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1. 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。

2. 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。

3. 发明授权

US4324894A Aminoisoquinoline derivatives 失效
标题翻译：氨基异喹啉衍生物
公开(公告)号：US4324894A
公开(公告)日：1982-04-13
申请号：US138843
申请日：1980-04-10
申请人： Pal Benko , Andras Gelleri , Gyorgy Hajos , Andras Messmer , Laszlo Pallos , Lujza Petocz , Ibolya Kosoczky , Katalin Grasser , Peter Gorog , Eniko Szirt nee Kiszelly
发明人： Pal Benko , Andras Gelleri , Gyorgy Hajos , Andras Messmer , Laszlo Pallos , Lujza Petocz , Ibolya Kosoczky , Katalin Grasser , Peter Gorog , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61P25/00 , A61P25/04 , C07D217/22 , C07D217/24 , C07D401/12 , C07D413/04 , C07D403/14
CPC分类号： C07D217/22 , C07D217/24
摘要： Novel aminoisoquinoline derivatives of the general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a C.sub.1-4 alkyl group,R.sub.2 represents a hydrogen atom,R.sub.3 represents a hydrogen atom,R.sub.4 represents a morpholinyl group or a piperazinyl group substituted with a pyridyl group, andpharmaceutically acceptable acid addition salts and quaternary derivatives thereof have been prepared. The novel compounds exert narcosis potentiating effects.
摘要翻译：通式（I）的新型氨基异喹啉衍生物其中R 1表示氢原子或C 1-4烷基，R 2表示氢原子，R 3表示氢原子，R 4表示吗啉基或哌嗪基已经制备了被吡啶基取代的基团，以及其药学上可接受的酸加成盐和其季衍生物。新型化合物发挥麻醉加强作用。

4. 发明授权

US4994448A Condensed quinolinium and isoquinolinium derivatives 失效
标题翻译：浓缩的喹啉和异喹啉衍生物
公开(公告)号：US4994448A
公开(公告)日：1991-02-19
申请号：US251445
申请日：1988-09-30
申请人： Andras Messmer , Gyorgy Hajos , Zsuzsa Juhasz nee Riedl , Pal Benko , Laszlo Pallos , Lujza Petocz , Eniko Szirt nee Kiszelly , Gabor Gigler , Istvan Gyertyan , Maria Hegedus
发明人： Andras Messmer , Gyorgy Hajos , Zsuzsa Juhasz nee Riedl , Pal Benko , Laszlo Pallos , Lujza Petocz , Eniko Szirt nee Kiszelly , Gabor Gigler , Istvan Gyertyan , Maria Hegedus
IPC分类号： A61K31/53 , A61P25/02 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , C07D471/04
CPC分类号： C07D471/04
摘要： The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-4 alkyl or aralkyl; andR.sub.2 represents hydroxy; orR.sub.1 and R.sub.2 together form a valency bond;R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl, amino, alkylthio or a group of the Formula --NR.sub.7 R.sub.8 in which R.sub.7 and R.sub.8 may be the same or different and stand for hydrogen, C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl or di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl or together with the nitrogen atom they are attached to form a 6-membered heterocyclic ring which may optionally contain a further nitrogen, oxygen or sulfur atom; orR.sub.2 and R.sub.3 together form an oxo (.dbd.O) or thixo (.dbd.S) group;R.sub.4 represents hydrogen, C.sub.1-4 alkyl or phenyl which may optionally bear one or two halogen or nitro substituent(s);Z is a group of the Formula (a) or (b) ##STR2## A.sup.- represents an anion) and isomers thereof possess useful local anaesthetic, antidepressant, tranquillo-sedative and smooth muscle relaxant properties accompanied by a weaker analgesic effect and are useful in therapy.
摘要翻译：通式I的新化合物Ⅰ（其中R1代表C1-4烷基或芳烷基，R2代表羟基;或R1和R2一起形成价键; R3是氢，C1-4烷基，C1- 烷氧基，苯基，氨基，烷硫基或式-NR7R8的基团，其中R 7和R 8可以相同或不同，代表氢，C 1-4烷基，苯基-C 1-4烷基，羟基-C 1-4烷基或二 - （C 1-4烷基） - 氨基-C 1-4烷基或与它们连接的氮原子一起形成可任选地含有另外的氮，氧或硫原子的6元杂环;或R 2和R 3 一起形成氧代（= O）或触变（= S）基团; R4代表氢，C1-4烷基或苯基，其可任选地带有一个或两个卤素或硝基取代基; Z是式（a ）或（b）和A-表示阴离子）及其异构体具有有用的局部麻醉剂，抗抑郁药，镇痛镇痛和平滑肌松弛剂性质，伴随较弱的镇痛剂 c效应，可用于治疗。

