NOVEL INDOL CARBOXYLIC ACID BISPYRIDYL CARBOXAMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD AND COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT
申请人:SEONG Churlmin
公开号:US20090258876A1
公开(公告)日:2009-10-15
Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT
2c
receptors, act selectively on the 5-HT
2c
receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT
2c
receptors.
current challenges in the field of C–H functionalization is the development of new removable/modifiable directinggroups (DGs). We report here the 4,6-dimethoxy-1,3,5-triazin-2-yloxy group as a new readily removable/modifiable DG for the regioselectiveacetoxylation of 2-(aryloxy)-4,6-dimethoxy-1,3,5-triazine. This developed phenol-derived DG can be easily removed to offer synthetically versatile pyrocatechols