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1. 发明授权

US3963735A Acylated 2-aminothiazole derivatives 失效
标题翻译：酰化2-氨基噻唑衍生物
公开(公告)号：US3963735A
公开(公告)日：1976-06-15
申请号：US518732
申请日：1974-10-29
申请人： Lajos Farkas , Endre Kasztreiner , Ferenc Andrasi , Jozsef Borsi , Istvan Elekes , Istvan Polgari
发明人： Lajos Farkas , Endre Kasztreiner , Ferenc Andrasi , Jozsef Borsi , Istvan Elekes , Istvan Polgari
IPC分类号： C07D277/20 , C07D277/46 , C07D295/14 , C07D417/04 , C07D417/14 , C07D213/56
CPC分类号： C07D417/04 , C07D277/46 , C07D417/14 , Y10S514/927
摘要： New acylated 2-aminothiazole derivatives of the general formula (I), ##SPC1##whereinR.sup.1 stands for phenyl group or a pyridyl group,R.sup.2 stands for hydrogen or lower alkyl,R.sup.3 stands for hydrogen, a lower alkyl group or benzyl group, andR.sup.4 and R.sup.5 each represent hydrogen, a C.sub.1-8 alkyl group, allyl group, a hydroxyalkyl group, a C.sub.3-6 cycloalkyl group, .beta.-dimethylaminoethyl group, .beta.-diethylaminoethyl group, benzyl group, 2-furylmethyl group, or a phenyl group having optionally a halogen, methyl, methoxy or trifluoromethyl substituent, orR.sup.4 and R.sup.5 may form, together with the adjacent nitrogen atom, a 5 to 8 membered polymethyleneimino group, morpholino group, piperazino group, N-methylpiperazino group or N-phenylpiperazino group, the compounds of formula I are anticholinergics.
摘要翻译：新的通式（I）的酰化2-氨基噻唑衍生物，其中R1代表苯基或吡啶基，R2代表氢或低级烷基，R3代表氢，低级烷基或苄基，R4和R5 各自表示氢，C1-8烷基，烯丙基，羟基烷基，C3-6环烷基，β-二甲基氨基乙基，β-二乙基氨基乙基，苄基，2-呋喃基甲基或任选具有卤素，甲基，甲氧基或三氟甲基取代基，或者R4和R5可以与相邻的氮原子一起形成5至8元多亚甲基亚氨基，吗啉代基，哌嗪基，N-甲基哌嗪基或N-苯基哌嗪基，配方I是抗胆碱能药。

2. 发明授权

US4308278A Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives 失效
标题翻译：厌氧性4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑烷酮衍生物
公开(公告)号：US4308278A
公开(公告)日：1981-12-29
申请号：US90450
申请日：1979-11-01
申请人： Geza Schneider , Ferenc Andrasi , Pal Berzsenyi , Arpad Lazar , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Geza Schneider , Ferenc Andrasi , Pal Berzsenyi , Arpad Lazar , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： A61K31/415 , A61K31/4166 , A61P1/00 , A61P3/04 , C07C45/71 , C07D233/32 , C07D233/34 , C07D233/38 , C07D233/78
CPC分类号： C07C255/00 , C07C45/71 , C07D233/32 , C07D233/38 , C07D233/78 , Y10S514/91
摘要： 4-[(3,4-Dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives having the formula I ##STR1## wherein R.sup.1 stands for a cycloalkyl group containing from 3 to 6 carbon atoms or benzyl group;R.sup.2 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.3 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.4 stands for hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms or an alkoxycarbonyl group containing from 1 to 4 carbon atoms; andR.sup.5 stands for hydrogen atom or an alkoxycarbonyl group containing from 1 to 4 carbon atoms,are prepared by(a) reducing a hydantoin derivative having the general formula II, wherein R.sup.1 and R.sup.2 are as defined above, with lithium aluminum hydride in a neutral organic solvent, or(b) hydrogenating catalytically an 1,3-dihydro-2H-imidazol-2-one derivative having the general formula III, wherein R.sup.1 and R.sup.3 are as defined above, while the meaning of R.sup.4 is hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, or(c) reacting a carbamate derivative having the general formula IV, wherein R.sup.1 is as defined above, while R.sup.6 stands for an alkyl group containing from 1 to 4 carbon atoms, with an organic or inorganic base.The compounds having the formula I possess valuable therapeutical properties, mainly anorexigenic activity.
摘要翻译： 4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑啉酮衍生物，其具有式I其中R1代表含有3至6个碳原子的环烷基或苄基; R2代表氢原子或含有1至4个碳原子的烷基; R3代表氢原子或含有1至4个碳原子的烷基; R4表示氢原子或含有1至4个碳原子的烷基或含有1至4个碳原子的烷氧基羰基; 并且R5代表氢原子或含有1至4个碳原子的烷氧基羰基，是通过以下步骤制备的：（a）将具有通式II的乙内酰脲衍生物（其中R 1和R 2如上定义）与中性的氢化铝锂有机溶剂，或（b）催化氢化具有通式III的1,3-二氢-2H-咪唑-2-酮衍生物，其中R 1和R 3如上所定义，而R 4的含义是氢原子或烷基含有1至4个碳原子的基团，或（c）使具有通式IV的氨基甲酸酯衍生物与其中R 1如上定义，而R6代表含有1至4个碳原子的烷基，与有机或无机基础。具有式I的化合物具有有价值的治疗性质，主要是厌食症活性。

