- Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin- 7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain
-
We report the synthesis and SAR of a series of novel azaindole CB 2 agonists. 6-Azaindole 18 showed activity in an acute pain model but was inactive in a chronic model. 18 is a Pgp substrate with low brain penetration. The template was redesign
- Giblin, Gerard M. P.,Billinton, Andrew,Briggs, Michael,Brown, Andrew J.,Chessell, Iain P.,Clayton, Nick M.,Eatherton, Andrew J.,Goldsmith, Paul,Haslam, Carl,Johnson, Matthew R.,Mitchell, William L.,Naylor, Alan,Perboni, Alcide,Slingsby, Brian P.,Wilson, Alex W.
-
supporting information; experimental part
p. 5785 - 5788
(2010/02/28)
-
- COMBINATION OF CB2 LIGAND AND PARACETAMOL
-
Combination of one or more CB2 modulators and paracetamol are useful of treating conditions which are mediated by the activity of CB2 receptors such as an immune disorder, an inflammatory disorder, pain, rheumatoid arthritis, multiple sclerosis, osteoarthritis, and osteoporosis.
- -
-
-
- PYRROLOPYRIDINE DERIVATIVES
-
The present invention relates to novel pyrrolopyridine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
- -
-
-