FIELD: organic chemistry, chemical technology, medicine, endocrinology, pharmacy.
SUBSTANCE: invention relates to new derivatives of thienopyrimidine of the formula (I)
or its salts that elicit significant GnRH-antagonistic activity and can be used for prophylaxis or treatment of hormone-dependent diseases. In compounds of the formula (I) each R1 and R2 represents hydrogen atom, hydroxy-group, (C1-C4)-alkoxy-group, (C1-C4)-alkoxycarbonyl group or (C1-C4)-alkyl group that can be substituted with hydroxy-group, (C1-C4)-alkylcarbonyloxy-group; R3 represents hydrogen atom, halogen atom, hydroxy-group or (C1-C4)-alkoxy-group that can be substituted with (C1-C4)-alkoxy-group; or two adjacent R3 taken in common can form (C1-C4)-alkylenedioxy-group; R4 represents hydrogen atom or (C1-C4)-alkyl group; R6 represents (C1-C4)-alkyl group that can be substituted with (C1-C4)-alkoxy-group; or group of the formula:
wherein R5 represents hydrogen atom; or R4 and R5 taken in common with nitrogen atom to which group R6 is joined can form 5-6-membered nitrogen-containing heterocycle; n represents a whole number from 0 to 5. Invention relates also to a method for preparing compounds of the formula (I), pharmaceutical composition based on thereof and a method for antagonization of gonadotropin-releasing hormone in mammals.
EFFECT: improved preparing method, valuable medicinal properties of compounds.
16 cl, 1 dwg, 41 ex
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