BIPHENYL DERIVATIVES HAVING BIOLOGICAL ACTIVITY, PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATMENT BASED ON SAID COMPOUNDS AND USE THEREOF Russian patent published in 2020 - IPC C07C43/205 C07C211/27 C07C211/48 A61K31/85 A61K31/135 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, which have NMDA receptor antagonist activity. In formula IX, -H, a halogen atom or -CH₃; Z is -OR' or -NR'R''; linker L denotes a group -(C_0-2alkylene)-Y-(C_0-2alkylene)-, where C₀alkylene refers to a single bond and where Y represents a group -O- or -NR'-; R1 denotes -H, -OR', -NR'R'' or -NR'-SO₂-(C_1-6-alkyl); R2 is -H, -OR' or -NR'R''; R in each case means H; R' and R'' in each case independently represent groups selected from H and C_1-6-alkyl; and m is 3, with the proviso that X, R1 and R2 are not all simultaneously H, and with the proviso that when one group of R1 and R2 is -NH₂ and the other is -H, X is -H, and L is -CH₂-O-, then Z is not -OH. Invention also relates to a pharmaceutical composition for inhibiting NMDA receptors containing a pharmacologically effective amount of one or more compounds of formula I or their pharmaceutically acceptable salts and one or more pharmaceutically acceptable adjuvants. In formula IX, -H, a halogen atom or -CH₃; Z is -OR' or -NR'R''; linker L denotes a group -(C_0-2alkylene)-Y-(C_0-2alkylene)-, where C₀-alkylene denotes a simple bond and where Y denotes a -O- or -NR'- group; R1 denotes -H, -OR', -NR'R'' or -NR'-SO₂-(C_1-6-alkyl); R2 is -H, -OR' or -NR'R''; R in each case means H; R' and R'' in each case independently represent groups selected from H and C_1-6-alkyl; and m is equal to 3. Also described is a method of treating a disorder or disease accompanied by high activation of the NMDA receptor, comprising a step, wherein an effective amount of one or more compounds of formula I or pharmaceutically acceptable salts or a pharmaceutical composition thereof is administered to a patient in need thereof. In formula IX, -H, a halogen atom or -CH₃; Z is -OR' or -NR'R''; linker L denotes a group - (C_0-2 alkylene)-Y-(C_0-2 alkylene)-, where C₀ alkylene refers to a single bond and where Y represents a group -O- or -NR'-; R1 denotes -H, -OR', -NR'R'' or -NR'-SO₂-(C_1-6-alkyl); R2 is -H, -OR' or -NR'R'' ; R in each case means H; R' and R'' in each case independently represent groups selected from H and C_1-6 -alkyl; and m is equal to 3. Also disclosed is use of compounds of formula I as inhibitors of NMDA-receptors. In formula IX, -H, a halogen atom or -CH₃; Z is -OR' or -NR'R''; linker L denotes a group -(C_0-2alkylene)-Y-(C_0-2alkylene)-, where C₀-alkylene denotes a simple bond, and where Y denotes a -O- or -NR'-group; R1 denotes -H, -OR', -NR'R'' or -NR'-SO₂-(C_1-6-alkyl); R2 is -H, -OR' or -NR'R''; R in each case means H; R' and R'' in each case independently represent groups selected from H and C_1-6 -alkyl; and m equals 3.

EFFECT: disclosed are biphenyl derivatives having biological activity, pharmaceutical compositions and methods of treatment based on said compounds and use thereof.

32 cl, 3 tbl, 4 ex, 2 dwg