Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists
摘要:
Low nanomolar corticotropin releasing factor type-1 (CRF1) receptor antagonists containing unique indanylamines were identified from the heteroatom-linked pyrazine chemotype. The most potent indanylpyrazine had a K-i = 11 +/- 1 nM. The oxygen-linked pyrazinyl derivatives were prepared through a copper-catalyzed coupling of a pyridinone to a bromo- or iodopyrazine. (C) 2007 Elsevier Ltd. All rights reserved.
The invention is directed to compounds of Formula I, described herein, as well as pharmaceutically acceptable salts thereof, which act as CRF
1
antagonists and are useful in the treatment of disorders and diseases associated with CRF
1
receptors, including CNS-related disorders and diseases.