863550-43-0Relevant academic research and scientific papers
CRF RECEPTOR ANTAGONISTS, THEIR PREPARATIONS, THEIR PHARMACEUTICAL COMPOSITION AND THEIR USES
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Page/Page column 10-11, (2008/06/13)
CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals. CRF receptor antagonists which are labeled with a posit
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility
Chen, Chen,Wilcoxen, Keith M.,Huang, Charles Q.,McCarthy, James R.,Chen, Takung,Grigoriadis, Dimitri E.
, p. 3669 - 3673 (2007/10/03)
In our efforts to identify potent CRF1 antagonists with proper physicochemical properties, a series of 3-phenylpyrazolo[1,5-a]pyrimidines bearing polar groups, such as amino, hydroxyl, methoxy, sulfoxide, were designed and synthesized. Several positions of the core structure were identified, where a polar group was tolerated with slight reduction in receptor binding. NBI 30545 (18n) was found to have good binding affinity and potent antagonistic activity at the human CRF1 receptor. Moreover, this compound had proper lipophilicity (logD=2.78) and good solubility in water (>10mg/mL), and exhibited good plasma and brain exposure when given orally.
Amino substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines
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, (2008/06/13)
Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the
