5-Substituted-2-arylpyrazines
AssigneeNeurogen Corporation
InventorsTaeyoung Yoon, Ping Ge, Stephane DeLombaert, Raymond F. Horvath
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Abstract
Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
Claims25
A compound of the Formula:
- 338
- or a pharmaceutically acceptable salt thereof, wherein:
- G is oxygen or NH;
- RX is straight or branched chain C1-8alkyl;
- R1 and R3 are independently selected from hydrogen, C1-4 alkyl, halogen, C1-2 haloalkyl, C1-2haloalkoxy, mono- and di-C1-4alkylamino, C1-4alkoxy, and C1-4 alkylthio;
- R5 is halogen, C1-4alkyl, or C1-4alkoxy;
- R6 is hydrogen, halogen, C1-2alkyl, or C1-2alkoxy;
- R7 is halogen, halogen, cyano, C1-4alkyl, C1-4alkoxy, C1-2 haloalkyl, C1-2haloalkoxy, mono- and di-C1-4alkylamino, mono- and di-(C1-2alkyl)aminoC1-4alkyl, C1-2alkoxyC1-4alkyl, C1-2alkoxycarbonyl, C1-2alkylcarboxaminde, —C(═O)NH2, hydroxyC1-2alkyl, trifluoromethylsulfonyl, 2,2,2-trifluoroethanol, or a 4-7 membered heterocycloalkyl group containing 1 or 2 atoms independently chosen from N, O, and S;
- R8 is hydrogen, halogen, C1-2alkyl, or C1-2alkoxy;
- and
- J is N or CR9 where R9 is hydrogen, halogen or C1-2alkyl.
Dependencies are inferred from the claim text.