PYRAZOLOTRIAZINE DERIVATIVES AS SELECTIVE INHIBITORS OF CYCLIN-DEPENDENT KINASES Russian patent published in 2018 - IPC C07D487/04 A61K31/53 A61P9/00 A61P31/00 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of the general formula (I)

,

in which R¹ is H or -CH₃; R² is -R⁸, -Q-R⁸, -R⁹, -Q-(CH₂)_n-R⁹, -(CH₂)_n-R⁹, -(CH₂)_m-NH-(CH₂)_n-R⁹, -CO-NH-(CH₂)_n-R⁹, -CO-NR¹⁰-(CH₂)_n-R⁹, -(CH₂)_a-(Q)_b-(CH₂)_c-(G¹)_d-(CH₂)_e-(G²)_f-(CH₂)_g-R⁸, -(Q)_b-(CH₂)_m-(G¹)_d-(CH₂)_e-R⁸, -Q-R¹⁰; R³ is i) -OH, -NH₂, -F, -Cl, -Br, -I, -CN, -OR¹¹, -CO-O-R¹¹, -NR¹¹-CO-OR¹², -NHR¹¹, -NR¹¹R¹², -CONR¹¹R¹², -O-CO-NR¹¹R¹², -O-CO-OR¹¹, -CH₃, -NR¹¹-CO-NR¹²R¹³, -SO₂NR¹¹R¹², -N=S(=O)R¹¹R¹², -SR¹¹, -S(=O)R¹¹, -NR¹¹-S(=O)R¹², -O-S(=O)R¹¹, -SO₂-R¹¹, -NR¹¹-SO₂-R¹², -O-SO₂-R¹¹, -SO(=NR¹¹)-R¹², -O-CO-R¹¹, -NR¹¹-CO-R¹², -CF₃; ii) unbranched or branched C₁-C₈-alkyl, C₃-C₈-cycloalkyl; iii) 4-membered heterocyclyl containing one heteroatom N, 5-membered heterocyclyl containing one heteroatom N, 6-membered heterocyclyl containing one to two heteroatoms N, O, 6-membered cycloalkenyl, 6-membered aryl, 5-membered heteroaryl containing one to four N, S, O, 6-membered heteroaryl heteroatoms containing one heteroatom N, wherein all of the above cyclic systems can be substituted with 1 to 2 substituents selected from Z¹ and Z²; Z¹ and Z², if they are attached to the same carbon atom, can together represent an atom = O which forms a carbonyl group with a carbon atom to which they are attached Z¹ and Z²; R³ together with R⁴ can form a carbocyclic or heterocyclic 5-, 6- or 7-membered ring with two carbon atoms of the benzene ring, to which R³ and R⁴, and said 5-, 6- or 7-membered ring may be partially saturated or unsaturated and may be substituted with 1 substituent selected from Z¹; R⁴-R⁷ independently of each other are -H, -F, -Cl, -CH₃; values of other radicals are given in the patent claim. Invention also relates to use of the compound for preparation of a pharmaceutical composition and to the pharmaceutical composition with CDK7 inhibiting activity.

EFFECT: new compounds of general formula (I) with inhibitory CDK7 activity were obtained.

7 cl, 7 tbl