abstract |
FIELD: chemistry. n SUBSTANCE: invention relates to a compound of the general formula (I) n , n in which R 1 is H or -CH 3 ; R 2 is -R 8 , -Q-R 8 , -R 9 , -Q-(CH 2 ) n -R 9 , -(CH 2 ) n -R 9 , -(CH 2 ) m -NH-(CH 2 ) n -R 9 , -CO-NH-(CH 2 ) n -R 9 , -CO-NR 10 -(CH 2 ) n -R 9 , -(CH 2 ) a -(Q) b -(CH 2 ) c -(G 1 ) d -(CH 2 ) e -(G 2 ) f -(CH 2 ) g -R 8 , -(Q) b -(CH 2 ) m -(G 1 ) d -(CH 2 ) e -R 8 , -Q-R 10 ; R 3 is i) -OH, -NH 2 , -F, -Cl, -Br, -I, -CN, -OR 11 , -CO-O-R 11 , -NR 11 -CO-OR 12 , -NHR 11 , -NR 11 R 12 , -CONR 11 R 12 , -O-CO-NR 11 R 12 , -O-CO-OR 11 , -CH 3 , -NR 11 -CO-NR 12 R 13 , -SO 2 NR 11 R 12 , -N=S(=O)R 11 R 12 , -SR 11 , -S(=O)R 11 , -NR 11 -S(=O)R 12 , -O-S(=O)R 11 , -SO 2 -R 11 , -NR 11 -SO 2 -R 12 , -O-SO 2 -R 11 , -SO(=NR 11 )-R 12 , -O-CO-R 11 , -NR 11 -CO-R 12 , -CF 3 ; ii) unbranched or branched C 1 -C 8 -alkyl, C 3 -C 8 -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 Z 1 and Z 2 ; Z 1 and Z 2 , 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 Z 1 and Z 2 ; R 3 together with R 4 can form a carbocyclic or heterocyclic 5-, 6- or 7-membered ring with two carbon atoms of the benzene ring, to which R 3 and R 4 , and said 5-, 6- or 7-membered ring may be partially saturated or unsaturated and may be substituted with 1 substituent selected from Z 1 ; R 4 -R 7 independently of each other are -H, -F, -Cl, -CH 3 ; 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. n EFFECT: new compounds of general formula (I) with inhibitory CDK7 activity were obtained. n 7 cl, 7 tbl |