Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists

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 Ki = 11 ± 1 nM. The oxygen-linked pyrazinyl derivatives were prepared through a copper-catalyzed coupling of a pyridinone to a bromo- or iodopyrazine.