Discovery and development of a novel class of phenoxyacetyl amides as highly potent TRPM8 agonists for use as cooling agents
作者:Alain Noncovich、Chad Priest、Jane Ung、Andrew P. Patron、Guy Servant、Paul Brust、Nicole Servant、Nathan Faber、Hanghui Liu、Nicole S. Gonsalves、Tanya L. Ditschun
DOI:10.1016/j.bmcl.2017.04.003
日期:2017.8
The paper presents the activity trends for a novel series of phenoxyacetyl amides as human TRPM8 receptor agonists. This series encompasses in vitro activity values ranging from the micromolar to the picomolar levels. Sensory evaluation of these molecules highlights their relevance as cooling agents for oral applications. The positive outcome of the complete evaluation of N-(1H-pyrazol-3-yl)-N-(th
N-glycinsulfonamide derivatives and uses as orexin receptor antagonists
申请人:Actelion Pharmaceuticals Ltd.
公开号:US08003654B2
公开(公告)日:2011-08-23
The invention relates to novel sulfonamide compounds of the formula (I)
and their use as orexin receptor antagonists.
该发明涉及一种新型磺酰胺化合物(I)及其作为促进睡眠荷尔蒙受体拮抗剂的用途。
COMPOUNDS USEFUL AS MODULATORS OF TRPM8
申请人:Priest Chad
公开号:US20130324557A1
公开(公告)日:2013-12-05
The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.