CRF antagonistic pyrazolo[4,3-b]pyridines

US6613777B1 · kind B1 · utility

Inventors

• Chen Chen · San Diego, US
• Keith Wilcoxen · San Diego, US
• Charles Huang · San Diego, US
• Mustapha Hadduch · San Diego, US
• James R. McCarthy · Dorpsstraat, US

Key dates

• Filing date: Feb 20, 2001
• Grant date: Sep 2, 2003
• Expiry date: Feb 20, 2021

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR5R6, OR6 or SR6; R2 is C1-6alkyl, C1-6alkyloxy, or C1-6alkylthio; R3 is Ar1 or Het1; R4 is hydrogen or C1-6alkyl; R5 is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl, mono- or di(C1-6alkyl)amino-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar2C1-6alkyl, Ar2oxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, tetrahydrofuranylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, or C1-6alkylcarbonylC1-6alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl, morpholinyl, or thiomorpholinyl group, optionally substituted with 1 or 2 substituents each independently selected from C1-6alkyl or C1-6alkyloxyC1-6alkyl; and and Ar1 and Ar2 are each optionally substituted phenyl; and Het1 is optionally substituted pyridinyl; having CRF r…