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21. 发明授权

US4602018A Condensed as-triazine derivatives 失效
标题翻译：浓缩的三嗪衍生物
公开(公告)号：US4602018A
公开(公告)日：1986-07-22
申请号：US652612
申请日：1984-09-20
申请人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko
发明人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko
IPC分类号： A61K31/53 , A61P9/02 , A61P9/06 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P29/00 , C07D217/16 , C07D471/04 , C07D253/08
CPC分类号： C07D471/04 , C07D217/16
摘要： The invention relates to new condensed as-triazine derivatives of the general Formula I ##STR1## and isomers thereof (wherein R.sub.1 stands for C.sub.1-10 alkyl or phenyl or naphthyl, wherein the two latter groups may be optionally substituted by one or more halogen, nitro, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.2 is hydrogen, C.sub.1-4 alkyl, hydroxy, halogen or phenyl or naphthyl, wherein the two latter groups may be optionally substituted by one or more halogen, nitro, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.3 represents hydrogen or C.sub.1-4 alkyl;Z is buta-1,3-dienyl or a group of the Formula (a) ##STR2## and A.sup.- is an anion).The compounds of the general Formula I possess useful pharmacological properties, particularly antiarrhythmial and antidepressant effect.
摘要翻译：本发明涉及通式I（I）的新的缩合的三嗪衍生物及其异构体（其中R1代表C1-10烷基或苯基或萘基，其中后两个基团可任选地被一个或多个更多的卤素，硝基，氨基，羟基，C 1-4烷基和/或C 1-4烷氧基取代基; R 2是氢，C 1-4烷基，羟基，卤素或苯基或萘基，其中后两个基团可以是任选的被一个或多个卤素，硝基，氨基，羟基，C 1-4烷基和/或C 1-4烷氧基取代基取代; R 3表示氢或C 1-4烷基; Z是丁-1,3-二烯基或基团（a）（a）或（b）（b），A-是阴离子）。通式I的化合物具有有用的药理学特性，特别是抗心律失常和抗抑郁作用。

