abstract |
The present invention relates to arylpyrazine compounds of formula I, including arylpyrazines, which bind to high CRF1 receptors with high affinity and high selectivity, including human CRF1 receptors. In the compounds of the formula Ar is a substituted phenyl group, an optionally substituted naphthyl group, or a optionally substituted 1-3 ring heterocyclic group in which the rings have from 3 to 8 members and contain from 1 to 3 heteroatoms; R 1 and R 3 are each independently hydrogen, halogen, cyano, nitro or amino, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted mono- or di-alkylamino, optionally substituted alkoxy, optionally substituted alkylthio, optionally substituted alkylsulfinyl, or substituted alkylsulfinyl, or optionally substituted alkylsulfonyl; and R2 is halogen, cyano, nitro or amino, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkylamino, optionally substituted alkoxy, optionally substituted alkylthio, optionally substituted alkylsulfinyl, or optionally substituted alkylsulfonyl; with the proviso that when Ar is a halogen substituted phenyl group, naphthyl group or a halogen substituted naphthyl group, then R3 is other than hydrogen or amino. HE |