COMPOUNDS TARGETING TAU PROTEIN AND RELATED USE THEREOF Russian patent published in 2023 - IPC C07D471/04 C07D401/04 C07D401/14 C07D417/14 A61K31/437 A61K31/4439 A61K31/444 A61K31/496 A61K31/4985 A61K31/517 A61K31/519 A61K31/53 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound having the chemical structure ULM-L-PTM, or a pharmaceutically acceptable salt thereof, wherein ULM has the chemical structure represented by structure (aa), where R_14a is either H or C_1-6 alkyl; R₉ is H; R₁₀ is H, ethyl, isopropyl, tert-butyl or sec-butyl; R₁₁ is structure (b) or (c); R₁₂ is H; R₁₃ is either C_1-6 alkyl or C_1-6 alkylcarbonyl; R₁₅ is selected from H, structures (d) and (e); dotted line indicates the site of attachment of L; or ULM has the chemical structure represented by (a), where W is either CH₂ or C=O; each X is O; Z is O; G is H; Q₁ , Q₂ , Q₃ and Q₄ represent a carbon atom C, substituted by the group R'; A is H; R is selected from -CONR'R”, -OR', -NR'R”, -CR'R”-, -CR'NR'R”-, -Cl, -F, -Br, -I, -CF₃, -CN, -NR'CONR'R”, -CONR'COR”, -CO₂R', -C(C=N-OR')R”, -CR'=CR'R”, -CCR' or -OCF₃; R' and R” are H; is a bond that may or may not provide a stereospecific configuration; n is either 1, 2, 3 or 4; PTM is represented by a chemical structure selected from the group shown in the claims, and where R¹, R² and R³ independently represent H or optionally substituted with 1-3 halogens C_1-6alkyl; and R⁷, R⁸ , R⁹ and R¹⁰, each represents either 1 or 2 substituents independently selected from H, C_1-6alkyl, C_1-6haloalkyl, halogen or cyano; and L is represented by the formula -(A)_q- where A is a group connected to either an ULM or PTM fragment; and q is an integer from 1 to 19, where A is selected from CR^L1R^L2, O, NR^L3, CO, CR^L1=CR^L2, C≡, cyclopropyl, cyclobutyl, bicyclopentyl, oxetanyl, azetidinyl, piperidinyl, piperazinyl, morpholinyl, phenyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, and cyclopropyl, cyclobutyl, bicyclopentyl, oxetanyl, azetidinyl, piperidinyl, piperazinyl, morpholinyl, phenyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl are optionally substituted with either 1 or 2 R ^L1 ; each of R^L1, R^L2 and R^L3 is independently selected from H, halo, C_1-8alkyl, OH, CN, CF₃, CHF₂ and CH₂F. The invention relates to a pharmaceutical composition containing an effective amount of a compound of the invention and a pharmaceutically acceptable carrier for use in the treatment of a disease or disorder associated with tau protein.

EFFECT: obtaining compounds for use in the treatment of a disease or disorder associated with a tau protein.

19 cl, 1 dwg, 2 tbl