6-substituted-3<i>H</i>-1,3-benzothiazol-2-one compounds as TARP-gamma 8 dependent AMPA receptor antagonists

摘要

A TARP γ8 dependant AMPA receptor antagonist of the formula:;
wherein X is CH or N;

A is
;
and

R1 is as defined herein;

its pharmaceutically acceptable salts, uses, and methods for its preparation are described.

主权项

1. A compound of the formulaor a pharmaceutically acceptable salt thereof,wherein X is CH or N;A isandR1 is selected from the group consisting of
hydrogen, deuterium, fluoro, methyl, HO—(C1-C4)-alkyl, optionally substituted with with one or two methyl or deuterium groups, HO—(C1-C3)-alkoxy, optionally substituted with one or two methyl or deuterium groups, fluoro-(C1-C3)-alkyl, HO—(C1-C3)-alkoxy-methyl, optionally substituted with with one or two methyl groups, cyano-(C1-C3)-alkoxy, HO—(C1-C3)-alkylthio, optionally substituted with with one or two methyl groups, HO—(C1-C3)-alkyl-NH—, HO—(C1-C3)-alkyl-N(CH3)—, methylsulfinyl, acyl, aminocarbonyl, methylcarbonylmethoxymethyl, aminomethylcarbonyloxyethoxy, triazolylmethyl, 1-methyl-imidizol-2-ylthio, 5-hydroxymethyl-tetrahydrofuran-2-yl, 3-hydroxy-3-methylazetidin-1-yl, 3-methoxy-azetidin-1-yl 3-methoxy-3-methylazetidin-1-yl 4-hydroxypiperidin-1-yl, 4-hydroxy-4-methyl-piperidin-1-yl, 4-hydroxy-4-vinyl-piperidin-1-yl, 4-hydroxymethyl-piperidin-1-yl, 4-(2-hydroxyethyl)-piperindin-1-yl, morpholin-4-yl, 2-hydroxymethyl-morpholin-4-yl, morpholin-4-yl-ethoxy, and tetrahydropyran-4-yl, provided that when A is then R1 is not unsubstituted HO—(C1-C3)-alkoxy, deuterium substituted HO—(C1-C3)-alkoxy, or HO—(C1-C3)-alkythio.