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1. 发明授权

US5635511A Treatment of heart rhythm disorders by administration of 3-phenylsulfonyl-3,7-diazabicyclo[3.3.1]nonane compounds. 失效
标题翻译：通过给予3-苯基磺酰基-3,7-二氮杂双环[3.3.1]壬烷化合物治疗心律紊乱。
公开(公告)号：US5635511A
公开(公告)日：1997-06-03
申请号：US594946
申请日：1996-01-31
申请人： Uwe Schoen , Arman Farjam , Reinhard Brueckner , Dieter Ziegler
发明人： Uwe Schoen , Arman Farjam , Reinhard Brueckner , Dieter Ziegler
IPC分类号： A61K31/435 , A61K31/439 , A61K31/445 , A61P9/00 , A61P9/06 , C07D471/08 , C07D471/10 , A61K31/44
CPC分类号： C07D471/08 , C07D471/10
摘要： The use of 3,7,9,9-tetrasubstituted 3-phenylsulfonyl-3,7-diazabicyclo[3.3.1]nonane compounds for treating cardiac arrhytmias in larger mammals, including humans; novel antiarrhythmically active 3,7,9,9-tetrasubstituted compounds corresponding to the general formula Ia ##STR1## in which R.sup.1 is an alkyl group having 1-6 carbon atoms or a cycloalkylalkyl group having 4-7 carbon atoms,R.sup.2 is lower alkyl, andR.sup.3 is lower alkyl, orR.sup.2 and R.sup.3 together form an alkylene chain having 3-6 carbon atoms,R.sup.4' is cyano, an R.sup.6 --O--CO-- group in which R.sup.6 is lower alkyl, an R.sup.7 --SO.sub.2 --NH-- group in which R.sup.7 is lower alkyl, or an R.sup.8 --CO--NH-- group in which R.sup.8 is lower alkyl or a phenyl group which is optionally substituted by halogen, cyano, nitro, or an R.sup.9 --SO.sub.2 -- radical in which R.sup.9 is lower alkyl, or an imidazolyl radical located in position 4 of the phenyl ring, andR.sup.5 is hydrogen or halogen,and physiologically acceptable acid addition salts thereof, and processes and intermediates for preparing them.
摘要翻译：使用3,7,9,9-四取代的3-苯基磺酰基-3,7-二氮杂双环[3.3.1]壬烷化合物治疗大型哺乳动物，包括人类的心脏病变; 对应于其中R 1为具有1-6个碳原子的烷基或具有4-7个碳原子的环烷基烷基的通式Ia Ia的新型抗心律失活的3,7,9,9-四取代化合物，R2较低烷基，R3为低级烷基，或R2和R3一起形成3-6个碳原子的亚烷基链，R4'为氰基，R6为低级烷基的R6-O-CO-基团，R7-SO2-NH - 其中R 7为低级烷基的基团，或其中R 8为低级烷基的R 8 -CO-NH基或任选被卤素，氰基，硝基或R 9 -SO 2 - 基团取代的苯基，其中R 9为低级烷基或位于苯环4位的咪唑基，R5为氢或卤素，以及其生理上可接受的酸加成盐，以及制备它们的方法和中间体。