22. 发明授权

US4324786A Pyrido[2,3-e]-as-triazine derivatives and pharmaceutical compositions 失效
标题翻译：吡啶并[2,3-e] -as-三嗪衍生物和药物组合物
公开(公告)号：US4324786A
公开(公告)日：1982-04-13
申请号：US143778
申请日：1980-04-25
申请人： Andras Messmer , Pal Benko , Gyorgy Hajos , Lujza Petocz , Ibolya Kosoczky , Peter Gorog
发明人： Andras Messmer , Pal Benko , Gyorgy Hajos , Lujza Petocz , Ibolya Kosoczky , Peter Gorog
IPC分类号： A61K31/53 , A61K31/535 , A61P25/00 , A61P25/04 , A61P25/20 , A61P29/00 , C07D221/04 , C07D253/10 , C07D471/04 , C07D471/14
CPC分类号： C07D471/04
摘要： New pyrido[2,3-e]-as-triazine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-20 alkylcarbonyl, halogenated (C.sub.1-4 alkyl)-carbonyl, C.sub.1-4 alkoxycarbonyl, benzoyl, phenyl-(C.sub.1-4 alkyl)-carbonyl or phenyl-(C.sub.2-4 alkenyl)-carbonyl group or a 5-10-membered mono- or bicyclic nitrogen-containing heterocyclic acid residue (preferably a pyridylcarbonyl group) containing optionally one or more additional nitrogen, oxygen and/or sulfur atoms in the heterocyclic ring, and optionally one or more identical or different substituents selected from the group consisting of halogen, C.sub.1-4 alkoxy, nitro and hydroxy are attached to the aromatic or heterocyclic rings, furthermore one of R.sup.1 and R.sup.2 may also stand for hydrogen atom, orR.sup.1 and R.sup.2 may form, together with the adjacent nitrogen atoms, a pyrazole-2,4 ring having optionally a C.sub.1-6 alkyl substituent in position 3, andR.sup.3 stands for hydrogen, halogen, C.sub.1-4 alkoxy, amino, mono-(C.sub.1-6 alkyl)-amino, di-(C.sub.1-6 alkyl)-amino, hydroxy, alkylated or acylated hydroxy, morpholino, piperazino, N-(C.sub.1-6 alkyl)-piperazino, N-benzylpiperazino or N-pyridylpiperazino group,and pharmaceutically acceptable acid addition salts thereof are prepared by acylating the respective 1,2-unsubstituted 1,2-dihydro-pyrido[2,3-e]-as-triazine derivatives.The new compounds according to the invention act on the central nervous system and exert sedative, analgesic, narcosis potentiating, tetrabenazine antagonizing and antiphlogistic effects. The new compounds according to the invention can be applied to advantage in the therapy.
摘要翻译：通式（I）的新的吡啶并[2,3-e] -as-三嗪衍生物，其中R 1和R 2各自代表C 1-20烷基羰基，卤代（C 1-4烷基） - 羰基，C 1-4烷氧基羰基，苯甲酰基，苯基 - （C 1-4烷基） - 羰基或苯基 - （C 2-4烯基） - 羰基或5-10元单环或双环含氮杂环酸残基（优选含有任选的一个或多个杂环中的一个或多个另外的氮，氧和/或硫原子，以及任选地一个或多个相同或不同的选自卤素，C 1-4烷氧基，硝基和羟基的取代基被连接到芳族或杂环，此外，R 1和R 2中的一个也可以代表氢原子，或者R 1和R 2可以与相邻的氮原子一起形成具有任选地C 1-6烷基取代基的吡唑-2,4环的位置 3，R3代表氢，卤素，C1-4烷氧基，氨基，单 - （C1-6烷基） - 氨基，二 - （C1-6烷基） - 氨羟基，烷基化或酰化羟基，吗啉代，哌嗪子基，N-（C 1-6烷基） - 哌嗪基，N-苄基哌嗪子基或N-吡啶基哌嗪子基及其药学上可接受的酸加成盐，未取代的1,2-二氢 - 吡啶并[2,3-e] -as-三嗪衍生物。根据本发明的新化合物作用于中枢神经系统，并施加镇静，止痛，麻醉增强，丁苯那嗪拮抗和消炎作用。根据本发明的新化合物可以在治疗中有利地应用。

23. 发明授权

US5126457A Process for the preparation of 1,4-dihydro-pyridine derivatives 失效
标题翻译：制备1,4-二氢吡啶衍生物的方法
公开(公告)号：US5126457A
公开(公告)日：1992-06-30
申请号：US321293
申请日：1989-03-08
申请人： Pal Benko , Daniel Bozsing , Laszlo Levai , Gyorgyi Kovanyi nee Lax , Gyorgy Mikite , Peter Tompe , Eva Furdyga , Ilona Dinnyes nee Nagy , Eva Poczik , Gyorgyi Zalavari nee Dosa , Ivan Beck , Istvan Simonyi , Kalman Nagy , Janos Imre , Erzsebet Kiss nee Bertok , Eva J. Tajthy nee Juhasz , Attila Mandi , Frigyes Gorgenyi
发明人： Pal Benko , Daniel Bozsing , Laszlo Levai , Gyorgyi Kovanyi nee Lax , Gyorgy Mikite , Peter Tompe , Eva Furdyga , Ilona Dinnyes nee Nagy , Eva Poczik , Gyorgyi Zalavari nee Dosa , Ivan Beck , Istvan Simonyi , Kalman Nagy , Janos Imre , Erzsebet Kiss nee Bertok , Eva J. Tajthy nee Juhasz , Attila Mandi , Frigyes Gorgenyi
IPC分类号： C07C251/24 , C07D211/90
CPC分类号： C07D211/90 , C07C251/24
摘要： The invention is directed to processes for the preparation of dimethyl-1,4-dihydro-2,6-dimethyl-4-(2'-nitrophenyl)-pyridine-3,5-dicarboxylate by reacting 1-methoxy-1-(2'-nitrophenyl)-N-(2'-nitrophenyl)methylene methanamie or 1-(2'-nitrophenyl)-N,N'-bis-(2'-nitrophenyl) methylene methanediamine with methyl acetoacetate in the presence of an amine compound or by reacting the monomeric or trimeric from of 2-nitrobenzaldimine with methyl acetoacetate.
摘要翻译：本发明涉及制备二甲基-1,4-二氢-2,6-二甲基-4-（2'-硝基苯基） - 吡啶-3,5-二羧酸二甲酯的方法，通过1-甲氧基-1-（ 2'-硝基苯基）-N-（2'-硝基苯基）亚甲基甲酰胺或1-（2'-硝基苯基）-N，N'-双 - （2'-硝基苯基）亚甲基甲二胺与乙酰乙酸甲酯在胺化合物或通过使2-硝基苯甲酰亚胺与乙酰乙酸甲酯的单体或三聚体反应。

