BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT

摘要

The present invention is directed to a compound of Formula I;;or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.

主权项

1. A compound of Formula Ior a pharmaceutically acceptable salt thereof; wherein:
R is selected from the group consisting of C1-6 alkyl which is unsubstituted or substituted with a substituent selected from the group consisting of —N(C1-6 alkyl)2, C6-12 aryl, C6-12 aryloxy and heteroaryl; each R1 and R2 are independently H or C1-6 alkyl; R3 is selected from the group consisting of C6-12 aryl and heteroaryl; each R4 independently is selected from the group consisting of C1-6 alkyl, and C1-6 alkoxy, wherein said C1-6 alkyl and the alkyl portion of said C1-6 alkoxy are independently unsubsubstituted or substituted with a substituent selected from the group consisting of hydroxyl, —C(═O)OH, —C(═O)O—C1-6 alkyl, —C(═O)-heterocyclyl, and —N(C1-6 alkyl)2; R5 is H or C1-6 alkyl; X is selected from the group consisting of a covalent bond, O, NR5, —S(═O)—, and —S(═O)2—; m is 1 or 2; and n is 0 or 1; with the proviso that when R is an unsubstituted C1-6 alkyl, then either (1) X is other than a covalent bond, or (2) R4 is C1-6 alkoxy, wherein the alkyl portion of said C1-6 alkoxy is substituted with a —N(C1-6 alkyl)2 substituent.