885220-98-4Relevant academic research and scientific papers
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties
Tellew, John E.,Lanier, Marion,Moorjani, Manisha,Lin, Emily,Luo, Zhiyong,Slee, Deborah H.,Zhang, Xiaohu,Hoare, Sam R.J.,Grigoriadis, Dimitri E.,Denis, Yves St.,Fabio, Romano Di,Modugno, Enza Di,Saunders, John,Williams, John P.
scheme or table, p. 7259 - 7264 (2011/02/22)
Antagonists of the corticotropin-releasing factor (CRF) neuropeptide may prove effective in treating stress and anxiety related disorders. In an effort to identify antagonists with improved physico-chemical properties a new series of CRF1 antagonists were designed to substitute the propyl groups at the C7 position of the pyrazolo[1,5-a]pyrimidine core of 1 with heterocycles. Compound (S)-8d was identified as a high affinity ligand with a pKi value of 8.2 and a functional CRF1 antagonist with pIC50 value of 7.0 in the in vitro CRF ACTH production assay.
NOVEL TRIAZOLOPYRIDINE COMPOUNDS FOR THE TREATMENT OF INFLAMMATION
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Page/Page column 98-99, (2008/06/13)
This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula (I): Wherein R1, R2, R3, R4, and R5are as defined in this specification. This invention also is directed to compositions of such triazolopyridines (particularly pharmaceutical compositions), intermediates for the syntheses of such triazolopyridines, methods for making such triazolopyridines, and methods for treating (including preventing) conditions (typically pathological conditions) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.
