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1. 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。

2. 发明授权

US4697013A Condensed as-triazine derivatives 失效
标题翻译：浓缩的三嗪衍生物
公开(公告)号：US4697013A
公开(公告)日：1987-09-29
申请号：US652613
申请日：1984-09-20
申请人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko , Laszlo Pallos , Lujza Petocz , Grasser Katalin , Ibolya Kosoczky
发明人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko , Laszlo Pallos , Lujza Petocz , Grasser Katalin , Ibolya Kosoczky
IPC分类号： C07D253/08 , C07D471/04
CPC分类号： C07D471/04
摘要： A one step process for the preparation of compounds having antidepressant activity of the formula I ##STR1## and isomers thereof, wherein R.sub.1, R.sub.2, Z and A.sup.- have the meanings indicated in the claims, which process comprises: heating a compound of the formula II ##STR2## wherein Z, A.sup.-, R.sub.1 and R.sub.2 have the meanings set out in the claims and R.sub.3 stands for hydrogen or C.sub.1-4 alkyl, in the presence of a dehydrating agent to split off a compound of the formula R.sub.3 OH. The invention is also directed to compounds of the formula I, wherein R.sub.2 is halogen and to compositions containing a compound of the formula I which exhibit antidepressant activity.
摘要翻译：制备具有式I的抗抑郁活性的化合物及其异构体的一步法，其中R1，R2，Z和A具有权利要求中所示的含义，该方法包括：将式II其中Z，A，R 1和R 2具有权利要求中所述的含义，R 3代表氢或C 1-4烷基，在脱水剂的存在下分离式R 3 OH的化合物。本发明还涉及式I化合物，其中R 2是卤素，以及含有表现出抗抑郁活性的式I化合物的组合物。

3. 发明授权

US4419355A Condensed as-triazine derivatives and method of using the same 失效
标题翻译：缩合三嗪衍生物及其使用方法
公开(公告)号：US4419355A
公开(公告)日：1983-12-06
申请号：US283971
申请日：1981-07-16
申请人： Ibolya Kosoczky , Eva Toncsev, nee Ravasz , Pal Benko , Laszlo Pallos , Lujza Petocz , Sandor Batori , Gyorgy Hajos , Andras Messmer , Katalin Grasser
发明人： Ibolya Kosoczky , Eva Toncsev, nee Ravasz , Pal Benko , Laszlo Pallos , Lujza Petocz , Sandor Batori , Gyorgy Hajos , Andras Messmer , Katalin Grasser
IPC分类号： C07D471/04 , A61K31/53 , A61P25/24 , A61P25/26 , C07D253/10 , C07D487/04 , C07D253/08
CPC分类号： C07D487/04
摘要： The invention relates to new condensed as-triazine derivatives of the general formula (I) ##STR1## wherein Z represents a buta-1,3-dienyl group or a group of the formula (a), (b), (c) or (d) ##STR2## R.sub.1 denotes a C.sub.1-10 alkyl group, an oxo group or a C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) group optionally substituted by one or more identical or different substituents selected from the group consisting of amino, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,R.sub.2 stands for hydrogen, C.sub.1-10 alkyl or amino,R.sub.3 represents hydrogen, C.sub.1-10 alkyl or C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) optionally substituted by one or more identical or different substituents selected from the group consisting of nitro, amino, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,X.sup.- denotes an anion, andn is 0 or 1,with the proviso that if n is O, R.sub.1 is other than an oxo group and R.sub.1 ' and R.sub.2 ' form together a double bond, and with the further provisos that if n is 1, R.sub.1 represents an oxo group and the symbols R.sub.1 ' and R.sub.2 ' are not present, and if Z is a buta-1,3-dienyl group and R.sub.1 denotes an oxo group, R.sub.3 is other than unsubstituted phenyl.The new compounds of the general formula (I) can be prepared by cyclizing the compounds of the general formula (II) or (V), wherein R.sub.1, Z, R.sub.3 and X.sup.- have the above defined meanings, R.sub.4 is a leaving group and R.sub.7 represents hydrogen or C.sub.1-10 alkyl.The new compounds of the general formula (I) possess a valuable antidepressant effect and can advantageously be used in the therapy.
摘要翻译：本发明涉及通式（I）的新的缩合的三嗪衍生物，其中Z代表丁-1,3-二烯基或式（a），（b），（ c）或（d）R1表示任选被一个或多个相同的C 1-6烷基，氧代基或C 6-10芳基或C 6-10芳基 - （C 1-3烷基）或选自氨基，硝基，C 1-6烷基，C 1-6烷氧基，羟基和卤素的不同取代基，R 2代表氢，C 1-10烷基或氨基，R 3表示氢，C 1-10烷基或C 6- 芳基或任选被一个或多个相同或不同的选自硝基，氨基，C 1-6烷基，C 1-6烷氧基，羟基和卤素的取代基取代的芳基或C 6-10芳基 - （C 1-3烷基）表示阴离子，n为0或1，条件是如果n为O，则R1不是氧代基，R1'和R2'一起形成双键，另外条件是，如果n为1， R1代表氧代基团， mbols R1'和R2'不存在，并且如果Z是丁-1,3-二烯基并且R 1表示氧代基，则R 3不是未取代的苯基。通式（I）的新化合物可以通过使通式（II）或（V）的化合物环化来制备，其中R1，Z，R3和X具有上述定义，R4是离去基团， R 7表示氢或C 1-10烷基。通式（I）的新化合物具有有价值的抗抑郁作用，可有利地用于治疗。

