DERIVATIVE OF THIOBENZIMIDAZOLE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEREOF Russian patent published in 2004 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention describes a derivative of thiobenzimidazole represented by the formula (1):

or its medicinally acceptable salt wherein R¹ and R² represent simultaneously or independently hydrogen, halogen atom, trihalogenmethyl group, cyano-group, hydroxy-group, alkyl group with 1-4 carbon atoms, alkoxy-group with 1-4 carbon atoms; or R¹ and R² form in common -O-CH₂-O-, -O-CH-CH₂-O- or -CH₂-CH₂-CH₂-; A represent a simple bond, linear alkylene group with 1-6 carbon atoms optionally substituted with alkyl group with 1-4 carbon atoms, substituted or unsubstituted phenylene group or thiophenylene group; E represents COOR³ or tetrazolyl group; R³ represents hydrogen atom or linear or branched alkyl group with 1-4 carbon atoms; G represents unsubstituted linear alkylene group with 1-6 carbon atoms, -CH₂CO-, -CH₂-CH₂-O-, -CH₂CONH-, -CO-, -SO₂-, -CH₂-CH₂-S- or -CH₂S-; m is a whole number from 0 to 2; J has different values depending on m and A; X represents CH or nitrogen atom. Also, invention describes a pharmaceutical composition eliciting activity inhibiting human chymase based on this compound. Indicated composition is a possible prophylactic and/or curative agent in different diseases wherein human chymase is involved.

EFFECT: valuable medicinal and biochemical properties of compound.

14 cl, 52 tbl, 24 ex