hermecz , Piroska Simon , Peter Szentmiklosy , Lelle Vasvari , Agnes Horvath , Gabor Horvath , Peter Dvortsak
IPC分类号： C07D213/74 , C07D215/38 , C07D239/42 , C07D239/84 , C07D239/94 , C07D213/02
CPC分类号： C07D213/74 , C07D215/38 , C07D239/42 , C07D239/84 , C07D239/94
摘要： The present invention is concerned with the preparation of chemical intermediates, namely, beta-amino-acrylic acid ester derivatives of nitrogen heterocycles, i.e. pyridine, quinoline, quinoxaline, pyrazine, pyrimidine and the like. Said intermediates are cyclized to form pyrido-pyrimidine type final products possessing analgesic activity.
摘要翻译：本发明涉及化学中间体的制备，即氮杂环的β-氨基 - 丙烯酸酯衍生物，即吡啶，喹啉，喹喔啉，吡嗪，嘧啶等。所述中间体环化形成具有止痛活性的吡啶并嘧啶型终产物。

13. 发明授权

US4220771A 2,3-Polymethylene-4-oxo-4H-pyrido[1,2-a]pyrimidines 失效
标题翻译： 2,3-二亚甲基-4-氧代-4H-吡啶并[1,2-a]嘧啶
公开(公告)号：US4220771A
公开(公告)日：1980-09-02
申请号：US935071
申请日：1978-08-18
申请人： Istvan Hermecz , Ferenc Fulop , Zoltan Meszaros , Gabor Bernath , Jozsef Knoll
发明人： Istvan Hermecz , Ferenc Fulop , Zoltan Meszaros , Gabor Bernath , Jozsef Knoll
IPC分类号： A61K31/505 , A61K31/517 , A61K31/55 , A61P7/02 , A61P9/10 , A61P11/00 , A61P25/04 , A61P29/00 , A61P31/04 , A61P43/00 , C07D471/04 , C07D487/04 , C07D487/14
CPC分类号： C07D471/04 , C07D487/04
摘要： Pharmaceutical intermediates, morphine potentiators and other compounds have the formula ##STR1## wherein R is hydrogen, halogen, C.sub.1-4 alkyl, hydroxy, nitro, amino, carboxy or a carboxylic acid derivate radical, R.sup.1 is hydrogen or a C.sub.1-4 alkyl, R.sup.2 is hydrogen or C.sub.1-4 alkyl, R.sup.3 is hydrogen, R.sup.4 is hydrogen or C.sub.1-4 alkyl, R.sup.5 is hydrogen R.sup.6 is hydrogen or R.sup.3 and R.sup.4 and/or R.sup.5 and R.sup.6 form a chemical bond, X is oxygen or imino, m is 1, 2, 3 or 4, n is 0, 1, 2 or 3, and if n is 1, then the dotted lines can stand for bonds, with the proviso that if m=1 and n=1 and if in the 2,3-, 6,7-, 8,9- and 1,10-positions double bonds are present, and R.sup.1 and R.sup.2 are hydrogen, then R is other than 9-hydroxy or 9-methyl; if m=2 and n=1 and R.sup.2 is hydrogen, then at least one of R and R.sup.1 is other than hydrogen; and if m=2 and n=2 and R.sup.2 is hydrogen and the molecule is a 2,3,4,6,7,8,9,10-octahydro derivative, then at least one of R and R.sup.1 is other than hydrogen or an acid-addition or quaternary salt thereof.
摘要翻译：药物中间体，吗啡增效剂和其它化合物具有式“IMAGE”，其中R是氢，卤素，C 1-4烷基，羟基，硝基，氨基，羧基或羧酸衍生物基团，R 1是氢或C 1-4烷基， R2是氢或C1-4烷基，R3是氢，R4是氢或C1-4烷基，R5是氢R6是氢或R3和R4和/或R5和R6形成化学键，X是氧或亚氨基，m 是1,2,3或4，n是0,1,2或3，如果n是1，则虚线可以代表键，条件是如果m = 1且n = 1，如果在存在2,3,6,7,8,9和1,10-位双键，R1和R2是氢，则R不是9-羟基或9-甲基; 如果m = 2且n = 1且R2是氢，则R和R1中的至少一个不是氢; 并且如果m = 2且n = 2且R 2是氢并且该分子是2,3,4,6,7,8,9,10-八氢衍生物，则R和R 1中的至少一个不是氢或其加酸或季盐。