3. 发明授权

US4835152A 1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H-2,3-b enzodiazepine and acid addition salts thereof same 失效
标题翻译： 1-（4-氨基苯基）-4-甲基-7,8-亚甲二氧基-3,4-二氢-5H-2,3-苯并二氮杂及其酸加成盐
公开(公告)号：US4835152A
公开(公告)日：1989-05-30
申请号：US87341
申请日：1987-08-20
申请人： Jeno Korosi , Tibor Lang , Ferenc Andrasi , Pal Berzsenyi , Peter Botka , Tamas Hamori , Katalin G. Horvath , Jozsef Borsi , Istvan Elekes , Zsuzsanna L. Rihmer
发明人： Jeno Korosi , Tibor Lang , Ferenc Andrasi , Pal Berzsenyi , Peter Botka , Tamas Hamori , Katalin G. Horvath , Jozsef Borsi , Istvan Elekes , Zsuzsanna L. Rihmer
IPC分类号： C07D405/10 , A61K31/55 , A61K31/551 , A61P25/26 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04
摘要： The invention relates to new 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H-2,3-benzodiazepi ne of formula (1), optically active isomers and acid addition salts thereof as well as to pharmaceutical compositions containing these compounds. ##STR1## The new compounds of formula (I) can be prepared by reducing 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine of formula (II) with an inorganic or organic-inorganic and/or complex metal hydride and, if desired, separating the optically active forms of the compound of formula (I) thus-obtained and, if desired, converting the base or bases into acid addition salts or converting the salts into the free bases(s). ##STR2## The new compound of formula (I) possesses significant central nervous effects and can advantageously be used in the therapy.
摘要翻译：本发明涉及式（1）的新的1-（4-氨基苯基）-4-甲基-7,8-亚甲二氧基-3,4-二氢-5H-2,3-苯并二氮杂，旋光异构体和酸加成其盐以及含有这些化合物的药物组合物。（I）式（I）的新化合物可以通过将式（II）的1-（4-氨基苯基）-4-甲基-7,8-亚甲二氧基-5H-2,3-苯并二氮杂与无机或有机 - 无机和/或络合金属氢化物，如果需要，分离由此获得的式（I）化合物的光学活性形式，如果需要，将碱或碱转化为酸加成盐或将盐进入游离碱。（II）式（I）的新化合物具有显着的中枢神经作用，可有利地用于治疗。

4. 发明授权

US4614740A 5H-2,3-benzodiazepine derivatives and pharmaceutical compositions containing the same 失效
标题翻译： 5H-2,3-苯并二氮杂衍生物和含有它们的药物组合物
公开(公告)号：US4614740A
公开(公告)日：1986-09-30
申请号：US759169
申请日：1985-07-26
申请人： Tibor Lang , Jeno Korosi , Ferenc Andrasi , Peter Botka , Tamas Hamori , Pal Berzsenyi , Katalin Goldschmidt , Gabor Zolyomi , Istvan Elekes , Zsuzsanna Lang nee Rihmer
发明人： Tibor Lang , Jeno Korosi , Ferenc Andrasi , Peter Botka , Tamas Hamori , Pal Berzsenyi , Katalin Goldschmidt , Gabor Zolyomi , Istvan Elekes , Zsuzsanna Lang nee Rihmer
IPC分类号： A61K31/55 , A61P21/02 , A61P25/20 , C07D243/02 , C07D243/04 , C07D243/10 , C07D491/04 , C07D491/056 , A61K31/35 , C07D243/00
CPC分类号： C07D491/04 , C07D243/02
摘要： The invention relates to new 5H-2,3-benzodiazepine derivatives and a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same.The new 5H-2,3-benzodiazepine derivatives of the invention possess valuable central nervous effect and in particular exert antiaggressive, anxiolytic, narcosis potentiating and soporific properties.
摘要翻译：本发明涉及新的5H-2,3-苯并二氮杂衍生物及其制备方法，此外涉及含有它们的药物组合物。本发明的新的5H-2,3-苯并二氮杂衍生物具有有价值的中枢神经效应，特别是具有抗刺激，抗焦虑，麻醉增效和口服特性。

