AMINOTHIAZOLE INHIBITORS OF CYCLIN-DEPENDENT KINASES Russian patent published in 2003 - IPC

FIELD: organic chemistry, biochemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of aminothiazole of the formula (I) and their pharmaceutically acceptable salts wherein R₁ and R₂ mean independently each of other hydrogen, fluorine atom or lower alkyl; R₃ means heteroaryl taken among oxazolyl that is substituted with one or some substituents taken among a lower alkyl, halogen atom, carbamoyl, alkyloxycarbonyl, alkyl- carbonyloxy or benzoxazole; R₄ means hydrogen atom, CO-alkyl that can be optionally substituted with halogen atom, alkoxy, hydroxy, alkyl- oxycarbonyl, alkylcarbonyloxy, amino, carbamoyl; CO-cycloalkyl; CO-aryl wherein aryl represents phenyl that can be optionally substituted with halogen atom, lower alkyl, alkoxy, amino, cyano or naphthyl group and so on; or COO-alkyl; COO-cycloalkyl; COO-phenyl; COO-alkyl- phenyl; SO₂-alkyl; SO₂-phenyl; C(NCN)NH-phenyl wherein phenyl can be optionally substituted with halogen atom; R₅ means hydrogen atom; m means a whole number from 0 to 2; n = 0. Invention relates also to a pharmaceutical composition eliciting as an inhibitor of protein kinase that comprises compound of the formula (I) and a pharmaceutically acceptable carrier and to a pharmaceutical composition eliciting effect of protein kinase inhibitor containing compound of the formula (I), a pharmaceutically acceptable carrier and an anticancer agent. Invention relates also to method for inhibition of activity of cyclin-dependent kinases involving administration of effective dose of compound of the formula (I) in mammal needing in such treatment. Invention provides preparing novel derivatives of isothiazole carboxylic acid. EFFECT: valuable medicinal properties of compounds. 26 cl, 2 tbl, 639 ex