DERIVATIVES OF IMIDAZO[1,2A]THIENO[2,3-D]AZEPINES, METHOD OF THEIR SYNTHESIS, INTERMEDIATE COMPOUNDS FOR THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND METHOD OF ITS PREPARING

摘要

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of imidazo[1,2a] thieno[2,3-d] -azepines of the formula (I) or their pharmaceutically acceptable addition salt or stereochemical isomer where each of dotted line means independently a possible (complementary) bond; R means hydrogen atom, C1-4-alkyl; R means hydrogen atom, C1-4-alkyl, C1-4-alkyl substituted with hydroxycarbonyl or C1-4-alkylhydroxycarbonyl; R means hydrogen atom, C1-4-alkyl; X means S-atom; L means hydrogen atom, C1-6-alkyl, C1-6-alkyl containing a substituent taken from a group including hydroxy-group, C1-4-alkylhydroxy-group, hydroxycarbonyl, C1-4-alkylhydroxycarbonyl, C1-4-alkylaminocarbonyl, C1-4-alkyl-hydroxycarbonylamino-group, C1-4-alkylhydroxycarbonyl-C1-4-alkylhydroxy-group, hydroxycarbonyl-C1-4-alkylhydroxy-group, C1-4-alkylaminocarbonylamino-group, C1-4-alkylaminocarbonyl- -amino-group, C1-4-alkylaminothiocarbonylamino-group, aryl and arylhydroxy-group; C3-6-alkenyl substituted with aryl where each aryl is phenyl or phenyl substituted with halogen atom, hydroxy-group, C1-4-alkylhydroxy-group or L means a radical of the formula -Alk-Y-Het , -Alk-NH-CO-Het or -Alk-Het where Alk means C1-4-alkanediyl; Y means O-atom or NH; Het means pyrimidinyl; Het - furanyl; Het - pyrrolyl substituted with C1-4-alkylhydroxycarbonyl, pyridinyl, 4,5-dihydro-5-oxo-1H-tetrazolyl substituted with C1-4-alkyl, 2-oxo-3-oxazolidinyl, 2,3-dihydro-2-oxo-1H-benzimidazol-1-yl or radical of the formula (II) where A-Z means a group S-CH=CH, S-CH2-CH2, S-CH2-CH2-CH2, CH= CH-CH=CH. Compounds show an antiallergic activity. Invention describes also a method of synthesis of the above indicated compounds, pharmaceutical compositio