CRF antagonistic thiophenopyridines

US6211195A · kind A · utility

Assignees

• Neurocrine Biosciences, Inc. · US
• Janssen Pharmaceutica NA · BE

Inventors

• Thomas R. Webb · Olivenhain, US
• James R. McCarthy · Dorpsstraat, US

Key dates

• Filing date: Oct 19, 1999
• Grant date: Apr 3, 2001
• Expiry date: Oct 19, 2019

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention concerns compounds of formula ##STR1## including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S or SO.sub.2 ; R.sup.1 is C.sub.1-6 alkyl, NR.sup.5 R.sup.6, OR.sup.6 or SR.sup.6 ; R.sup.2 is C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or C.sub.1-6 alkylthio; R.sup.3 is Ar.sup.1 or Het.sup.1 ; R.sup.4 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.5 is hydrogen, C.sub.1-8 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.6 is C.sub.1-8 alkyl, mono- or di(C.sub.3-6 cycloalkyl)methyl, Ar.sup.2 CH.sub.2, C.sub.1-6 alkyloxyC.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, 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; or R.sup.5 and R.sup.6 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group…