2. 发明授权

US5576327A Treatment of heart rhythym disorders by administration of 3-phenylsulfonyl-3, 7-diazabicyclo[3.3.1]nonane compounds 失效
标题翻译：通过给予3-苯基磺酰基-3,7-二氮杂双环[3.3.1]壬烷化合物治疗心律失调症
公开(公告)号：US5576327A
公开(公告)日：1996-11-19
申请号：US382262
申请日：1995-02-01
申请人： Uwe Schoen , Arman Farjam , Reinhard Brueckner , Dieter Ziegler
发明人： Uwe Schoen , Arman Farjam , Reinhard Brueckner , Dieter Ziegler
IPC分类号： A61K31/435 , A61K31/439 , A61K31/445 , A61P9/00 , A61P9/06 , C07D471/08 , C07D471/10
CPC分类号： C07D471/08 , C07D471/10
摘要： The use of 3,7,9,9-tetrasubstituted 3-phenylsulfonyl-3,7-diazabicyclo[3.3.1]nonane compounds for treating cardiac arrhythmias in larger mammals, including humans; novel antiarrhythmically active 3,7,9,9-tetrasubstituted compounds corresponding to the general formula Ia ##STR1## in which R.sup.1 is an alkyl group having 1-6 carbon atoms or a cycloalkylalkyl group having 4-7 carbon atoms,R.sup.2 is lower alkyl, andR.sup.3 is lower alkyl, orR.sup.2 and R.sup.3 together form an alkylene chain having 3-6 carbon atoms,R.sup.4 ' is cyano, an R.sup.6 --O--CO-- group in which R.sup.6 is lower alkyl, an R.sup.7 --SO.sub.2 --NH-- group in which R.sup.7 is lower alkyl, or an R.sup.8 --CO--NH-- group in which R.sup.8 is lower alkyl or a phenyl group which is optionally substituted by halogen, cyano, nitro or an R.sup.9 --SO.sub.2 -- radical in which R.sup.9 is lower alkyl, or an imidazolyl radical located in position 4 of the phenyl ring, andR.sup.5 is hydrogen or halogen,and physiologically acceptable acid addition salts thereof, and processes and intermediates for preparing them.
摘要翻译：使用3,7,9,9-四取代的3-苯基磺酰基-3,7-二氮杂双环[3.3.1]壬烷化合物治疗大型哺乳动物，包括人类的心律失常; 对应于其中R 1为具有1-6个碳原子的烷基或具有4-7个碳原子的环烷基烷基的通式Ia Ia的新型抗心律失活的3,7,9,9-四取代化合物，R2较低烷基，R3为低级烷基，或R2和R3一起形成3-6个碳原子的亚烷基链，R4'为氰基，R6为低级烷基的R6-O-CO-基团，R7-SO2-NH - 其中R 7为低级烷基的基团，或其中R 8为低级烷基的R 8 -CO-NH-基团或任选被卤素，氰基，硝基或R 9 -SO 2 - 基团取代的苯基，其中R 9为低级烷基或位于苯环4位的咪唑基，R5为氢或卤素，以及其生理上可接受的酸加成盐，以及其制备方法和中间体。

3. 发明授权

US5474988A 5-phenylpyrrolo-1,4-benzoxazine and 5-phenylpyrrolo-1,4-benzothiazine compounds, process and intermediates for their production and pharmaceutical compositions containing them 失效
标题翻译： 5-苯基吡咯并-1,4-苯并恶嗪和5-苯基吡咯并-1,4-苯并噻嗪化合物，其制备方法和中间体以及含有它们的药物组合物
公开(公告)号：US5474988A
公开(公告)日：1995-12-12
申请号：US196462
申请日：1994-02-15
申请人： Patrice Demonchaux , Patrick Lenoir
发明人： Patrice Demonchaux , Patrick Lenoir
IPC分类号： A61K31/535 , A61K31/538 , A61K31/54 , A61K31/5415 , A61P29/00 , A61P37/08 , C07D265/36 , C07D279/16 , C07D498/06 , C07D513/06 , C07D265/34 , C07D279/14
CPC分类号： C07D513/06
摘要： Pharmacologically active compounds of formula I ##STR1## which can be substituted in the phenyl rings and in which R.sup.1 denotes hydrogen or lower alkyl,R.sup.2 denotes hydrogen or lower alkyl,Y denotes oxygen or sulfurn represents an integer from 1 to 3Z represents a bond, a CO group or a CH.dbd. group,Q denotes nitrogen or the CH group andR.sup.7, if Q denotes nitrogen, represents an optionally substituted pyridyl or phenyl radical or, if Q denotes the CH group, represents the N-methyl-N-(4-oxo-3H-pyrimidin-2-yl)amino group,and their acid addition salts and processes and intermediates for their preparation.
摘要翻译：可以在苯环中取代的式I的药理学活性化合物，其中R 1表示氢或低级烷基，R 2表示氢或低级烷基，Y表示氧或硫，n表示1至3的整数Z表示键，CO基或CH =基，Q表示氮或CH基，R7表示任选取代的吡啶基或苯基，或者如果Q表示CH基，则表示N-甲基 - N-（4-氧代-3H-嘧啶-2-基）氨基及其酸加成盐及其制备方法和中间体。

