ESTROGEN RECEPTOR PROTEOLYSIS MODULATORS AND RELATED USES THEREOF Russian patent published in 2023 - IPC C07D409/12 C07D409/14 C07D413/14 C07D417/14 C07D471/04 C07D487/04 C07D487/08 C07D487/10 A61K31/381 A61K31/426 A61K31/4412 A61K31/454 A61K31/4545 A61K31/496 A61K31/551 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to bifunctional compounds of the general formula CLM-L-PTM having the properties of estrogen receptor inhibitors and their use in the treatment of estrogen receptor-associated breast cancer. In the general formula CLM-L-PTM, PTM is PTM-I or PTM-II, CLM is the chemical structure of (a) or (e), L is a chemical linker moiety comprising a chemical structural unit represented by the formula -(A^L)_q- where (A^L)_q is a group that is connected to CLM and PTM; X_PTM is O; each of X_PTM1 and X_PTM2 is independently N or CH; R_PTM1 is OH or OC_1-3 alkyl; R_PTM2 and R_PTM4 are independently selected from H, OH, halogen, CF₃ and OC_1-3 alkyl; R_PTM3 and R_PTM5 are H; W is CH₂ or C=O; each X is O; Z is O; G is H; Q₁, Q₂, Q₃ and Q₄ are N or CH; A is H or linear and branched C_1-6 alkyl; where n is 1, R is -OR', -NR'R" or -CR'R"-, wherein R is covalently bonded to the chemical linker moiety; R' and R” are independently selected from bond, H, C_1-6 alkyl; is a bond that may or may not provide a stereospecific configuration; q is an integer from 3 to 15; each A^L is independently selected from a bond, CR^L1 R^L2, O, NR^L3, CONR^L3, CO and C_3-8 heterocyclyl; and R^L1, R^L2 and R^L3 are each independently H, halogen and C_1-8 alkyl, each heterocyclyl having one or two heteroatoms, each heteroatom independently selected from nitrogen.

EFFECT: obtaining estrogen receptor proteolysis modulators.

8 cl, 2 dwg, 5 tbl, 245 ex