4. 发明授权

US4871846A Process for the preparation of condensed as-triazine derivatives 失效
标题翻译：缩合的三嗪衍生物的制备方法
公开(公告)号：US4871846A
公开(公告)日：1989-10-03
申请号：US43600
申请日：1987-04-28
申请人： Sandor Batori , Gyorgy Hajos , Andras Messmer , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly
发明人： Sandor Batori , Gyorgy Hajos , Andras Messmer , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly
IPC分类号： C07D215/12 , C07D215/58 , C07D217/16 , C07D217/18 , C07D471/04
CPC分类号： C07D471/04 , C07D215/58 , C07D217/18
摘要： A process for the preparation of condensed as-triazinium derivatives of the formula I ##STR1## and isomers thereof, wherein R.sub.1 inter alia is an alkyl group, R.sub.2 inter alia is hydrogen or an alkyl group and R.sub.3 is hydrogen and where Z is a group of the formula a or b ##STR2## which comprises reacting a compound of the formula II ##STR3## where Y is a group of the formula c or d ##STR4## with a compound of the formula IIaNH.sub.2 --CO--R.sub.2 (IIa)in the presence of a dehydrating agent. The advantage of the process is that it consists of fewer reaction steps and provides higher yields than the known methods. The compounds of formula I are pharmaceutically active known derivatives.
摘要翻译：一种制备式I（I）的缩合的三嗪鎓衍生物及其异构体的方法，其中R1特别是烷基，R 2特别是氢或烷基，R 3是氢，并且其中Z 是式a或b的基团（a）（b），其包括使式II的化合物（II）其中Y是式c的基团或d （c）在脱水剂存在下，用式IIa NH 2 -CO-R 2（IIa）化合物与（d）化合物反应。该方法的优点在于其由较少的反应步骤组成，并提供比已知方法更高的产率。式I的化合物是药学活性的已知衍生物。

5. 发明授权

US4753938A Condensed as-triazine derivatives 失效
标题翻译：浓缩的三嗪衍生物
公开(公告)号：US4753938A
公开(公告)日：1988-06-28
申请号：US787704
申请日：1985-10-15
申请人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
发明人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/53 , A61P9/06 , A61P25/02 , A61P25/24 , A61P29/00 , A61P43/00 , C07D471/04 , C07D253/08
CPC分类号： C07D471/04
摘要： The invention relates to new compounds of the general Formula I ##STR1## and isomers thereof wherein R.sub.1 is C.sub.1-10 alkyl, C.sub.3-6 cycloalkyl or phenyl, naphthyl or phenyl-(C.sub.1-4 alkyl), wherein the aryl ring of the three latter groups may optionally bear one or more halogen, nitro, trifluoromethyl, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.2 stands for hydrogen, halogen, hydroxy, oxo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or naphthyl, wherein the two latter groups may optionally bear one or more halogen, nitro, trifluoromethyl, amino, hydroxy, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy substituent(s);R.sub.3 represents hydrogen, hydroxy or C.sub.1-4 alkoxy;Z is buta-1,3-dienyl or a group of the general Formula (a) ##STR2## or (b) ##STR3## and X is hydrogen or halogen.The compounds of the general Formula I possess useful pharmacological properties, particularly antidepressant and antiarrhythmial effect.
摘要翻译：本发明涉及通式I（I）的新化合物及其异构体，其中R 1为C 1-10烷基，C 3-6环烷基或苯基，萘基或苯基 - （C 1-4烷基），其中芳基环三个后面的基团可任选地带有一个或多个卤素，硝基，三氟甲基，氨基，羟基，C 1-4烷基和/或C 1-4烷氧基取代基; R2代表氢，卤素，羟基，氧代，C1-4烷基，C1-4烷氧基，苯基或萘基，其中后两个基团可任选地具有一个或多个卤素，硝基，三氟甲基，氨基，羟基，C 1-4烷基和/或C 1-4烷氧基取代基; R3表示氢，羟基或C1-4烷氧基; Z是丁-1,3-二烯基或通式（a）的基团（a）或（b）图像（b），X是氢或卤素。通式I的化合物具有有用的药理学特性，特别是抗抑郁药和抗心律失常作用。

