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21. 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。

22. 发明授权

US4621101A Pharmaceutical compositions with antianginal activity 失效
标题翻译：具有抗心绞痛活性的药物组合物
公开(公告)号：US4621101A
公开(公告)日：1986-11-04
申请号：US751623
申请日：1985-07-02
申请人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Zsuzsanna Orr
发明人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Zsuzsanna Orr
IPC分类号： A61K31/15 , A61P43/00 , C07C251/38
CPC分类号： C07C251/58 , C07C2101/14 , C07C2101/18
摘要： The invention relates to pharmaceutical compositions possessing valuable antianginal activity. These compositions show higher activity and more favorable therapeutic indices than the reference compound Prenylamine. Preparation of different kinds of pharmaceutical compositions, such as tablets, dragees, capsules and injectable solutions, containing compounds of general formula (I) ##STR1## or their acid addition salts as active ingredients, is disclosed, wherein in formula (I)R is phenyl or 4-chlorophenyl;R.sup.1 and R.sup.2 each represent hydrogen, methyl or isopropyl;R.sup.3 and R.sup.4 are hydrogen, or together form a chemical bond;n is an integer from 4 to 6;A means trimethylene, if n is 4 or 6; or ethylene, if n is 5.
摘要翻译：本发明涉及具有有价值的抗心绞痛活性的药物组合物。这些组合物显示比参考化合物Prenylamine更高的活性和更有利的治疗指数。公开了含有通式（I）化合物或其酸加成盐作为活性成分的不同种类的药物组合物如片剂，硫化物，胶囊和可注射溶液的制备，其中在式（I）中R是苯基或4-氯苯基; R1和R2各自表示氢，甲基或异丙基; R3和R4是氢，或一起形成化学键; n为4-6的整数; 如果n为4或6，则表示三亚甲基; 或乙烯，如果n为5。

23. 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。

24. 发明授权

US5276030A Triazolyl thioamide derivates 失效
标题翻译：三唑基硫代酰胺衍生物
公开(公告)号：US5276030A
公开(公告)日：1994-01-04
申请号：US755219
申请日：1991-09-09
申请人： Josef Barkoczy , Josef Reiter , Laszlo Pongo , Lujza Petocz , Marton Fekete , Frigyes Gorgenyi , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan
发明人： Josef Barkoczy , Josef Reiter , Laszlo Pongo , Lujza Petocz , Marton Fekete , Frigyes Gorgenyi , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan
IPC分类号： A61K31/41 , A61K31/4196 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61P13/06 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P29/00 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14
CPC分类号： C07D249/14
摘要： The invention relates to novel triazolyl thioamides of the general formula (I), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s), or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.1-4 alkyl bearing a heterocyclic group containing a nitrogen atom, with the proviso that if Q represents methylthio, dimethylamino, piperidino or morpholino, Y is other than benzyl,and pharmaceutically acceptable acid additional salts thereof.Furthermore the invention relates to a process for preparing these compounds.The compounds according to the invention possess tranquillant, antidepressant, spasmolytic, antiinflammatory, analgesic and antiperistaltic effects.
摘要翻译：本发明涉及通式（I）的新型三唑基硫代酰胺，其中Q表示氢或任选带有一个或多个C 1-4烷基取代基的杂环基或式SR1的基团，其中R 1 代表包含1至6个碳原子的直链或支链烷基或式NR2R3基团，其中R2和R3各自表示氢，直链或支链C 1-4烷基或C 2-6烯基，Y 表示具有一个或多个羟基或C 1-4烷氧基取代基的C 1-4烷基，任选地在苯环上带有一个或多个C 1-4烷氧基的苯基 - （C 1-4烷基）或苯氧基 - （ C 1-4烷基），其任选在苯环上被带有含氮原子的杂环基的C 1-4烷基取代，条件是如果Q表示甲硫基，二甲基氨基，哌啶子基或吗啉代，则Y不是苄基，其酸加成盐。此外，本发明涉及一种制备这些化合物的方法。根据本发明的化合物具有镇静，抗抑郁，解痉，抗炎，止痛和抗静脉作用。

