862695-75-8Relevant academic research and scientific papers
Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors
Scott, James S.,Gill, Adrian L.,Godfrey, Linda,Groombridge, Sam D.,Rees, Amanda,Revill, John,Schofield, Paul,S?rme, Pernilla,Stocker, Andrew,Swales, John G.,Whittamore, Paul R.O.
, p. 6756 - 6761 (2013/01/14)
11β-HSD1 is increasingly seen as an attractive target for the treatment of type II diabetes and other elements of the metabolic syndrome. In this program of work we describe how a series of neutral 2-thioalkyl-pyridine 11β-HSD1 inhibitors were optimized in terms of their pharmacokinetic properties to give compounds with excellent bioavailability in both rat and dog through a core change to pyrimidine. A potential reactive metabolite issue with 4-thioalkyl-pyrimidines was circumvented by a switch from sulfur to carbon substitution.
PYRIDINE DERIVATIVES AS CONNABINOID RECEPTOR MODULATORS
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Page/Page column 25, (2008/06/13)
The present invention relates to novel pyridine derivatives such as compounds of the formula (I): and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of t
PYRIDINE DERIVATIVES AND THEIR USE AS CB2 RECEPTOR MODULATORS
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Page/Page column 35, (2010/02/13)
The present invention relates to novel pyridine derivatives such as compounds of the formula (I) and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of th
