FIELD: pharmaceuticals.
SUBSTANCE: invention relates to a compound of formula (I) or its tautomer, stereoisomer, optical isomer or pharmaceutically acceptable salt, where X is selected from a chemical bond, -O- and -CH2-; Y is N, Y1 is C, Y2 is -CH-, Y3 is N, and Y4 is -CH-; X2 is selected from the chemical bond, -(CH2)p - and -NH-, where p is 1; 
means that a chemical bond is absent or present; R is selected from phenyl or pyridinyl, wherein each phenyl or pyridinyl is unsubstituted or substituted with at least one substituent selected from R1; each R1, if present, is independently selected from hydrogen, halogen, -OH, amino, -NHC1-6 alkyl, -N(C1-6alkyl)2, cyano, C1-6 alkyl C1-6 alkoxi and -SC1- 6 alkyl; R2 is selected from H, halogen, hydroxyl, amino; R3 represents H; ring A is selected from heterocycloalkyl containing from 4 to 6 ring atoms, 6-8 membered heterobridged cyclyl, 8-10 membered heterofused cyclyl or 7-10 membered heterospirocyclyl, the heteroatoms in the heterocycloalkyl, heterobridged cyclyl, heterofused cyclyl and heterospirocyclyl being independently selected from O and N, and the number of heteroatoms selected from 1, 2, 3 or 4; R4 is at any substitutable position on ring A and is independently selected from -H, -OH, halogen, -CN, substituted or unsubstituted C1-6 alkyl, -(CH2)m -OH, -(CH2)m - COOH, -(CH2)m -CO-NH2, -CO-(CH2)m -NH2, -CO-CR4aR4b-OH and -CO-R4b; R4a is selected from hydrogen and unsubstituted or substituted C1-4 alkyl; R4b is selected from H, unsubstituted or substituted C1-6 alkyl and unsubstituted or substituted C3-6 cycloalkyl, the substituent is independently selected from -OH, -NH2 and halogen, and the number of substituents is selected from 1, 2 and 3; n is selected from 1, 2, 3 and 4. The invention also relates to a pharmaceutical composition having inhibitory activity against TRK, based on these compounds.
I
EFFECT: obtaining new compounds that have a strong inhibitory effect on various cells containing TRK mutations and tumors, have good safety and can be used in medicine as medicinal products for the treatment of hyperproliferative diseases.
22 cl, 1 dwg, 6 tbl, 47 ex
| Title | Year | Author | Number |
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|
RU2778294C2 |
