929345-60-8Relevant articles and documents
Targeting low-druggability bromodomains: Fragment based screening and inhibitor design against the BAZ2B bromodomain
Ferguson, Fleur M.,Fedorov, Oleg,Chaikuad, Apirat,Philpott, Martin,Muniz, Joao R. C.,Felletar, Ildiko,Von Delft, Frank,Heightman, Tom,Knapp, Stefan,Abell, Chris,Ciulli, Alessio
supporting information, p. 10183 - 10187 (2014/01/17)
Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower pockets. We describe successful tar
γ-Carbolines: A novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration
Cheng, Yun-Xing,Pourashraf, Mehrnaz,Luo, Xuehong,Srivastava, Sanjay,Walpole, Christopher,Salois, Dominic,St-Onge, Stephane,Payza, Kemal,Lessard, Etienne,Yu, Xiao Hong,Tomaszewski, Miros?aw J.
scheme or table, p. 1619 - 1624 (2012/04/04)
An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. γ-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues.
TETRAHYDRO-LH-PYRIDO [3,4 -B] INDOLE DERIVATIVES AS CBL RECEPTOR LIGANDS
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Page/Page column 15-16, (2010/11/30)
The present invention provides tetrahydro-lH-pyrido [3, 4- b] indole derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds act as cannabinoid receptor ligands (CB1) and thus may be used in the treatment of pain, cancer, multiple sclerosis, Parkinson's disease, Huntington's chorea, Alzheimer's disease, anxiety disorders, gastrointestinal disorders and/or cardiovascular disorders.
TETRAHYDRO-LH-PYRIDO[3,4-B] INDOLE DERIVATIVES AS CB1 RECEPTOR LIGANDS
-
Page/Page column 16, (2010/11/30)
The present invention provides tetrahydro-1H-pyrido [3,4- b] indole derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds act as cannabinoid receptor ligands (CB1) and thus may be used in the treatment of pain, cancer, multiple sclerosis, Parkinson's disease, Huntington's chorea, Alzheimer's disease, anxiety disorders, gastrointestinal disorders and/or cardiovascular disorders.