5. 发明授权

US4322346A 5H-2,3-Benzodiazepine derivatives 失效
标题翻译： 5H-2,3-苯并二氮杂衍生物
公开(公告)号：US4322346A
公开(公告)日：1982-03-30
申请号：US191811
申请日：1980-09-26
申请人： Jeno Korosi , Tibor Lang , Jozsef Szekely , Ferenc Andrasi , Gabor Zolyomi , Jozsef Borsi , Katalin Goldschmidt nee Horvath , Tamas Hamori , Gabriella Szabo nee Czibula , Zsuzsanna Meszaros nee Dunai-Kovacs , Erzsebet Miglecz
发明人： Jeno Korosi , Tibor Lang , Jozsef Szekely , Ferenc Andrasi , Gabor Zolyomi , Jozsef Borsi , Katalin Goldschmidt nee Horvath , Tamas Hamori , Gabriella Szabo nee Czibula , Zsuzsanna Meszaros nee Dunai-Kovacs , Erzsebet Miglecz
IPC分类号： C07D253/02 , A61K31/55 , A61P25/00 , A61P25/20 , C07D243/02 , C07D243/04 , C07D311/76 , C07D405/04 , C07D409/04 , C07D491/056 , C07D243/00 , C07D407/04
CPC分类号： C07D243/02 , C07D311/76
摘要： New 5H-2,3-benzodiazepine derivatives of the formula ##STR1## wherein R is phenyl having a trifluoromethyl or halogen substituent,R.sup.1 is methyl,R.sup.2 is hydrogen,R.sup.3 is methoxy and R.sup.4 is methoxy, and the pharmaceutically acceptable acid addition salts thereof, are potent tranquilizers.
摘要翻译：式（I）的新的5H-2,3-苯并二氮杂衍生物，其中R是具有三氟甲基或卤素取代基的苯基，R 1是甲基，R 2是氢，R 3是甲氧基，R 4是甲氧基，其药学上可接受的酸加成盐它们是有力的镇定剂。

