DERIVATIVES OF 5-SUBSTITUTED 1,2,4-THIADIAZOLYL, METHOD OF THEIR SYNTHESIS (VERSIONS), PHARMACEUTICAL COMPOSITION, INTERMEDIATE COMPOUND AND METHOD OF ITS SYNTHESIS Russian patent published in 2003 - IPC

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of 1,2,4-thidiazole substituted by position 5 of the general formula (I) where X means N atom; R¹ means C_1-6-alkyl; R² means hydrogen atom; each of R³, R⁴, R⁵ is taken independently among hydrogen atom, trifluoromethyl group; means Ar², Ar²CH₂- or Het² where Ar² means phenyl; Het² means monocyclic heterocycle taken among thiadiazolyl, pyridinyl, pyrimidinyl or pyrazinyl, their N-oxide forms, pharmaceutically acceptable acid-additive salts and stereochemical isomeric forms. Invention describes also methods of synthesis of these compounds, intermediate substances used in synthesis and method of synthesis of intermediate substance. Compounds act as inhibitors of angiogenesis and therefore they can be used in treatment the following diseases: diabetic retinopathy, angiofibroma, psoriasis, osteoarthrosis and others. EFFECT: improved methods of synthesis, valuable medicinal properties of compounds. 10 cl, 3 tbl, 6 ex