4. 发明授权

US5418224A 4,13-dioxabicyclo[8.2.1]tridecenone compounds and pharmaceutical compositions containing them 失效
标题翻译： 4,13-二氧杂双环[8.2.1]十三酮化合物和含有它们的药物组合物
公开(公告)号：US5418224A
公开(公告)日：1995-05-23
申请号：US996083
申请日：1992-12-23
申请人： Dagmar Hoeltje , Ulf Preuschoff , Christian Eeckhout
发明人： Dagmar Hoeltje , Ulf Preuschoff , Christian Eeckhout
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/14 , A61P43/00 , C07H17/08
CPC分类号： C07H17/08
摘要： Ring-contracted N-demethyl-N-isopropylerythromycin A derivatives with gastrointestinally effective motilin-agonistic properties, a method for preparing such compounds, and pharmaceutical compositions containing them.
摘要翻译：具有胃肠道有效的胃动素激动性的收缩N-去甲基-N-异丙基红霉素A衍生物，制备这些化合物的方法和含有它们的药物组合物。

5. 发明授权

US5324725A 7-fused 2-(piperazinoalkyl) indole derivatives, intermediates and compositions thereof 失效
标题翻译： 7-稠合的2-（哌嗪基烷基）吲哚衍生物，其中间体及其组合物
公开(公告)号：US5324725A
公开(公告)日：1994-06-28
申请号：US933476
申请日：1992-08-21
申请人： Daniel Jasserand , Dominique Paris , Patrice Demonchaux , Michel Cottin , Francois Floc'H , Pierre Dupassieux , Richard White
发明人： Daniel Jasserand , Dominique Paris , Patrice Demonchaux , Michel Cottin , Francois Floc'H , Pierre Dupassieux , Richard White
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/435 , A61K31/44 , A61K31/47 , A61K31/4745 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/54 , A61K31/542 , A61K31/5513 , A61P1/00 , A61P9/00 , A61P11/08 , A61P29/00 , A61P37/08 , C07D209/56 , C07D209/94 , C07D471/06 , C07D487/06 , C07D498/06 , C07D513/06 , A61K31/55
CPC分类号： C07D471/06 , C07D487/06 , C07D513/06
摘要： Pharmacologically active compounds having anti-allergic properties corresponding to the formula I ##STR1## which can be mono- or disubstituted in the phenyl ring and their acid addition salts and/or S-mono- or dioxides of sulfur-containing compounds of the formula I are described, together with processes and intermediates for their preparation.
摘要翻译：描述了具有对应于式I的抗过敏性质的药理学活性化合物，其中式I与式I的含硫化合物的苯环及其酸加成盐和/或S-单或二氧化物，以及其制备方法和中间体制备。