6. 发明授权

US5854250A N-benzoylamino acid derivatives, pharmaceutical compositions containing them and process of preparing same 失效
标题翻译： N-苯甲酰氨基酸衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5854250A
公开(公告)日：1998-12-29
申请号：US908602
申请日：1997-08-08
申请人： Peter Matyus , Erzsebet Zara , Lajos Farkas , Agnes Papp , Antal Simay , Lajos Toldy , Ferenc Andrasi , Katalin Goldschmidt , Eszter Hodula , Ildiko Mathe , Klara Sutka , Zsuzsanna Fittler , Valeria Vitkoczi , Laszlo Sebestyen , Istvan Sziraki , Marta Rusz , Eva Gal
发明人： Peter Matyus , Erzsebet Zara , Lajos Farkas , Agnes Papp , Antal Simay , Lajos Toldy , Ferenc Andrasi , Katalin Goldschmidt , Eszter Hodula , Ildiko Mathe , Klara Sutka , Zsuzsanna Fittler , Valeria Vitkoczi , Laszlo Sebestyen , Istvan Sziraki , Marta Rusz , Eva Gal
IPC分类号： C07C235/60 , C07C237/22 , C07C259/06 , C07D207/26 , C07D207/263 , C07D239/50 , C07D295/185 , A61K31/495 , A61K31/505 , C07D241/04
CPC分类号： C07D207/27 , C07C235/60 , C07C237/22 , C07C259/06 , C07D239/50 , C07D295/185
摘要： An N-benzoylamino acid compound of the formula (I), ##STR1## wherein R.sup.3 is an NR.sup.4 R.sup.5 group where R.sup.4 and R.sup.5 which are the same or different are selected from the group consisting of hydrogen, a hydroxyl group, a C.sub.1-12 alkyl group, a C.sub.1-4 alkyl group substituted by a hydroxyl group and a C.sub.1-4 alkyl group substituted by an amino group; R.sup.4 and R.sup.5 when taken together with the adjacent nitrogen form a substituted or unsubstituted 5- or 6-membered heterocyclic group, a 5- or 6-membered heterocyclic group containing an additional nitrogen atom, a 5- or 6-membered heterocyclic group containing an additional nitrogen atom and being substituted by an oxo group, a phenyl-substituted C.sub.1-4 alkyl group or C.sub.3-5 alkenyl group; with the proviso that when the heterocyclic group is piperazine, this heterocyclic group may also be substituted by a diaminopyrimidinyl or di(pyrrolidino)-pyrimidinyl group; n is an integer from 2 to 15; and their tautomers, racemates and the pure optically active individual isomers or mixtures thereof, and a pharmaceutically acceptable salt thereof is described. These compounds are useful for the treatment of patients suffering from disorders being in an indirect or direct connection with pathological oxidation processes occurring in the organism, particularly ischaemic and reperfusion tissue injuries, inflammations, atherosclerosis, or degenerative neurological disorders.
摘要翻译：式（I）的N-苯甲酰氨基酸化合物，其中R 3是NR 4 R 5基团，其中R 4和R 5相同或不同，选自氢，羟基，C 1-12烷基基团，被羟基取代的C 1-4烷基和被氨基取代的C 1-4烷基; R 4和R 5与相邻的氮原子一起形成取代或未取代的5元或6元杂环基，含有另外的氮原子的5元或6元杂环基，含有另外的氮原子被氧代基取代，苯基取代的C 1-4烷基或C 3-5烯基; 条件是当杂环基为哌嗪时，该杂环基也可以被二氨基嘧啶基或二（吡咯烷子基） - 嘧啶基取代; n为2〜15的整数。及其互变异构体，外消旋体和纯的光学活性单体异构体或其混合物及其药学上可接受的盐。这些化合物可用于治疗患有与生物体内发生的病理氧化过程间接或直接相关的疾病的患者，特别是缺血和再灌注组织损伤，炎症，动脉粥样硬化或退行性神经障碍。

7. 发明授权

US5705529A N-benzoyl amino acid derivatives pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：含有它们的N-苯甲酰氨基酸衍生物药物组合物及其制备方法
公开(公告)号：US5705529A
公开(公告)日：1998-01-06
申请号：US540924
申请日：1995-10-11
申请人： Peter Matyus , Erzsebet Zara , Lajos Farkas , Agnes Papp , Antal Simay , Lajos Toldy , Ferenc Andrasi , Katalin Goldschmidt , Eszter Hodula , Ildiko Mathe , Klara Sutka , Zsuzsanna Fittler , Valeria Vitkoczi , Laszlo Sebestyen , Istvan Sziraki , Marta Rusz , Eva Gal
发明人： Peter Matyus , Erzsebet Zara , Lajos Farkas , Agnes Papp , Antal Simay , Lajos Toldy , Ferenc Andrasi , Katalin Goldschmidt , Eszter Hodula , Ildiko Mathe , Klara Sutka , Zsuzsanna Fittler , Valeria Vitkoczi , Laszlo Sebestyen , Istvan Sziraki , Marta Rusz , Eva Gal
IPC分类号： A61K31/165 , A61K31/19 , A61K31/215 , A61K31/505 , A61P3/06 , C07C231/02 , C07C235/52 , C07C235/60 , C07C237/22 , C07C259/06 , C07D207/26 , C07D207/263 , C07D239/50 , C07D295/185 , C07C229/14
CPC分类号： C07D207/27 , C07C235/60 , C07C237/22 , C07C259/06 , C07D239/50 , C07D295/185
摘要： The invention relates to novel N-benzoylamino acid derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, stand for a hydroxyl group optionally bearing an acetyl group; or a C.sub.1-6 alkoxy group optionally substituted by a phenyl group; n means an integer from 2 to 15 as well as their tautomers, racemates and optically active individual (pure) isomers or mixtures thereof and the salts of these compounds and pharmaceutical compositions containing these compounds. The invention relates also to a process for the preparation of compounds of the general formula (I). The compounds of general formula (I) inhibit the peroxidation of lipids and therefore, they are expected to be useful for the treatment of diseases being in an indirect or direct connection with pathological oxidation processes, chiefly for the treatment and/or prevention of ischaemic and reperfusion tissue injuries, inflammatory reactions, atherosclerosis, various degenerative neurological disorders as well as for delaying the natural process of the ageing of cells.
摘要翻译：本发明涉及通式（I）的新型N-苯甲酰氨基酸衍生物，其中R1和R2相同或不同，代表任选带有乙酰基的羟基; 或任选被苯基取代的C 1-6烷氧基; n表示2至15的整数，以及它们的互变异构体，外消旋体和光学活性个体（纯）异构体或其混合物，以及这些化合物的盐和含有这些化合物的药物组合物。本发明还涉及制备通式（I）化合物的方法。通式（I）的化合物抑制脂质的过氧化，因此预期它们可用于治疗与病理氧化过程间接或直接相关的疾病，主要用于治疗和/或预防缺血和再灌注组织损伤，炎症反应，动脉粥样硬化，各种退行性神经障碍以及延缓细胞老化的自然过程。

