DERIVATIVES OF HYDANTOINS, THIOHYDANTOINS, PYRIMIDINEDIONES AND THIOXOPYRIMIDINEDIONES, METHOD FOR THEIR PREPARING (VARIANTS), INTERMEDIATE COMPOUNDS AND PHARMACEUTICAL COMPOSITION Russian patent published in 2006 - IPC C07D403/04 C07D403/06 C07D403/14 C07D405/14 C07D409/14 C07D417/14 A61K31/513 A61K31/4178 A61K31/427 A61P35/00 A61P3/10 A61P1/04 A61P43/00 

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to new compounds of the general formula (I) in racemic form, enantiomer form or in any combinations of these forms possessing affinity to somatostatin receptors. In the general formula (I): R1 means phenyl; R2 means hydrogen atom (H) or -(CH₂)_p-Z3 or one of the following radicals: and Z3 means (C₃-C₈)-cycloalkyl, possibly substituted carbocyclic or heterocyclic aryl wherein carbocyclic aryl is chosen from phenyl, naphthyl and fluorenyl being it can be substituted, and heterocyclic aryl is chosen from indolyl, thienyl, thiazolyl, carbazolyl, or radicals of the formulae and and it can be substituted with one or some substitutes, or also radical of the formula: R4 means -(CH₂)_p-Z4 or wherein Z4 means amino-group, (C₁-C₁₂)-alkyl, (C₃-C₈)-cycloalkyl substituted with -CH₂-NH-C(O)O-(C₁-C₆)-alkyl, radical (C₁-C₆)-alkylamino-, N,N-di-(C₁-C₁₂)-alkylamino-, amino-(C₃-C₆)-cycloalkyl, amino-(C₁-C₆)-alkyl-(C₃-C₆)-cycloalkyl-(C₁-C₆)-alkyl, (C₁-C₁₂)-alkoxy-, (C₁-C₁₂)-alkenyl, -NH-C(O)O-(C₁-C₆)-alkyl, possibly substituted carbocyclic or heterocyclic aryl; p = 0 or a whole number from 1 to 6 if it presents; q = a whole number from 1 to 5 if it presents; X means oxygen (O) or sulfur (S) atom n = 0 or 1. Also, invention relates to methods for preparing compounds of the general formula (I), intermediate compounds and a pharmaceutical composition. Proposed compounds can be used in treatment of pathological states or diseases, for example, acromegaly, hypophysis adenomas, Cushing's syndrome and others.

EFFECT: improved preparing method, valuable medicinal properties of compounds and composition.

11 cl, 2 tbl