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Imidazo 1,2-a (Pyrrolo, Thieno or Furano) 3,2-d azepine derivatives, preparations and their use

机译:咪唑并[1,2-a](吡咯并,蒂诺或富良野)[3,2-d]氮杂pine衍生物,制剂及其用途

摘要

The present invention is concerned with novel imidazo[1,2-a](pyrrolo, thieno or furano)[3,2-d]azepines 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, C1-4alkyl, halo, ethenyl substituted with hydroxycarbanyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl, hydroxycarbonyl or hydroxycarbonylC1-4alkyl; R2 represents hydrogen, C1-4alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R3 represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl, phenyl 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, C1-4alkyloxycarbonylC1-4alkyloxy, 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; L represents a radical of formula -Alk-Y-Het1 (a-1), -Alk-NH-CO-Het2 (a-2) or -Alk-Het3 (a-3); which are useful antiallergic compounds. Compositions comprising said compounds, methods of using, and processes for preparing the same.
机译:本发明涉及式的新型咪唑并[1,2-a](吡咯并,噻吩并呋喃并呋喃)[3,2-d]氮杂s,其药学上可接受的加成盐及其立体化学异构形式,其中每个虚线独立地表示可选的键; R 1代表氢,C 1-4烷基,卤素,被羟基碳烷基或C 1-4烷氧基羰基,羟基C 1-4烷基,甲酰基,羟基羰基或羟基羰基C 1-4烷基取代的乙烯基; R 2代表氢,C 1-4烷基,被羟羰基或C 1-4烷氧羰基取代的乙烯基,C 1-4烷基被羟羰基或C 1-4烷氧羰基取代,羟基C 1-4烷基,甲酰基或羟羰基; R 3代表氢,C 1-4烷基,羟基C 1-4烷基,苯基或卤素; 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; L表示式-Alk-Y-Het 1(a-1),-Alk-NH-CO-Het 2(a-2)或-Alk-Het 3(a-3)的基团;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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