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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 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。

9. 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。

10. 发明授权

US5284950A Process for the preparation of quinoline carboxyolic acids 失效
标题翻译：喹啉羧酸的制备方法
公开(公告)号：US5284950A
公开(公告)日：1994-02-08
申请号：US691633
申请日：1991-04-25
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： C07D215/56 , C07F5/02 , C07F5/04 , C07D403/04
CPC分类号： C07D215/56 , C07F5/022 , C07F5/04
摘要： A method of using a compound of the Formula (V) ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, wherein R.sup.1 and R.sup.2 are each C.sub.1 to C.sub.6 aliphatic acyloxy, unsubstituted or substituted by halogen, or are each C.sub.7 to C.sub.11 aromatic acyloxy,for preventing amination of the 6-position when a compound of the Formula (I) ##STR2## or a pharmaceutically acceptable salt thereof is to be formed, which comprises the steps of:(a) aminating the compound of the Formula (V) or a pharmaceutically acceptable salt thereof with piperazine in an inert organic solvent to yield a compound of the Formula (VII) ##STR3## or a pharmaceutically acceptable salt thereof, and (b) hydrolyzing the compound of the Formula (VII) or a pharmaceutically acceptable salt thereof, after or without isolation, to obtain the compound of the Formula (I), and if desired, converting the compound of the Formula (I) into a pharmaceutically acceptable salt thereof, or setting free the compound of the Formula (I) from its pharmaceutically acceptable salt.
摘要翻译：公开了使用式（V）的化合物或其药学上可接受的盐的方法，其中R 1和R 2各自是未被取代或被卤素取代的C 1至C 6脂族酰氧基，或各自为C7至 C11芳族酰氧基，用于防止当式（I）化合物或其药学上可接受的盐形成时，6-位的胺化，其包括以下步骤：（a）胺化化合物（VII）化合物或其药学上可接受的盐，和（b）将式（Ⅴ）化合物或其药学上可接受的盐与哌嗪在惰性有机溶剂中反应，得到式式（VII）化合物或其药学上可接受的盐在得到式（I）化合物后，如果需要，将式（I）化合物转化为其药学上可接受的盐，或设定释放式的化合物（I）的药学上可接受的盐。

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