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IMIDAZO2,1-B3BENZAZEPINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING, AND PROCESS FOR PREPARING THEM AND INTERMEDIATES
IMIDAZO2,1-B3BENZAZEPINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING, AND PROCESS FOR PREPARING THEM AND INTERMEDIATES
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机译:咪达唑[2,1-B] [3]苯扎西汀衍生物,包含的药物组合物及其制备方法和中间体
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摘要
The present invention is concerned with novel imidazo[2,1-b][3]benzazepines of formula CHEM the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R1 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy; R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy; R3 represents hydrogen, C1-4alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R4 represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl, phenyl or halo; R5 represents hydrogen, C1-4alkyl or halo; L represents hydrogen; C1-6alkyl; C1-6alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C1-4alkyloxy, hydroxycarbonyl, C1-4alkyloxycarbonyl, C1-4alkyloxycarbonyl-C1-4alkyloxy, hydroxycarbonylC1-4alkyloxy, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonyl, C1-4alkylaminocarbonylamino, C1-4alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C1-6alkyl substituted with both hydroxy and aryloxy; C3-6alkenyl; C3-6alkenyl substituted with aryl; or, L represents a radical of formula -Alk-Y-Het1 (a-1), -Alk-NH-CO-Het2 (a-2) or -Alk-Het3 (a-3); provided that 6,11-dihydro-11-(4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine is ecxluded, which are useful antiallergic compounds. Compositions comprising said compounds, methods of using and processes for preparing the same.
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机译:本发明涉及式的新型咪唑并[2,1-b] [3]苯并ze庚因的药学上可接受的加成盐及其立体化学异构体形式,其中每个虚线独立地表示任选的键; R 1代表氢,卤素,C 1-4烷基或C 1-4烷氧基; R 2代表氢,卤素,C 1-4烷基或C 1-4烷氧基; R 3代表氢,C 1-4烷基,被羟基羰基或C 1-4烷氧基羰基取代的乙烯基,C 1-4烷基被羟基羰基或C 1-4烷氧基羰基取代,羟基C 1-4烷基,甲酰基或羟基羰基; R 4代表氢,C 1-4烷基,羟基C 1-4烷基,苯基或卤素; R 5代表氢,C 1-4烷基或卤素; L代表氢; C 1-6烷基;被一个选自以下的取代基取代的C 1-6烷基:羟基,卤素,C 1-4烷氧基,羟基羰基,C 1-4烷氧基羰基,C 1-4烷氧基羰基-C 1-4烷氧基,羟基羰基C 1-4烷氧基,C 1-4烷氧基羰基氨基,C 1-4烷基氨基羰基,C 1-4烷基氨基羰基氨基,C 1-4烷基氨基硫代羰基氨基,芳基,芳氧基和芳基羰基;被羟基和芳氧基均取代的C 1-6烷基; C3-6链烯基; C3-6链烯基被芳基取代;或者,L表示式-Alk-Y-Het 1(a-1),-Alk-NH-CO-Het 2(a-2)或-Alk-Het 3(a- 3);只要排除了6,11-二氢-11-(4-哌啶亚基)-5H-咪唑并[2,1-b] [3]苯并ze庚因,它们是有用的抗过敏化合物。包含所述化合物的组合物,其使用方法和制备方法。
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