6. 发明授权

US5010076A 1,7-fused 1H-indole-2-carboxylic acid-N-(1,4-benzodiazepin-3-yl)amides 失效
标题翻译： 1,7-稠合的1H-吲哚-2-羧酸-N-（1,4-苯并二氮杂-3-基）酰胺
公开(公告)号：US5010076A
公开(公告)日：1991-04-23
申请号：US489502
申请日：1990-03-07
申请人： Harald Waldeck , Werner Benson , Horst Zeugner , Klaus-Ullrich Wolf , Peter-Colin Gregory , Derk Hamminga , Ineke van Wijngaarden
发明人： Harald Waldeck , Werner Benson , Horst Zeugner , Klaus-Ullrich Wolf , Peter-Colin Gregory , Derk Hamminga , Ineke van Wijngaarden
IPC分类号： C07D487/04 , A61K31/397 , A61K31/55 , A61P1/00 , C07D471/06 , C07D487/06 , C07D498/06 , C07D513/06 , C07D519/00
CPC分类号： C07D471/06 , C07D487/06 , C07D513/06
摘要： Compounds corresponding to the formula I ##STR1## in which R.sup.1 represents hydrogen, lower alkyl or cycloalkylalkyl with 4-7 carbon atoms,R.sup.2 represents hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl, andR.sup.3 represents hydrogen, halogen, lower alkyl or lower alkoxy, orR.sup.2 and R.sup.3 together denote an alkylenedioxy group,R.sup.4 represents cycloalkyl with 5 to 6 carbon atoms, thiophene or optionally substituted phenyl,R.sup.5 represents hydrogen or halogen,R.sup.6 represents hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl, andZ represents an alkylene chain with 2-4 carbon atoms, which can optionally be mono- or disubstituted by lower alkyl or onto which a 5-6-membered carbocyclic ring can optionally be fused, or represents an --X--CH.sub.2 --CH.sub.2 -- chain,which have pharmacologically valuable properties, are described, together with a method for their preparation.
摘要翻译：对应于式I的化合物（I）其中R1代表氢，具有4-7个碳原子的低级烷基或环烷基烷基，R2代表氢，卤素，低级烷基，低级烷氧基或三氟甲基，R3代表氢，卤素，低级烷基或低级烷氧基，或R 2和R 3一起表示亚烷基二氧基，R 4表示具有5至6个碳原子的环烷基，噻吩或任选取代的苯基，R 5表示氢或卤素，R 6表示氢，卤素，低级烷基，低级烷氧基或三氟甲基，Z表示具有2-4个碳原子的亚烷基链，其可以任选被低级烷基单取代或二取代，或其上可以任选地稠合5-6元碳环，或表示-X-CH2- 描述了具有药理学有价值性质的CH2-链及其制备方法。

7. 发明授权

US4814345A 1-phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： 1-苯基-2-氨基羰基吲哚化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4814345A
公开(公告)日：1989-03-21
申请号：US123201
申请日：1987-11-20
申请人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuhl , Gerd Buschmann , Stephen J. Magda
发明人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuhl , Gerd Buschmann , Stephen J. Magda
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/06 , C07D209/42 , A61K31/405
CPC分类号： C07D209/42
摘要： Novel 1-phenyl-2-aminocarbonylindole compounds are disclosed having the general formula I ##STR1## wherein R.sub.1 is an aliphatic or aromatic acyl group or an optionally substituted benzyl group; R.sub.2 is hydrogen or a lower alkyl radical; R.sub.3 is a hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.4 is hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.5 has the significance given R.sub.3 ; R.sub.6 has the significance given for R.sub.4, or R.sub.6 is nitro or trifluoromethyl; R.sub.7 and R.sub.8 each represent hydrogen or a lower alkyl radical, or together with a nitrogen atom form a heterocyclic group; and Z signifies an alkylene chain optionally substituted by hydroxy or acyloxy. The compounds have pharmacological, in particular antiarrhythmic, properties.
摘要翻译：公开了具有通式I的新型1-苯基-2-氨基羰基吲哚化合物，其中R 1是脂族或芳族酰基或任选取代的苄基; R2是氢或低级烷基; R3是氢，卤素，低级烷基或低级烷氧基; R4是氢，卤素，低级烷基或低级烷氧基; R5具有给定R3的意义; R6对R4具有重要意义，或R6是硝基或三氟甲基; R7和R8各自表示氢或低级烷基，或与氮原子一起形成杂环基; Z表示任选被羟基或酰氧基取代的亚烷基链。这些化合物具有药理学，特别是抗心律不齐的特性。