14. 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。

15. 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。

16. 发明授权

US4814336A Method of treating a vascular obstructive lesion resulting from restricted blood circulation 失效
标题翻译：治疗血液循环受限血管阻塞性病变的方法
公开(公告)号：US4814336A
公开(公告)日：1989-03-21
申请号：US937536
申请日：1986-12-03
申请人： Peter Szentmiklosi , Istvan Hermecz , Zoltan Meszaros , Laszo Tardos , Jeno Marton , Lelle Vasvari (nee Debreczy) , Agnes Horvath , Katalin Marmarosi (nee Kellner)
发明人： Peter Szentmiklosi , Istvan Hermecz , Zoltan Meszaros , Laszo Tardos , Jeno Marton , Lelle Vasvari (nee Debreczy) , Agnes Horvath , Katalin Marmarosi (nee Kellner)
IPC分类号： A61K31/485 , A61K31/52 , A61K31/522 , A61P9/00 , C07D473/08 , A61K31/47
CPC分类号： A61K31/52 , A61K31/485
摘要： A new method of treatment is disclosed for a vascular obstructive lesion resulting from restricted blood circulation, characterized by an erythrocyte pathology, in an effected animal subject. The new method involves the administration of 1-(3',4'-diethoxybenzyl)-6,7-diethoxy-3,4-dihydroisoquinolinium-theophylline-7-acetat e, in a dosage and at a rate sufficient to maintain a blood concentration of at least 0.5 to at most 3 .gamma./ml, calculated on the basis of 1-(3',4'-diethoxybenzyl)-6,7-diethoxy-3,4-dihydroisoquinoline.
摘要翻译：公开了一种新的治疗方法，用于在受影响的动物受试者中由特征在于红细胞病理学的限制性血液循环导致的血管阻塞性病变。该新方法涉及以足以维持一个（3'，4'-二乙氧基苄基）-6,7-二乙氧基-3,4-二氢异喹啉鎓-γ-甲基-7-乙酸乙酯的剂量和速率基于1-（3'，4'-二乙氧基苄基）-6,7-二乙氧基-3,4-二氢异喹啉计算血液浓度为至少0.5至3μg/ ml。

17. 发明授权

US4806645A Boric anhydrides of 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 失效
标题翻译： 6-氟-7-氯-1-甲基氨基-4-氧代-1,4-二氢 - 喹啉-3-羧酸的硼酸酐
公开(公告)号：US4806645A
公开(公告)日：1989-02-21
申请号：US105295
申请日：1987-08-07
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07F5/02 , C07D215/56 , C07D215/58 , C07F5/00 , C07F5/04
CPC分类号： C07F5/04
摘要： The invention relates to new 6-fluoro-7-chloro-1-methylamino-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid/boric acid anhydrides of the general Formula I ##STR1## (wherein R and R.sup.1 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms).The new compounds of the general Formula I are valuable intermediates useful in the preparation of the antibacterial agent 6-fluoro-1-methylamino-7-(4-methyl-piperazino)-4-oxo-1,4-dihydro-quinoline-3- carboxylic acid.The new compounds of the general Formula I may be prepared by reacting a compound of the Formula II ##STR2## or a compound of the general Formula III ##STR3## (wherein R.sup.2 stands for alkyl comprising 1-4 carbon atoms) with hydrogen fluoro borate of the Formula IVHBF.sub.4 /IV/or a borone trihalide of the general Formula VBX.sub.3 /V/(wherein X stands for fluorine, chlorine or bromine) or a complex thereof formed with an ether or a borone derivative of the general Formula VI ##STR4## (wherein R.sup.3, R.sup.4 and R.sup.5 stand for alkyl comprising 1-5 carbon atoms and optionally substituted by halogen or aryl comprising 6-10 carbon atoms).
摘要翻译： PCT No. PCT / HU86 / 00066 Sec。 371日期1987年8月7日 102（e）日期1987年8月7日PCT申请日1986年12月9日PCT公布。公开号WO87 / 03594 日期：1987年6月18日本发明涉及通式I的新的6-氟-7-氯-1-甲基氨基-4-氧代-1,4-二氢 - 喹啉-3-羧酸/硼酸酐，图像（I）（其中R和R1代表卤素;包含2-6个碳原子并任选被卤素取代的脂族酰氧基;或包含7-11个碳原子的芳族酰氧基）。通式I的新化合物是可用于制备抗菌剂6-氟-1-甲基氨基-7-（4-甲基 - 哌嗪子基）-4-氧代-1,4-二氢 - 喹啉线衍生物的有价值的中间体， 3-羧酸。通式I的新化合物可以通过使式II的化合物（II）或通式III的化合物（III）（其中R 2代表包含1-4个碳原子的烷基）原子）与式IV的氢氟硼酸盐HBF 4 / IV /或通式V BX 3 / V /（其中X表示氟，氯或溴）的三卤化硼硼烷或其与醚或硼烷衍生物形成的络合物通式VI（VI）（其中R 3，R 4和R 5代表包含1-5个碳原子并且任选地被卤素或包含6-10个碳原子的芳基取代的烷基）。