6. 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。

7. 发明授权

US07812031B2 Pyrimidine derivatives as orexin receptor antagonists 有权
标题翻译：嘧啶衍生物作为食欲素受体拮抗剂
公开(公告)号：US07812031B2
公开(公告)日：2010-10-12
申请号：US11463825
申请日：2006-08-10
申请人： Peter Aranyi , Maria Balogh , Sandor Batori , Judit Bence , Michel Finet , Zoltan Kapui , Christophe Philippo , Tibor Szabo , Zoltan Szlavik , Zsuzsanna Tomoskozi , Katalin Urban-Szabo , Olivier Venier
发明人： Peter Aranyi , Maria Balogh , Sandor Batori , Judit Bence , Michel Finet , Zoltan Kapui , Christophe Philippo , Tibor Szabo , Zoltan Szlavik , Zsuzsanna Tomoskozi , Katalin Urban-Szabo , Olivier Venier
IPC分类号： C07D239/42 , A61K31/505 , A61P43/00
CPC分类号： C07D401/14 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/06
摘要： The present invention relates to substituted pyrimidine compounds of formula I useful as orexin receptor antagonists. The invention also relates to pharmaceutical compositions containing said compounds.
摘要翻译：本发明涉及用作食欲素受体拮抗剂的式I的取代嘧啶化合物。本发明还涉及含有所述化合物的药物组合物。

8. 发明授权

US07419977B2 Imidazoquinoline derivatives as adenosine A3 receptor ligands 失效
标题翻译：咪唑喹啉衍生物作为腺苷A3受体配体
公开(公告)号：US07419977B2
公开(公告)日：2008-09-02
申请号：US11130429
申请日：2005-05-16
申请人： Peter Aranyi , Laszlo Balazs , Maria Balogh , Sandor Batori , Lajos T. Nagy , Geza Timari , Kinga Boer , Zoltan Kapui , Endre Mikus , Katalin Gerber , Judit Vargane Szeredi , Katalin Urban Szabo , Erzsebet Walcz
发明人： Peter Aranyi , Laszlo Balazs , Maria Balogh , Sandor Batori , Lajos T. Nagy , Geza Timari , Kinga Boer , Zoltan Kapui , Endre Mikus , Katalin Gerber , Judit Vargane Szeredi , Katalin Urban Szabo , Erzsebet Walcz
IPC分类号： A61K31/5377 , C07D411/14
CPC分类号： C07D471/04 , A61K31/415
摘要： This invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Z, m, n, o, p and r are as defined herein, its preparation, pharmaceutical composition and use as an adenosine A3 receptor ligand preferably an antagonist.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8，R 9，R 9， R 10，X，Z，m，n，o，p和r如本文所定义，其制备，药物组合物和用作腺苷A 3 >受体配体优选为拮抗剂。

9. 发明授权

US07348327B2 Compounds 失效
标题翻译：化合物
公开(公告)号：US07348327B2
公开(公告)日：2008-03-25
申请号：US10507005
申请日：2003-03-04
申请人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
发明人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
IPC分类号： C07D401/04 , C07D403/04 , C07D211/06 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/501
CPC分类号： C07D451/04 , C07D207/16 , C07D211/58 , C07D401/04 , C07D401/14 , C07D405/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/14
摘要： The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
摘要翻译：本发明涉及含有氟原子的新的具有通式（I）的DPP-IV酶抑制剂。

10. 发明授权

US08338411B2 Compounds 有权
标题翻译：化合物
公开(公告)号：US08338411B2
公开(公告)日：2012-12-25
申请号：US12631139
申请日：2009-12-04
申请人： Edit Susan , Kinga Boer , Zoltan Kapui , Geza Timari , Sandor Batori , Zoltan Szlavik , Endre Mikus , Judit Vargane Szeredi , Michel Finet , Katalin Urban Szabo , Tibor Szabo
发明人： Edit Susan , Kinga Boer , Zoltan Kapui , Geza Timari , Sandor Batori , Zoltan Szlavik , Endre Mikus , Judit Vargane Szeredi , Michel Finet , Katalin Urban Szabo , Tibor Szabo
IPC分类号： A61K31/535 , C07D215/38
CPC分类号： C07D471/04
摘要： The present invention relates to the adenosine A3 receptor ligands of the general formula (I), within them favourably to the antagonists, to their salts, solvates, N-oxides and isomers, to the pharmaceutical compositions containing the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the use of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the preparation of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, as well as to the new intermediates of the general formula (II), (VI), (XI), (XII) and (XV), and to the preparation thereof.
摘要翻译：本发明涉及含有通式（I）的化合物的药物组合物，其通式（I）的腺苷A 3受体配体，其有利于拮抗剂，其盐，溶剂合物，N-氧化物和异构体，），它们的盐，溶剂合物，N-氧化物和异构体，通式（I）的化合物，其盐，溶剂合物，N-氧化物和异构体用于制备通式（I ），它们的盐，溶剂合物，N-氧化物和异构体，以及通式（II），（VI），（XI），（XII）和（XV）的新中间体及其制备。

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