8. 发明授权

US6075018A 1-[2-(substituted vinyl)]-3,4-dihydro-4-dihydro-5H-2,3-benzodiazepine derivatives 失效
标题翻译： 1- [2-（取代的乙烯基）] -3,4-二氢-4-二氢-5 + E，H + EE -2,3-苯并二氮杂衍生物
公开(公告)号：US6075018A
公开(公告)日：2000-06-13
申请号：US599235
申请日：1996-02-09
申请人： Pal Vago , Jozsef Reiter , Istvan Gyertyan , Gabor Gigler , Ferenc Andrasi , Anna Bakonyi , Pal Berzsenyi , Peter Botka, deceased , Erszebet Birkas , Tamas Hamori , Edit Horvath , Katalin Horvath , Jeno Korosi, deceased , Gyorgyne Mate , Imre Moravcsik , Gyorgy Somogyi , Eszter Szentkuti , Gabor Zolyomi
发明人： Pal Vago , Jozsef Reiter , Istvan Gyertyan , Gabor Gigler , Ferenc Andrasi , Anna Bakonyi , Pal Berzsenyi , Peter Botka, deceased , Erszebet Birkas , Tamas Hamori , Edit Horvath , Katalin Horvath , Jeno Korosi, deceased , Gyorgyne Mate , Imre Moravcsik , Gyorgy Somogyi , Eszter Szentkuti , Gabor Zolyomi
IPC分类号： A61K31/55 , A61K31/551 , A61P25/00 , C07D243/02 , C07D243/04 , C07D405/06 , C07D491/04 , C07D491/056 , C07D493/04 , A61K31/395
CPC分类号： C07D405/06 , C07D243/02 , C07D491/04 , C07D493/04
摘要： The invention relates to new 1-[2-(substituted vinyl)]-3,4-dihydro-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof and pharmaceutical compositions comprising them. The new 1-[2-(substituted vinyl)]-3,4-dihidro-5H-2,3-benzodiazepine derivatives according to the invention correspond to the general formula (I), ##STR1## wherein the variables are hereinbelow defined: The new compounds according to the invention affect the central nervous system and can be used to advantage in the therapy.
摘要翻译：本发明涉及新的1- [2-（取代的乙烯基）] -3,4-二氢-5 + E，非H + EE-2,3-苯并二氮杂衍生物，其制备方法和包含它们的药物组合物。根据本发明的新的1- [2-（取代的乙烯基）] -3,4-二阴离子-5 + E，非H + EE -2,3-苯并二氮杂衍生物对应于通式（I），其中变量在下文中定义：根据本发明的新化合物影响中枢神经系统并且可以在治疗中有利地使用。