18. 发明授权

US4803274A Norfloxacin intermediate 失效
标题翻译：诺氟沙星中间体
公开(公告)号：US4803274A
公开(公告)日：1989-02-07
申请号：US105298
申请日：1987-08-07
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Gabor Kovacs , Zoltan Meszaros, deceased , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07F5/02 , C07D215/56 , C07F5/00 , C07F5/04
CPC分类号： C07F5/04
摘要： The invention relates to a process for the preparation of compounds of the Formula I ##STR1## (wherein R and R.sup.1 stand for an aliphatic acyloxy group comprising 2-5 carbon atoms and optionally substituted by halogen or for an aromatic acyloxy group comprising 7-11 carbon atoms), which comprises reacting a compound of the general Formula II ##STR2## (wherein R.sup.2 stands for hydrogen or alkyl comprising 1-4 carbon atoms) with a boron derivative of the Formula III ##STR3## (wherein R.sup.3, R.sup.4 and R.sup.5 stand for an alkyl group comprising 1-4 carbon atoms and optionally substituted by halogen or for an aryl group comprising 6-10 carbon atoms).The new compounds of the general Formula I are useful pharmaceutical intermediates.
摘要翻译： PCT No.PCT / HU86 / 00068 Sec。 371日期1987年8月7日 102（e）日期1987年8月7日PCT申请日1986年12月9日PCT公布。第WO87 / 03595号公报日本1987年6月18日。本发明涉及制备式I化合物（I）的方法（其中R和R 1代表包含2-5个碳原子并任选被卤素取代的脂族酰氧基或包含7-11个碳原子的芳族酰氧基），其包括使通式II的化合物（II）（其中R 2表示氢或包含1-4个碳原子的烷基）与式式III（III）（其中R3，R4和R5代表含有1-4个碳原子的烷基，任选被卤素取代或含有6-10个碳原子的芳基）。通式I的新化合物是有用的药物中间体。

19. 发明授权

US4404205A 2-Oxo-2,6,7,8,9,10 hexahydro-pyrimido[1,2-a]azepines and antianginal method of use thereof and of 4-oxo-4,6,7,8,9,10-hexahydropyrimido[1,2-a]azepines 失效
标题翻译： 2-氧代-2,6,7,8,9,10-六氢 - 嘧啶并[1,2-a]吖庚因及其抗肾功能方法和4-氧代-4,6,7,8,9,10- 六氢嘧啶并[1,2-a]吖庚因
公开(公告)号：US4404205A
公开(公告)日：1983-09-13
申请号：US148234
申请日：1980-05-09
申请人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Gyorgy Szasz , Lelle Vasvari nee Debreczy , Agnes Horvath , Tibor Breining
发明人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Gyorgy Szasz , Lelle Vasvari nee Debreczy , Agnes Horvath , Tibor Breining
IPC分类号： A61K31/55 , A61K31/551 , A61P9/00 , A61P9/04 , C07D487/04 , A61K31/305
CPC分类号： C07D487/04
摘要： 3 Substituted hexahydro-pyrimido[1, 2 a]azepines and quaternary derivatives, useful as antianginals are prepared. Specifically tested are 3 carboxylates and carbo hydrazides. 3 Cyano Carbamonyl and alkyl compounds are also disclosed.
摘要翻译： 3制备用作抗坏血酸的取代的六氢 - 嘧啶并[1,2]吖庚因和季衍生物。具体测试的是3个羧酸酯和碳酰肼。还公开了3种氰基氨基甲酰基和烷基化合物。

20. 发明授权

US4395549A 6-Hydrazono-pyrido[2,1-b] quinazoline-11 ones 失效
标题翻译： 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。

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