DIAMINOTHIAZOLES POSSESSING PROPERTY OF CYCLIN-DEPENDENT KINASE 4 INHIBITOR Russian patent published in 2007 - IPC C07D277/42 C07D417/06 C07D417/12 A61K31/426 A61K31/427 A61P35/00 

FIELD: organic chemistry, biochemistry, medicine, oncology, pharmacy.

SUBSTANCE: invention relates to novel diaminothiazoles of the formula (I) , their pharmaceutically acceptable salts and esters, and to a pharmaceutical composition based on thereof. Proposed compounds inhibit activity of cyclin-dependent kinase 4 (Cdk4), shows selectivity with respect to Cdk2 and Cdk1 and can be used in treatment against cancer, in particular, against solid tumors. In the general formula (I) R² and R³ represent hydrogen atom; R⁴ is chosen from group comprising lower alkyl, (C₃-C₆)-cycloalkyl, O-lower alkyl, halogen atom, -NO₂, S-lower alkyl, -CF₃ and -CN; R⁵ is chosen from group comprising hydrogen atom, O-lower alkyl, lower alkyl, halogen atom and -OH, or, alternatively, R⁴ and R in common with two carbon atoms and a bond binding them belonging to benzene cycle (C) to which R⁴ and R⁵ are bound can form a cycle consisting of 5-6 atoms comprising one or two heteroatoms chosen from oxygen atom and optionally substituted with (C₁-C₄)-alkyl; R⁶ and R are chosen independently from group comprising hydrogen atom, lower alkyl and -COOR¹², or, alternatively, group -NR⁶R⁷ can mean cycle consisting of 5-6 atoms optionally comprising heteroatom chosen from nitrogen or oxygen atoms; R⁸ and R⁹ are chosen independently from group comprising hydrogen atom and lower alkyl; R¹⁰ is chosen from group comprising hydrogen atom, lower alkyl, lower alkyl substituted with hydroxyl, and -COOR¹²; R¹¹ is chosen from group comprising hydrogen atom, lower alkyl and -COOR¹² wherein R¹² means lower alkyl; m can mean 1 or 2; n can mean 0, 1 or 2 under condition that if m means 2 and R⁴ means fluorine atom then R⁵ is not hydrogen atom, and under condition if m means 1 and R⁴ means lower alkyl then R⁵ is not hydroxyl.

EFFECT: valuable biochemical and medicinal properties of compounds and pharmaceutical compositions.

20 cl, 6 sch, 3 tbl, 153 ex