25. 发明授权

US5240918A 2-(substituted imino)-thiazolidines and process for the preparation thereof 失效
标题翻译： 2-（取代的亚氨基） - 噻唑啉及其制备方法
公开(公告)号：US5240918A
公开(公告)日：1993-08-31
申请号：US857067
申请日：1992-03-24
申请人： Karoly Lempert , Gyula Hornyak , Jozsef Fetter , Antal Feller , Klara Gaso , Gabor Gigler , Laszlo Kapolnai , Lujza Petocz , Katalin Szemeredi , Marton Fekete
发明人： Karoly Lempert , Gyula Hornyak , Jozsef Fetter , Antal Feller , Klara Gaso , Gabor Gigler , Laszlo Kapolnai , Lujza Petocz , Katalin Szemeredi , Marton Fekete
IPC分类号： C07D277/18
CPC分类号： C07D277/18
摘要： The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.1-6 alkenyl optionally carrying a halogen or a di-(C.sub.1-4 alkyl)-amino substituent; orZ and R.sup.5 together stand for a trivalent nitrogen atom, with the proviso that if Z denotes a substituted imino group, R.sup.5 stands for C.sub.1-4 alkylthio, and if R.sup.5 is C.sub.1-4 alkylthio, Z represents a substituted imino, and with the further proviso that if Z denotes sulfur, R.sup.5 is other than hydrogen or C.sub.1-4 alkyl,and possess valuable antianginal and analgesic properties.
摘要翻译：本发明涉及新的2-（取代的亚氨基） - 噻唑烷，其制备方法，包含该方法的药物组合物，所述2-（取代的亚氨基）噻唑烷用于治疗疾病和用于制备药物适用于治疗疾病的组合物。本发明提供的新的2-（取代亚氨基） - 噻唑烷衍生物对应于通式（I），其中R 1和R 2各自表示卤素，硝基，C 1-4烷氧基或C 1-4烷基，其可以任选地带有一个或多个卤素取代基，R 3和R 4各自表示氢或C 1-4烷基，Z表示氧，硫或亚氨基，后者被C 1-6烷基或C 1-6 烯基，R5代表氢，C1-4烷基，C1-4烷硫基或基团-NH-R，其中R表示C1-6烷基，芳基，芳烷基或任选携带卤素或二（C 1-4烷基） - 氨基取代基; 或Z和R5一起代表三价氮原子，条件是如果Z表示取代的亚氨基，则R5表示C1-4烷硫基，如果R5是C1-4烷硫基，则Z表示取代的亚氨基，并且与进一步的条件是，如果Z表示硫，R5不是氢或C1-4烷基，并且具有有价值的抗心绞痛和止痛特性。

26. 发明授权

US5175163A Triazolyl thioamide derivates 失效
标题翻译：三唑氧化物衍生物
公开(公告)号：US5175163A
公开(公告)日：1992-12-29
申请号：US617126
申请日：1990-11-21
申请人： Jozsef Barkoczy , Jozsef Reiter , Laszlo Pongo , Lujza Petocz , Marton Fekete , Frigyes Gorgenyi , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan
发明人： Jozsef Barkoczy , Jozsef Reiter , Laszlo Pongo , Lujza Petocz , Marton Fekete , Frigyes Gorgenyi , Gabor Gigler , Istvan Gacsalyi , Istvan Gyertyan
IPC分类号： A61K31/41 , A61K31/4196 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61P13/06 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P29/00 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14
CPC分类号： C07D249/14
摘要： The invention relates to novel triazolyl thioamides of the general formula (I), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s), or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl optionally bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.1-4 alkyl bearing a heterocyclic group containing a nitrogen atom,and pharmaceutically acceptable acid addition salts thereof.Furthermore the invention relates to a process for preparing these compounds.The compounds according to the invention possess tranquillant, antidepressant, spacmolytic, antiinflammatory, analgesic and antiperistaltic effects.
摘要翻译：本发明涉及通式（I）的新型三唑基硫代酰胺，其中Q表示氢或任选带有一个或多个C 1-4烷基取代基的杂环基或式SR 1的基团其中R1代表包括1至6个碳原子的直链或支链烷基或式NR2R3基团，其中R2和R3各自表示氢，直链或支链C 1-4烷基或C 2-6烯基基团，Y表示任选带有一个或多个羟基或C 1-4烷氧基取代基的C 1-4烷基，任选地在苯环上带有一个或多个C 1-4烷氧基的苯基 - （C 1-4烷基）或在苯环上被含有含有氮原子的杂环基的C 1-4烷基任选取代的苯氧基 - （C 1-4烷基）及其药学上可接受的酸加成盐。此外，本发明涉及一种制备这些化合物的方法。根据本发明的化合物具有镇静，抗抑郁，间质，抗炎，止痛和抗静脉作用。

