NOVEL PIPERIDINE-SUBSTITUTED DIAMINOTHIAZOLES Russian patent published in 2010 - IPC C07D417/14 C07D417/12 A61K31/427 A61K31/4523 A61K31/5377 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula and their pharmaceutically acceptable salts and esters. The disclosed compounds have cdk4 inhibition properties. In formula (I) n equals 0 or 1; R¹ and R² are each independently selected from a group consisting of H, lower alkyl, CO₂R⁵, SO₂R⁶ and COR⁶; or alternatively, R¹ and R² can form a ring containing 5-6 atoms in the ring, where the said ring contains carbon atoms, where the said carbon atoms are optionally substituted with oxygen, and the said atoms in the ring are optionally substituted with OR⁶; R³ is selected from a group consisting of H, lower alkyl, O-lower alkyl, halogen, OH, CN, NO₂ and COOH; R⁴ is selected from a group consisting of H, lower alkyl, C₃-C₆-cycloalkyl, O-lower alkyl, halogen, NO₂, S-lower alkyl, NR⁵R⁶, CONR⁷R⁸, OH and CN; or alternatively R³ and R⁴, together with two carbon atoms and the bond between them from the benzene ring, to which R³ and R⁴ are bonded, can form a ring containing 5-7 atoms, where the said 5-7-member ring contains carbon atoms, where the said carbon atoms are optionally substituted with one or two heteroatoms selected from O and N, and the said atoms in the ring are optionally substituted with CO₂R⁶; R⁴ represents H or halogen; R⁵ and R⁶ are each independently selected from a group consisting of H and lower alkyl; R⁷ and R⁸ each represents H. The invention also relates to a pharmaceutical composition for treating or controlling diseases progression of which can be enhanced by inhibiting cdk4, containing an effective amount of the disclosed compound as an active ingredient, to use of disclosed compounds for preparing medicinal agents and method of producing said compounds.

EFFECT: more effective treatment.

30 cl, 1 tbl, 142 ex