8. 发明授权

US4803198A 1-Phenyl-2-aminocarbonylindole compounds, preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： 1-苯基-2-氨基羰基吲哚化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4803198A
公开(公告)日：1989-02-07
申请号：US885684
申请日：1986-07-15
申请人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuehl , Gerd Buschmann , Stephen J. Magda
发明人： Heinrich-Wilhelm Ohlendorf , Wilhelm Kaupmann , Ulrich Kuehl , Gerd Buschmann , Stephen J. Magda
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61P9/06 , C07D209/24 , C07D209/42 , A61K31/55 , C07D403/12 , C07D403/14
CPC分类号： C07D209/42
摘要： New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is an alkylene chain which is optionally substituted by hydroxyl. The compounds have pharmaceutical properties, in particular antiarrhythmic properties. The compounds may be in the form of the free bases or acid addition salts. Pharmaceutical compositions containing these compounds are described as is a method of preparing them.Valuable intermediates for the production of these compounds and methods of preparing the intermediates are also described.
摘要翻译：描述了具有通式Ⅰ的新的1-苯基-2-氨基羰基吲哚化合物，其中R 1是氢原子，或低级烷基，烯基，环烷基烷基，R 2是氢原子或低级烷基，R 3 是氢或卤素原子，或低级烷基，羟基或低级烷氧基，R4是氢或卤素原子，或低级烷基，羟基或低级烷氧基，或者如果R3是氢原子，R4可以是硝基或三氟甲基，或R 3和R 4一起表示亚甲二氧基或亚乙二氧基，R 5具有R 3的含义，R 6具有对R 4的定义，R 7是氢原子，或者如果R 5和R 6是低级烷氧基，则R 7 也可以是低级烷氧基，R 8和R 9各自为氢原子或低级烷基，或者与氮原子一起形成杂环基，Z为任选被羟基取代的亚烷基链。这些化合物具有药物性质，特别是抗心律失常性质。化合物可以是游离碱或酸加成盐的形式。含有这些化合物的药物组合物被描述为制备它们的方法。还描述了制备这些化合物的有价值的中间体和制备中间体的方法。

9. 发明授权

US4533662A 2-Acylaminomethyl-1,4-benzodiazepine compounds and analgesic use 失效
标题翻译： 2-酰氨基甲基-1,4-苯并二氮杂化合物和止痛用途
公开(公告)号：US4533662A
公开(公告)日：1985-08-06
申请号：US330324
申请日：1981-12-14
申请人： Horst Zeugner , Dietmar Roemer , Hans Liepmann , Wolfgang Milkowski
发明人： Horst Zeugner , Dietmar Roemer , Hans Liepmann , Wolfgang Milkowski
IPC分类号： A61K31/55 , A61K31/551 , A61P25/04 , C07D243/16 , C07D405/12 , C07D491/04 , C07D491/056 , C07D405/10
CPC分类号： C07D491/04 , C07D243/16
摘要： Novel 2-acyl amino methyl-5-phenyl-1H-2,3-dihydro-1,4-benzo diazepine compounds of the following Formula I ##STR1## which have valuable pharmacological properties are provided. In said Formula I the acyl group --CO--R.sub.3 represents a benzoyl group or a phenyl alkanoyl group which may be unsubstituted or mono- or di-substituted in the phenyl ring. The substituent R.sub.1 in said compounds indicates lower alkyl, lower alkenyl, or cyclopropyl methyl, and the substituent R.sub.2 indicates hydrogen, lower alkyl, or lower alkenyl, while the substituent R.sub.6 indicates hydrogen, halogen, lower alkyl, lower alkoxy, hydroxyl, lower alkylthio, nitro, trifluoro methyl, cyano, amino, mono- or di-lower alkyl amino, lower mono-alkanoyl amino, lower N-alkyl-N-alkanoyl amino, or lower alkanoyloxy, and the substituent R.sub.7 indicates hydrogen, halogen, lower alkyl, lower alkoxy, hydroxyl, or lower alkanoyloxy, whereby R.sub.6 and R.sub.7, when attached to adjacent carbon atoms, may form together the methylene dioxy or the ethylene dioxy group. The substituents R.sub.8 and R.sub.9 designate the same substituents as indicated for the substituents R.sub.6 and R.sub.7.The compounds of Formula I have a surprising analgesic activity.
摘要翻译：提供了具有有价值的药理学性质的下列通式I的2-酰基氨基甲基-5-苯基-1H-2,3-二氢-1,4-苯并二氮杂化合物。在所述式I中，酰基-CO-R 3表示苯基或苯基烷酰基，其可在苯环中未被取代或单取代或二取代。所述化合物中的取代基R 1表示低级烷基，低级烯基或环丙基甲基，取代基R 2表示氢，低级烷基或低级烯基，而取代基R 6表示氢，卤素，低级烷基，低级烷氧基，羟基，低级烷硫基硝基，三氟甲基，氰基，氨基，一或二低级烷基氨基，低级单烷酰基氨基，低级N-烷基-N-烷酰基氨基或低级烷酰氧基，取代基R7表示氢，卤素，低级烷基，低级烷氧基，羟基或低级烷酰氧基，其中当连接到相邻碳原子上时，R 6和R 7可以一起形成亚甲基二氧基或亚乙基二氧基。取代基R8和R9表示与取代基R6和R7相同的取代基。式I的化合物具有惊人的止痛活性。

