INHIBITOR CONTAINING BICYCLIC DERIVATIVE, METHOD OF PREPARATION AND USE THEREOF Russian patent published in 2024 - IPC A61K35/00 C07D471/04 A61K31/437 

FIELD: medicine; pharmaceutics.

SUBSTANCE: invention relates to the field of drug synthesis, in particular to RET inhibitor compounds containing a bicyclic derivative. Disclosed are a compound of general formula (IX), a stereoisomer or a pharmaceutically acceptable salt thereof, in which X₃ is selected from N or CR₅; each of M₁ and M₂ is independently selected from CR_aa or N; each of G₁ and G₂ is independently selected from CR_aa or N; L is selected from communication, -(CH₂)_n1CR_aaR_bb-, -(CH₂)_n1NR_aaC(O)(CH₂)_n2-, -(CH₂)_n1C(O)(CR_aaR_bb)_m(CH₂)_n2-_; -(CH₂)_n1C(O)(CH₂)_m(CR_aaR_bb)_n2-, -(CH₂)_n1C(O)NR_cc(CR_aaR_bb)_n2-, -(CH₂)_n1(O)(CH₂)_n2- or -(CH₂)_n1NR_aa(CH₂)_n2-, R₅ is selected from cyano, -(CH₂)_n1C(O)NR_aaR_bb or -(CH₂)_n1P(O)R_aaR_bb; R₇ is selected from C_2-6alkynyl, 3-12-membered heterocyclyl containing 1-4 oxygen atoms, nitrogen atom or sulfur atom, -(C≡C)_n1CR_aaR_bb)_mR_cc, -(C≡C)_n1(CR_aaR_bb)_mR_cc, -(CH₂)_n1O(CH₂)_n2(CR_aaR_bb)_mR_cc, -(CH₂)_n1S(CH₂)_n2(CR_aaR_bb)_mR_cc, -(CH₂)_n1O(CH₂)_n2S(O)_mR_aa, -(CH₂)_n1O(CH₂)_n2S(O)(-NR_aa)(CH₂)_mR_bb, -(CH₂)_n1NR_aaC(O)R_bb, -(CH₂)_n1NR_aa(CH₂)_n2R_bb or -(CH₂)_n1S(O)(-NR_aa)(CH₂)_n2R_bb; compound of general formula (IX-D), a stereoisomer thereof or a pharmaceutically acceptable salt thereof; compound represented by specific structures; method of producing a compound of general formula (IX-A), a stereoisomer thereof or a pharmaceutically acceptable salt thereof; method of producing a compound of general formula (IX-B), a stereoisomer or a pharmaceutically acceptable salt thereof; method of producing a compound of general formula (IX-B), a stereoisomer or a pharmaceutically acceptable salt thereof; method of producing a compound of general formula (IX-C), a stereoisomer thereof or a pharmaceutically acceptable salt thereof; use of the disclosed compounds of their stereoisomers and their pharmaceutical salts in the preparation of medicinal preparations related to the RET inhibitor, and use of disclosed compounds of their stereoisomers and their pharmaceutical salts for treating diseases associated with RET.

EFFECT: creation of a class of compounds-inhibitors of RET, having excellent activity.

25 cl, 10 tbl, 176 ex