Deazapurine derivatives: a new class of CRF1 specific ligands

Details Deazapurine derivatives: a new class of CRF1 specific ligands Deazapurine derivatives: a new class of CRF1 specific ligands

1995-06-07

1998-09-08

Ford, John M.

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544 55, 544 61, 544 96, 544127, 544280, 544362, 544296, 544 60, 544364, 540553, 540597, 540467, 540481, 540544, 540575, 546113, 546 82, 546 94, 546127, C07D48704

Patent

active

058046852

ABSTRACT:
Disclosed are compounds of the formula ##STR1## wherein Ar represents an aryl or heteroaryl group; and
R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 represent organic or inorganic substituents,
which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.

REFERENCES:
patent: 4605642 (1986-08-01), Rivier et al.
patent: 5063245 (1991-11-01), Abreu et al.
Owens et al., (1991), "Physiology and Pharmacology of Corticotropin-releasing Factor," Pharmacological Reviews, vol. 43, No. 4, pp. 425-473.
Montgomery et al., (1972), "The Use of Enamines in the Synthesis of Heterocycles (1)," J. Het. Chem., vol. 9, pp. 1077-1079.

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