114500-32-2Relevant articles and documents
Novel sulfamoyl benzamides as selective CB2 agonists with improved in vitro metabolic stability
Sellitto, Ian,Bourdonnec, Bertrand Le,Worm, Karin,Goodman, Allan,Savolainen, Markku A.,Chu, Guo-Hua,Ajello, Christopher W.,Saeui, Christopher T.,Leister, Lara K.,Cassel, Joel A.,DeHaven, Robert N.,LaBuda, Christopher J.,Koblish, Michael,Little, Patrick J.,Brogdon, Bernice L.,Smith, Steven A.,Dolle, Roland E.
scheme or table, p. 387 - 391 (2010/04/06)
A lead optimization campaign in our previously reported sulfamoyl benzamide class of CB2 agonists was conducted to improve the in vitro metabolic stability profile in this series while retaining high potency and selectivity for the CB2 receptor. From this study, compound 14, N-(3,4-dimethyl-5-(morpholinosulfonyl)phenyl)-2,2-dimethylbutanamide, was identified as a potent and selective CB2 agonist exhibiting moderate in vitro metabolic stability and oral bioavailability. Compound 14 demonstrated in vivo efficacy in a rat model of post-surgical pain.
CB2 selective sulfamoyl benzamides: Optimization of the amide functionality
Goodman, Allan J.,Ajello, Christopher W.,Worm, Karin,Bourdonnec, Bertrand Le,Savolainen, Markku A.,O'Hare, Heather,Cassel, Joel A.,Stabley, Gabriel J.,DeHaven, Robert N.,LaBuda, Christopher J.,Koblish, Michael,Little, Patrick J.,Brogdon, Bernice L.,Smith, Steven A.,Dolle, Roland E.
scheme or table, p. 309 - 313 (2011/02/26)
Previous research within our laboratories identified sulfamoyl benzamides as novel cannabinoid receptor ligands. Optimization of the amide linkage led to the reverse amide 40. The compound exhibited robust antiallodynic activity in a rodent pain model whe
PYRIMIDINES, TRIAZINES AND THEIR USE AS PHARMACEUTICAL AGENTS
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Page/Page column 37, (2009/10/22)
A compound of formula (I) and its pharmaceutically acceptable salts or solvates and physiologically hydrolysable, solubilising or immobilisable derivatives wherein: Ar is a 5-membered heteroaryl ring wherein X1 and X2 are one or two
