25391-59-7Relevant academic research and scientific papers
5-Azidoepibatidine: An Exceptionally Potent Photoaffinity Ligand for Neuronal α4β2 and α7 Nicotinic Acetylcholine Receptors
Zhang, Nanjing,Tomizawa, Motohiro,Casida, John E.
, p. 525 - 528 (2003)
Racemic 5-azidoepibatidine [(+/-)-1] was synthesized via 5-aminoepibatidine as a candidate photoaffinity ligand with exceptionally high affinity at the mammalian neuronal nicotinic receptors (Ki values of 0.027 nM for α4β2 and 9.7 nM for α7) and excellent photoreactivity.
ANTI-FIBROTIC PYRIDINONES
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Paragraph 0413, (2015/11/02)
This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.
ANTI-FIBROTIC PYRIDINONES
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Paragraph 0656-0657, (2014/04/17)
Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
Identification of benzoxazole analogs as novel, S1P3 sparing S1P1 agonists
Deng, Guanghui,Meng, Qinghua,Liu, Qian,Xu, Xuesong,Xu, Qiongfeng,Ren, Feng,Guo, Taylor B.,Lu, Hongtao,Xiang, Jia-Ning,Elliott, John D.,Lin, Xichen
scheme or table, p. 3973 - 3977 (2012/07/03)
A novel series of benzoxazole-derived S1P1 agonists were designed based on scaffold hopping molecular design strategy combined with computational approaches. Extensive SAR studies led to the discovery of compound 17d as a selective S1P1 agonist (over S1P3) with high CNS penetration and favorable DMPK properties. 17d also demonstrated in vivo pharmacological efficacy to reduce blood lymphocyte in mice after oral administration.
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
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)
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
COMBINATION OF CB2 LIGAND AND PARACETAMOL
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Page/Page column 141, (2008/12/04)
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
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Page/Page column 31, (2008/06/13)
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.