27. 发明授权

US4727074A 2-(phenylmethylene)-1-(diaminoalkoxy) cycloalkanes and their pharmaceutical uses 失效
标题翻译： 2-（苯基亚甲基）-1-（二氨基烷氧基）环烷烃及其药物用途
公开(公告)号：US4727074A
公开(公告)日：1988-02-23
申请号：US578286
申请日：1984-02-08
申请人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
发明人： Zoltan Budai , Tibor Mezei , Aranka Lay nee Konya , Lujza Petocz , Katalin Grasser , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/15 , A61P9/06 , A61P23/00 , A61P25/04 , C07C67/00 , C07C239/00 , C07C251/44 , C07C251/58 , C07D295/088 , A61K31/495 , A61K31/205 , C07C131/02
CPC分类号： C07D295/088
摘要： The invention relates to selected stereoisomers having the E, E or E, Z configuration and within the Formula (I) ##STR1## wherein N is 2-4, A is alkylene or 2 or 3 carbon atoms, R is phenyl or substituted phenyl and R.sup.1 and R.sup.2 are lower alkyl, or, together with the carbon to which attached, form a heterocyclic ring; and pharmaceutically acceptable acid addition salts thereof, a process for their preparation and pharmaceutical compositions comprising the same.The compounds of the general formula (I) can be used in therapy due to their narcosis potentiating, analgesic and antiarrhythmial effect.
摘要翻译：本发明涉及具有E，E或E，Z构型的选定的立体异构体，并且在其中N为2-4的式（I）中，A为亚烷基或2或3个碳原子，R为苯基或取代的苯基，R 1和R 2为低级烷基，或与连接的碳一起形成杂环; 及其药学上可接受的酸加成盐，其制备方法和包含其的药物组合物。通式（I）的化合物可以用于治疗，因为它们具有麻醉增效，止痛和抗心律失常作用。

28. 发明授权

US4424351A Pyrido�3,4-e!-as-triazines 失效
标题翻译：吡啶并[3,4-e] -as-三嗪
公开(公告)号：US4424351A
公开(公告)日：1984-01-03
申请号：US123807
申请日：1980-02-22
申请人： Pal Benko , Gyo/ rgyi nee Lax Kovanyi , Judit nee Gergely Timar , Maria nee Lakatos Sigmond , Lujza Petocz , Peter Go/ ro/ g , Ibolya Kosoczky , Eniko nee Kiszelly Szirt , Hristone Toncsev
发明人： Pal Benko , Gyo/ rgyi nee Lax Kovanyi , Judit nee Gergely Timar , Maria nee Lakatos Sigmond , Lujza Petocz , Peter Go/ ro/ g , Ibolya Kosoczky , Eniko nee Kiszelly Szirt , Hristone Toncsev
IPC分类号： A61K31/53 , A61P25/04 , A61P29/00 , C07D471/04
CPC分类号： C07D471/04
摘要： Acylated pyrido �3,4-e!-as-triazines of the formula (I), ##STR1## wherein R.sub.1 stands for alkyl, alkoxy, haloalkyl, furyl, pyridyl, phenyl, phenyl-(C.sub.1-4 alkyl) or phyenyl-(C.sub.2-4 alkenyl) optionally substituted. R.sub.2 stands for hydrogen or a group of the formula R.sub.1 --CO--, R.sub.3 stands for hydrogen, a phenyl group or a naphthy6l group optionally substituted, or a phenyl-(C.sub.1-4 alkyl) group, pyridyl group or a C.sub.1-20 alkyl group, and R.sub.4 stands for hydrogen or a group of the formula R.sub.1 --CO--, and R.sub.5 forms together with R.sub.2 or R.sub.4 a valence bond, wherein R.sub.2 or R.sub.4 taking part in forming said valence bond may not have the above meaning, and pharmaceutically acceptable acid addition salts thereof, which are prepared by reacting a pyrido �3,4-e!-as-triazine of the formula (II) or an acid addition salt thereof ##STR2## R.sub.6 stands for hydrogen, and R.sub.5 forms together with R.sub. and R.sub.4 a valence bond, with an acylating agent of the formula (III). R.sub.1 --CO--X (III) The compounds exert favourable effects on the central nervous system, and can be applied primarily as analgesic and antiphlogistic agents.
摘要翻译：式（I）的酰化吡啶并[3,4-e] -as-三嗪，其中R1代表烷基，烷氧基，卤代烷基，呋喃基，吡啶基，苯基，苯基 - （C1-4烷基）或（烯基）（C 2-4烯基）任意取代。 R2代表氢或式R1-CO-的基团，R3代表氢，苯基或任选取代的萘基，或苯基 - （C 1-4烷基）基，吡啶基或C 1-20烷基， R4代表氢或式R1-CO-基团，R5与R2或R4一起形成价键，其中参与形成所述价键的R2或R4可能不具有上述含义，并且其药学上可接受的酸通过使式（II）的吡啶并[3,4-e]-α-三嗪或其酸加成盐反应制备的加成盐，其中R6代表氢，R5与兰德R4是价键，具有式（III）的酰化剂。 R1-CO-X（III）该化合物对中枢神经系统具有有利的作用，可主要用作镇痛药和消炎药。