24. 发明授权

US4320127A Pyrido[3,2-e]-as-triazines 失效
标题翻译：吡啶并[3,2-e] -as-三嗪
公开(公告)号：US4320127A
公开(公告)日：1982-03-16
申请号：US152833
申请日：1980-05-23
申请人： Pal Benko , Andras Messmer , Gyorgy Hajos , Sandor Batori , Lujza Petocz , Iboly Kosoczky , Peter Gorog
发明人： Pal Benko , Andras Messmer , Gyorgy Hajos , Sandor Batori , Lujza Petocz , Iboly Kosoczky , Peter Gorog
IPC分类号： A61K31/53 , A61P25/00 , A61P25/04 , A61P25/20 , A61P29/00 , C07D471/04 , C07D471/14
CPC分类号： C07D471/04 , C07D471/14
摘要： The invention relates to new pyrido[3,2-e]-as-triazine derivatives of the formula I and pharmaceutically acceptable acid addition salts thereof, ##STR1## wherein R.sub.1 stands for a C.sub.1-20 alkyl-carbonyl group, halogen-C.sub.1-4 alkyl-carbonyl, benzoyl, phenyl-C.sub.1-4 alkyl-carbonyl, or pyridyl-carbonyl group;R.sub.2 is a hydrogen atom or a C.sub.1-4 alkyl-carbonyl group; or R.sub.1 and R.sub.2 form together with the adjacent nitrogen atoms a pyrazole-2,4-dione ring which carries a C.sub.1-6 alkyl substituent in position 3;R.sub.3 is a hydrogen atom, a C.sub.1-20 alkyl, phenyl, phenyl-C.sub.1-3 alkyl, furyl or pyridyl group or a phenyl group optionally substituted by one to three C.sub.1-4 alkoxy-groups.The compounds of the formula I are prepared by acylating the respective 1,2-un-substituted 1,2-dihydropyrido [3,2-e]-as-triazine derivatives. The new compounds exert valuable effects on the central nervous system and possess analgesic, antiphlogistic effects, and can be applied to advantage in therapy.
摘要翻译：本发明涉及式I的新的吡啶并[3,2-e] -as-三嗪衍生物及其药学上可接受的酸加成盐，其中R1代表C1-20烷基羰基，卤素C1 -4-烷基 - 羰基，苯甲酰基，苯基-C 1-4烷基 - 羰基或吡啶基 - 羰基; R2是氢原子或C1-4烷基 - 羰基; 或R 1和R 2与相邻的氮原子一起形成在3位上带有C1-6烷基取代基的吡唑-2,4-二酮环; R 3是氢原子，C 1-20烷基，苯基，苯基-C 1-3烷基，呋喃基或吡啶基或任选被一至三个C 1-4烷氧基取代的苯基。通过酰化相应的1,2-未取代的1,2-二氢吡啶并[3,2-e] -as-三嗪衍生物制备式I化合物。新化合物对中枢神经系统起重要作用，具有镇痛，消炎作用，可用于治疗。

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