Patent Number: 6,255,310

Title: Thiophenopyrimidines

Abstract: This invention concerns compounds of formula ##STR1## including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO.sub.2 ; R.sup.1 is NR.sup.4 R.sup.5 or OR.sup.5 ; R.sup.2 is C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or C.sub.1-6 alkylthio; R.sup.3 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkylsulfonyl, C.sub.1-6 alkylsulfoxy or C.sub.1-6 alkylthio; R.sup.4 is hydrogen, C.sub.1-6 alkyl, mono- or di(C.sub.3-6 cycloalkyl)methyl, C.sub.3-6 cycloalkyl, C.sub.3-6 alkenyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkylcarbonyloxyC.sub.1-6 alkyl or C.sub.1-6 alkyloxyC.sub.1-6 alkyl; R.sup.5 is C.sub.1-8 alkyl, mono- or di(C.sub.3-6 cycloalkyl)methyl, Ar.sup.1 CH.sub.2, C.sub.1-6 alkyloxy-C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.3-6 alkenyl, thienylmethyl, furanylmethyl, C.sub.1-6 alkylthioC.sub.1-6 alkyl, morpholinyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylC.sub.1-6 alkyl, C.sub.1-6 alkyl substituted with imidazolyl; or a radical of formula --Alk--O--CO--Ar.sup.1 ; or R.sup.4 and R.sup.5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

Inventors: Webb; Thomas R. (Olivenhain, CA), Chen; Chen (San Diego, CA), McCarthy; James R. (Solana Beach, CA), Moran; Terence J. (San Diego, CA)

Assignee: Neurocrine Biosciences Inc.

International Classification: C07D 495/04 (20060101); C07D 495/00 (20060101); A61K 031/519 (); A61P 005/04 (); A61P 025/18 (); C07D 495/04 ()

Expiration Date: 07/03/2018