9. 发明授权

US5807851A 2,3-Benzodiazepine Derivatives as non-competitive AMPA 失效
标题翻译： 2,3-苯并二氮杂衍生物作为非竞争性AMPA
公开(公告)号：US5807851A
公开(公告)日：1998-09-15
申请号：US832777
申请日：1997-04-04
申请人： Istvan Ling , Gizella Abraham , Pal Berzsenyi , Istvan Tarnawa , Sandor Solyom , Ferenc Andrasi , Tamas Hamori , Emese Csuzdi , Katalin Horvath , Melinda Gal , Imre Moravcsik , Marta Szollosy
发明人： Istvan Ling , Gizella Abraham , Pal Berzsenyi , Istvan Tarnawa , Sandor Solyom , Ferenc Andrasi , Tamas Hamori , Emese Csuzdi , Katalin Horvath , Melinda Gal , Imre Moravcsik , Marta Szollosy
IPC分类号： A61K31/55 , A61K31/551 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07D243/02 , C07D243/04 , A01N43/62 , C07D243/00
CPC分类号： C07D243/02
摘要： Derivatives of 2,3-benzodiazepine are substituted by one or two halogen atom(s) and have the general formula ##STR1## These derivatives are non-competitive AMPA antagonists and are used in pharmaceutical compositions. A process to make the 2,3-benzodiazepine derivatives includes converting starting compounds which are substituted by one or two halogen groups and have the general formula ##STR2##
摘要翻译： 2,3-苯并二氮杂的衍生物被一个或两个卤素原子取代并具有通式<这些衍生物是非竞争性的AMPA拮抗剂，并用于药物组合物中。制备2,3-苯并二氮杂衍生物的方法包括转化被一个或两个卤素基团取代的起始化合物，并具有通式

10. 发明授权

US5639751A N-acyl-2,3-benzodiazepine derivatives for treating acute and chronic neurodegenerative disorders 失效
标题翻译：用于治疗急性和慢性神经变性疾病的N-酰基-2,3-苯并二氮杂衍生物
公开(公告)号：US5639751A
公开(公告)日：1997-06-17
申请号：US477801
申请日：1995-06-07
申请人： Ferenc Andrasi , Pal Berzsenyi , Peter Botka , Sandor Farkas , Katalin Goldschmidt , Tamas Hamori , Jeno Korosi , Imre Moravcsik , Istvan Tarnawa
发明人： Ferenc Andrasi , Pal Berzsenyi , Peter Botka , Sandor Farkas , Katalin Goldschmidt , Tamas Hamori , Jeno Korosi , Imre Moravcsik , Istvan Tarnawa
IPC分类号： C07D491/04 , A61K31/55 , A61K31/44
CPC分类号： C07D491/04
摘要： The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I)R stands for a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group, or by one or more halogen(s); or R is a benzoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; or R is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.1 means hydrogen; or R.sup.1 is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.2 means a C.sub.1-3 alkyl group; orR.sup.1 and R.sup.2 together stand for a methylene group and no double bond is present between the N(3) and C(4) atoms;R.sup.3 means hydrogen or a C.sub.1-4 alkanoyl group;R.sup.4 represents hydrogen; a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group or by one or more halogen(s); as well as a benzoyl, palmitoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; andthe dotted lines represent valence bonds optionally being present, with the proviso that no double bond exists between the N(3) and C(4) atoms when both R.sup.3 and R.sup.4 stand for hydrogen.The compounds of the general formula (I) possess valuable central nervous system effects, particularly muscle-relaxant, anticonvulsive and neuroprotective action. Thus, they may be useful for the treatment of various diseases of central nervous system origin.
摘要翻译：本发明涉及通式（I）的新型N-酰基-2,3-苯并二氮杂萘衍生物，其立体异构体和酸加成盐，含有它们的药物组合物及其制备方法。在通式（I）中，R代表任选被甲氧基，氰基，羧基，氨基，C 1-4烷基氨基，二（C 1-4烷基）氨基，吡咯烷子基，邻苯二甲酰亚胺基或苯基取代的C 1-6烷酰基，或通过一个或多个卤素; 或R是苯甲酰基，环丙烷羰基，C 1-5烷基氨基甲酰基或苯基氨基甲酰基; 或者当N（3）和C（4）原子之间存在双键时，R不存在; R1表示氢; 当N（3）和C（4）原子之间存在双键时，R1不存在; R2表示C1-3烷基; 或者R 1和R 2一起代表亚甲基，N（3）和C（4）原子之间不存在双键; R3表示氢或C1-4烷酰基; R4代表氢; 任选被甲氧基，氰基，羧基，氨基，C1-4烷基氨基，二（C1-4烷基）氨基，吡咯烷子基，苯二甲酰亚氨基或苯基或一个或多个卤素取代的C 1-6烷酰基; 以及苯甲酰基，棕榈酰基，环丙烷羰基，C 1-5烷基氨基甲酰基或苯基氨基甲酰基; 并且虚线表示任选存在的价键，条件是当R3和R4均代表氢时，N（3）和C（4）原子之间不存在双键。通式（I）的化合物具有有价值的中枢神经系统作用，特别是肌肉松弛剂，抗惊厥和神经保护作用。因此，它们可用于治疗中枢神经系统起源的各种疾病。

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