FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to novel derivatives of thiazole of the formula (I) where R1 means the group of formulas (a) , (b) , (c) ; R2 means the group of the formula (d) where Het means five- or hexa-membered heterocyclic group that is substituted with R9 and cycle can contain oxygen atom additionally, except for nitrogen atom; R3 means hydrogen atom, alkyl, cycloalkyl, phenyl group; R4 means hydrogen atom, phenyl group; R5-R8 each means independently hydrogen atom; R9 means the group of the formula (e) R10 and (f) means phenyl group; a-i means 0 0 or whole positive number, i. e. a and b = 0-4, is equal 0 or 1; f is equal 0 when d is equal 0; sum c, d and e is equal ≥ 1 and ≅ 4; f and h is equal 0 or 1 being i is not equal 0 when h is equal 1; sum g, h and i is equal ≥ 2 ≅ 5, and their pharmaceutically acceptable salts. Invention relates to also intermediate compounds of the formula (II) where R1 and R3 are given above under condition that when compound (II) is acid or ester where R1 means (b), (c) then R3 is not hydrogen atom or methyl group. Method of synthesis of compound of the formula (I) involves interaction of compound of the formula (II) with amine of the formula (III) or its salt. Invention relates to also pharmaceutical composition showing ability to suppress binding adhesive proteins with vitronectin receptors and it involves compound of the formula (I) and therapeutically acceptable carrier. EFFECT: new compounds indicated above, improved method of synthesis, valuable pharmacological properties. 9 cl, 6 dwg, 1 tbl, 38 ex
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Authors
Dates
2001-05-10—Published
1999-01-05—Filed