5. 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。

6. 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。

7. 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。

8. 发明授权

US4316022A Benzo-as-triazine derivatives 失效
标题翻译：苯并三嗪衍生物
公开(公告)号：US4316022A
公开(公告)日：1982-02-16
申请号：US135143
申请日：1980-03-28
申请人： Gyorgy Hajos , Andras Messmer , Pal Benko , Lujza Petocz , Peter Gorog , Ibolya Kasoczky
发明人： Gyorgy Hajos , Andras Messmer , Pal Benko , Lujza Petocz , Peter Gorog , Ibolya Kasoczky
IPC分类号： A61K31/53 , A61K31/5513 , A61P23/00 , A61P29/00 , C07D249/08 , C07D253/10 , C07D487/04 , C07D487/14 , C07D401/14 , C07D403/14
CPC分类号： C07D487/04 , C07D487/14
摘要： The invention relates to new benzo-as-triazine derivatives of the formulae (I) and (Ia) and pharmaceutically acceptable acid addition salts thereof, ##STR1## wherein R.sub.1 and R.sub.2 each represent hydrogen, a C.sub.1-20 alkylcarbonyl group, a phenylcarbonyl or phenyl-(C.sub.1-4 alkyl)-carbonyl group having optionally one or more halogen, hydroxy or C.sub.1-3 alkoxy substituents which may be the same or different, furthermore a pyridylcarbonyl, a pyrazinylcarbonyl, a furylcarbonyl, a chloroacetyl or a C.sub.1-4 alkoxycarbonyl group, orR.sub.1 and R.sub.2 may form, together with the adjacent nitrogen atoms, a pyrazole ring having optionally a C.sub.1-6 alkyl substituent in position 4,with the proviso that one of R.sub.1 and R.sub.2 is always different from hydrogen,R.sub.3 stands for hydrogen, mercapto group, a C.sub.1-4 alkylmercapto group, amino group, a C.sub.1-4 alkylamino group, a piperazino group having optionally an N-alkyl or 2-pyridyl substituent, a morpholino group or a piperidino group, andR.sub.4 stands for hydrogen, halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy group.The compounds of the formulae (I) and (Ia) are prepared by acylating the respective 2,4,5-unsubstituted 4,5-dihydro-benzo-as-triazine derivatives.The new compounds of the formulae (I) and (Ia) possess analgesic, antiphlogistic and narcosis-potentiating effects.
摘要翻译：本发明涉及式（I）和（Ia）的新的苯并三嗪衍生物及其药学上可接受的酸加成盐，其中R 1和R 2各自代表氢， C1-20烷基羰基，具有任选一个或多个卤素的苯基羰基或苯基 - （C 1-4烷基） - 羰基，可以相同或不同的羟基或C 1-3烷氧基取代基，此外，吡啶基羰基，吡嗪基羰基，呋喃基羰基，氯乙酰基或C 1-4烷氧基羰基，或者R 1和R 2可以与相邻的氮原子一起形成在4位具有任选的C 1-6烷基取代基的吡唑环，条件是R1和R2之一总是不同于氢，R3代表氢，巯基，C1-4烷基巯基，氨基，C1-4烷基氨基，任选具有N-烷基或2-吡啶基取代基的哌嗪基，吗啉代基或哌啶子基，R4代表氢，卤素， C 1-4烷基或C 1-4烷氧基。式（I）和（Ia）的化合物通过酰化各自的2,4,5-未取代的4,5-二氢 - 苯并 - 三嗪衍生物来制备。式（I）和（Ia）的新化合物具有镇痛，消炎和麻醉增效作用。

9. 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。

10. 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。

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