29. 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。

30. 发明授权

US4342762A Basic ethers and pharmaceutical compositions containing the same 失效
标题翻译：碱性醚和含有它们的药物组合物
公开(公告)号：US4342762A
公开(公告)日：1982-08-03
申请号：US215154
申请日：1980-12-11
申请人： Zoltan Budai , Laszlo Magdanyi , Aranka Lay nee Konya , Tibor Mezei , Katalin Grasser , Lujza Petocz , Ibolya Kosoczky
发明人： Zoltan Budai , Laszlo Magdanyi , Aranka Lay nee Konya , Tibor Mezei , Katalin Grasser , Lujza Petocz , Ibolya Kosoczky
IPC分类号： A61K31/13 , A61K31/135 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/431 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , A61P29/00 , C07C67/00 , C07C213/00 , C07C217/00 , C07C217/04 , C07C217/12 , C07C217/26 , C07C217/52 , C07D295/03 , C07D295/08 , C07D295/088 , C07D333/16 , A61K31/54 , A61K31/445 , C07D245/02
CPC分类号： C07D295/088 , C07D333/16
摘要： The invention relates to novel basic ethers of the general formula /I/ and pharmaceutically acceptable acid addition salts and quaternary salts thereof, ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and represent a C.sub.1-5 alkyl group or a C.sub.3-6 cycloalkyl group or they form, together with the adjacent nitrogen atom, a heterocyclic ring containing 4-7 carbon atoms and optionally a further hetero atom, e.g. an oxygen, sulfur or nitrogen atom, and this latter may be optionally substituted by a C.sub.1-3 alkyl, benzyl or phenyl group,R represents a phenyl, phenyl-/C.sub.1-3 alkyl/ or thienyl group optionally substituted by one or more halogen or C.sub.1-3 alkoxy substituent/s/,A represents a C.sub.2-5 straight or branched alkylene chain, and represents a valence bond of .alpha. or .beta. configuration.The new compounds of the general formula /I/ possess valuable anticonvulsive, motility inhibiting, hexobarbital narcose potentiating and analgesic effects, which are, in case of certain compounds, complemented by week antiserotonine, gastro-intestinal-tract inhibiting and antiinflammatory effects, and can be applied to advantage in the therapy.
摘要翻译：本发明涉及通式I I和其药学上可接受的酸加成盐和季盐的新型碱性醚，其中R 1和R 2可以相同或不同，表示C 1-5烷基或与相邻的氮原子一起形成含有4-7个碳原子和任选的另外的杂原子的杂环，例如氧，硫或氮原子，并且后者可任选被C 1-3烷基，苄基或苯基取代，R表示任选被一个或多个卤素取代的苯基，苯基 - / C 1-3烷基或噻吩基或C 1-3烷氧基取代基/ s，A表示C 2-5直链或支链亚烷基链，并且表示α或β构型的价键。新化合物的通式I /具有有价值的抗惊厥，运动抑制，六硼麻醉加强镇痛作用，在某些化合物的情况下，辅以一周抗塞冬糖，胃肠道抑制和抗炎作用，并且可以适用于治疗的优势。

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