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1. 发明授权

US5380845A Process for the preparation of quinoline carboxylic acid derivatives 失效
标题翻译：制备喹啉羧酸衍生物的方法
公开(公告)号：US5380845A
公开(公告)日：1995-01-10
申请号：US149692
申请日：1993-11-09
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Peter Ritli , Judit Sipos , Aniko Pajor
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Peter Ritli , Judit Sipos , Aniko Pajor
IPC分类号： C07D215/56 , C07D401/02 , C07D401/04
CPC分类号： C07D215/56
摘要： The invention relates to a new process for the preparation of antibacterial compounds of the Formula I ##STR1## wherein R.sup.1 stands for phenyl substituted by 1 or 2 halogen atoms;R.sup.2 stands for piperazinyl or 4-methyl-piperazinyl;and pharmaceutically acceptable salts thereof which comprises using a compound of the Formula II ##STR2## wherein R stands for halogen or an aliphatic acyloxy group containing 2 to 6 carbon atoms or an aromatic acyloxy group containing 7 to 11 carbon atoms andR.sup.4 stands for fluorine or chlorine as a starting material.
摘要翻译：本发明涉及制备式I的抗菌化合物（I）的新方法，其中R1代表被1或2个卤素原子取代的苯基; R2代表哌嗪基或4-甲基 - 哌嗪基; 其包括使用式II的化合物（II）其中R代表卤素或含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，R4代表以氟或氯为原料。

2. 发明授权

US4460771A Antiphlogistic and anticoagulant condensed pyrimidine derivatives 失效
标题翻译：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。

3. 发明授权

US5300644A 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：US5300644A
公开(公告)日：1994-04-05
申请号：US756345
申请日：1991-09-06
申请人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
发明人： Istvan Hermecz , Geza Kereszturi , Lelle Vasvari , Agnes Horvath , Maria Balogh , Peter Ritli , Judit Sipos , Aniko Pajor , Katalin Marmarosi
IPC分类号： C07D401/04 , A61K31/4709 , A61K31/495 , A61P31/04 , C07D215/56 , C07F5/02
CPC分类号： C07D215/56
摘要： The invention relates to a new process for the preparation of compounds of the general Formula I ##STR1## wherein R stands for piperazinyl, 4-methyl-piperazinyl or 4-ethyl-piperazinyl group and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II ##STR2## wherein R.sup.1 and R.sup.2 stand for halogen, for an aliphatic acyloxy group containing 2 to 6 carbon atoms and optionally substituted by halogen, or for an aromatic acyloxy group containing 7 to 11 carbon atoms with a piperazine derivative of the general Formula III ##STR3## wherein R.sup.3 stands for hydrogen, methyl or ethyl or a salt thereof and subjecting the compound of the general Formula IV ##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 general Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the general Formula I are known antibacterial agents.
摘要翻译：本发明涉及制备通式Ⅰ（I）化合物的新方法，其中R代表哌嗪基，4-甲基 - 哌嗪基或4-乙基 - 哌嗪基及其药物上可接受的盐，其包括使通式II的化合物（II）其中R1和R2代表卤素，含2至6个碳原子的脂族酰氧基并任选被卤素取代，或含有7至11个碳原子的芳族酰氧基与通式III的哌嗪衍生物（III）其中R3代表氢，甲基或乙基或其盐，并对由此得到的通式IV的化合物（IV）进行反应，其中R 1，R 2和R 2 如上所述，在分离后或不分离时进行水解，如果需要，将由此获得的通式I的化合物转化为其盐或使其与其盐相同。通式I的化合物是已知的抗菌剂。

4. 发明授权

US5252572A 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：US5252572A
公开(公告)日：1993-10-12
申请号：US903246
申请日：1992-06-23
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。

5. 发明授权

US5158951A Pyridopyrimidine derivatives useful in treatment of ulcers 失效
标题翻译：用于治疗溃疡的吡啶并嘧啶衍生物
公开(公告)号：US5158951A
公开(公告)日：1992-10-27
申请号：US307665
申请日：1989-02-06
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： A61K31/505 , A61K31/513 , A61K31/519 , A61P1/04 , C07D221/00 , C07D239/26 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine -3-carbonamide 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## wherein: 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 repesents 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。通式（I）其中：R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代表氢或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。

6. 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）。

7. 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。

8. 发明授权

US4452982A Process for the preparation of nitrogen-bridgehead condensed pyrimidine compounds, and pharmaceutical compositions containing them 失效
标题翻译：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。

9. 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。

10. 发明授权

US5475000A 3-(substituted tetrazolyl)-4-oxo-4H-pyrido-[1,2-a]pyrimidines, salts thereof, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译： 3-（取代的四唑基）-4-氧代-4H-吡啶并[1,2-a]嘧啶，其盐，含有它们的药物组合物及其制备方法
公开(公告)号：US5475000A
公开(公告)日：1995-12-12
申请号：US193080
申请日：1994-02-10
申请人： Istvan Hermecz , Jozsef Knoll , Judit Sipos , Klara Gyires , Agnes Horvath , Lelle Vasvari , Laszlo Tardos , Maria Balogh , Zoltan Kapui , Ilona Papp
发明人： Istvan Hermecz , Jozsef Knoll , Judit Sipos , Klara Gyires , Agnes Horvath , Lelle Vasvari , Laszlo Tardos , Maria Balogh , Zoltan Kapui , Ilona Papp
IPC分类号： A61K31/505 , A61P1/04 , C07D239/00 , C07D403/00 , C07D471/04
CPC分类号： C07D471/04
摘要： 4-oxo-4H-pyrido[1,2-a]-pyrimidines are disclosed of the formula ##STR1## wherein R is a C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl, --(CH.sub.2).sub.n --COOR.sup.3 wherein R.sup.3 is C.sub.1 to C.sub.4 alkyl and n is 0 or 1 or a C.sub.7-8 aralkyl group, optionally substituted by one or more halogen atom(s), or by a nitro-group, R.sup.1 is a hydrogen atom or a C.sub.1-4 alkyl group, and salts thereof, as well as a process for their preparation, and pharmaceutical compositions containing them. These compounds are therapeutically useful as gastroprotectives in the treatment and prevention of ulcer.
摘要翻译： PCT No.PCT / HU92 / 00031 Sec。 371日期：1994年2月10日 102（e）日期1994年2月10日PCT提交1992年8月13日PCT公布。出版物WO93 / 04065 日期1993年3月4日.4-氧代-4H-吡啶并[1,2-a] - 嘧啶公开于式（Ⅰ）和/或其中R为C 1-6烷基，（CH 2）n -COOR 3，其中R 3为C 1至C 4烷基，n为0或1或C 7-8芳烷基，任选被一个或多个卤素原子取代）或硝基，R 1为氢原子或C 1-4烷基，及其盐，以及其制备方法，以及含有它们的药物组合物。这些化合物在治疗和预防溃疡中是治疗上有用的胃肠保护剂。

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