885221-08-9Relevant 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.
PYRAZOLO [1,5-ALPHA] PYRIMIDINYL DERIVATIVES USEFUL AS CORTICOTROPIN-RELEASING FACTOR (CRF) RECEPTOR ANTAGONISTS
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Page/Page column 86, (2008/06/13)
CRF receptor antagonists are disclosed which may have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in mammals. The CRF receptor antagonists of this invention have the following structure: (I); and pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof, wherein R1, R2a, R2b, Y, Het, n, o, R6, Ar and R7 are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
