FIELD: pharmaceuticals.
SUBSTANCE: O-aminoheteroaryl-alkynyl-containing compound, method of preparation and use thereof. The invention relates to a compound of formula (I), its deuterated derivative or a pharmaceutically acceptable salt thereof, a method for its preparation and its use for the preparation of an RFGF kinase inhibitor and/or an RET kinase inhibitor or for the preparation of a drug for the treatment of a tumor associated with kinase overexpression or overactivation FRFR or RET kinases. In general formula (I), R is amino; M represents C or N, and when M represents N, R2 is absent; R1 select en from the group consisting of: -H, halogen, cyano, amino, C3-6 cycloalkyl; mono- or di- C1-4 alkylamino; C1-4 alkyl unsubstituted or substituted with one hydroxyl, C1-4 alkoxy, trifluoromethoxy, mono- or di- C1-4 alkylamino or 1–5 halogens; C1-4 alkoxy, unsubstituted or substituted with one hydroxyl, C1-4 alkoxy, mono- or di- C1-4 alkylamino or 1–5 halogens; C1-4 alkylamido unsubstituted or substituted with one mono- or di- C1-4 alkylamino; C3-6 cycloalkylamido unsubstituted or substituted with one mono- or di- C1-4 alkylamino; C2-4 alkenylamido, unsubstituted or substituted with one mono- or di- C1-4 alkylamino; R2 is selected from -H, halogen, C1 alkyl; R3 is selected from -H, halogen, cyano, C1-4 alkoxy, C1-4 alkyl, unsubstituted or substituted with 1–5 halogens; R4 is selected from -(CH2)nN(R7)(R8), -OR9; R7 and R8 together with the neighboring N atom form a 5–6-membered aliphatic heterocycle with 1–2 N atoms in the ring, unsubstituted or substituted with C1-4 alkyl; R9 selected from 5-6-membered aliphatic heterocycle with 1–2 N atoms in the ring, unsubstituted or substituted with C1-4 alkyl; each halogen is independently selected from the group consisting of F, Cl, Br and I; n=0–3.
EFFECT: obtaining O-aminoheteroarylalkynyl containing compound.
18 cl, 7 dwg, 8 tbl, 55 ex
(I)
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