| 摘要 |
FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention relates to new derivatives of 2-aryl-8-oxodihydropurine of the formula (I) eliciting selective affinity to BZw3-receptor, method for its preparing, pharmaceutical composition and agent comprising thereof and to intermediate compound of the formula (II) used for preparing derivatives of 2-aryl-8-oxodihydropurine. In compounds of the formula (I) W represents hydrogen atom, lower alkyl group, halogen atom, lower alkoxy- group, amino-group, mono- or di-lower alkylamino-group or unsubstituted phenyl group either phenyl group substituted with trifluoromethyl; X represents hydrogen atom, lower alkyl group, cycloalkyl-lower alkyl group, phenyl-lower alkyl group, lower alkenyl group, carbamoyl group, di-lower alkylcarbamoyl group or group of the formula (Q): -CH(R3)CONR(R1)(R2) wherein R1 represents lower alkyl group, lower alkenyl group, cycloalkyl group, cycloalkyl-lower alkyl group or hydroxy-lower alkyl group; R2 represents lower alkyl group, cycloalkyl group, unsubstituted phenyl group or phenyl group substituted with halogen atom, lower alkoxy- group or hydroxy-group, unsubstituted phenyl-lower alkyl group or substituted with halogen atom, lower alkoxy-group or hydroxy-group; or R1 and R2 can be combined with adjacent nitrogen atom with formation if piperidine ring, pyrrolidine ring, morpholine ring or piperazine ring and these rings can be optionally substituted with one or some lower alkyl groups; R3 represents hydrogen atom, lower alkyl group or hydroxy-lower alkyl group; Y represents hydrogen atom, lower alkyl group, phenyl-lower alkyl group or group of the formula (Q) indicated above; A represents unsubstituted phenyl group or phenyl group substituted with halogen atom, lower alkyl, nitro-group, lower alkoxy-group, trifluoromethyl or hydroxy- group or unsubstituted heteroaryl group taken among pyridyl, thienyl or furyl. In compounds of the formula (II) W represents hydrogen atom, lower alkyl group, halogen atom, lower alkoxy-group, unsubstituted phenyl group or phenyl group substituted with trifluoromethyl; Y2 represents hydrogen atom, lower alkyl group or phenyl-lower alkyl group; A represents unsubstituted phenyl group or phenyl group substituted with halogen atom, lower alkyl, nitro-group, lower alkoxy-group, trifluoromethyl or hydroxy-group or unsubstituted heteroaryl group taken among pyridyl, thienyl or furyl. Compounds of the formula (I) can be used in anxiolytic agents for treatment of diseases associated with anxiety state. EFFECT: improved preparing method, valuable medicinal properties of compounds. 15 cl, 24 tbl, 323 ex
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