10. 发明授权

US4508716A [1,2]-Fused 1,4-benzodiazepine compounds, process for their preparation and compositions containing them 失效
标题翻译： [1,2] - 熔融的1,4-苯并二氮杂化合物，其制备方法和含有它们的组合物
公开(公告)号：US4508716A
公开(公告)日：1985-04-02
申请号：US453785
申请日：1982-12-27
申请人： Hans Liepmann , Michael Ruhland , Herbert Muesch , Werner Benson , Henning Heinemann , Horst Zeugner
发明人： Hans Liepmann , Michael Ruhland , Herbert Muesch , Werner Benson , Henning Heinemann , Horst Zeugner
IPC分类号： A61K31/55 , A61K31/5513 , A61P25/00 , C07D307/54 , C07D333/38 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14 , C07D487/04 , C07D491/04 , C07D491/056 , C07D491/14 , C07D491/147 , C07D498/04 , C07D498/14 , C07D513/04 , A61K31/495
CPC分类号： C07D405/04 , C07D307/54 , C07D333/38 , C07D407/04 , C07D409/04 , C07D487/04 , C07D491/04 , C07D491/14 , C07D513/04
摘要： [1,2]-fused 1,4-benzodiazepine compounds are disclosed corresponding to the general formula I ##STR1## wherein X is an oxygen or sulfur atom or an optionally substituted imino group, R.sub.1 is a hydrogen or halogen atom, lower alkyl radical, a lower alkoxy radical or a nitro group and R.sub.2 is a hydrogen or halogen atom, a lower alkyl radical, a lower alkoxy radical or a nitro group, or if R.sub.1 is a hydrogen atom, R.sub.2 may also be a lower alkylthio radical, or, if R.sub.1 is a hydrogen atom and X is a sulfur atom or an imino group, R.sub.2 may be a trifluoromethyl radical; or R.sub.1 and R.sub.2 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy radical; R.sub.3 is an optionally substituted furyl, thienyl, pyrrolyl or pyridyl radical and n is zero or, if R.sub.3 is furyl or thienyl, n may be 0 or 1. The compounds may be in the form of their optical isomers or acid addition salts. The compounds exhibit neuroleptic properties. Processes for preparing the compounds and pharmaceutical compositions containing them are also disclosed.
摘要翻译： [1,2] - 稠合的1,4-苯并二氮杂化合物对应于通式I的化合物，其中X是氧或硫原子或任选取代的亚氨基，R 1是氢或卤原子，低级烷基基团，低级烷氧基或硝基，R 2是氢或卤素原子，低级烷基，低级烷氧基或硝基，或者如果R 1是氢原子，则R 2也可以是低级烷硫基，或者，如果R1是氢原子，X是硫原子或亚氨基，则R2可以是三氟甲基; 或R 1和R 2与相邻的碳原子键合并且一起表示亚甲二氧基或亚乙二氧基; R3是任选取代的呋喃基，噻吩基，吡咯基或吡啶基，n是0，或者如果R3是呋喃基或噻吩基，则n可以是0或1.这些化合物可以是其旋光异构体或酸加成盐的形式。该化合物表现出精神安定药物的特性。还公开了制备含有它们的化合物和药物组合物的方法。

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