Modulators of p38 MAP kinase

US6537996B2 · kind B2 · utility

Assignee

• Iconix Pharmaceuticals, Inc. · US

Inventors

• David J. Morgans, Jr. · Los Altos, US
• Silke Thode · Los Gatos, US
• Dongxu Sun · Cupertino, US

Key dates

• Filing date: Feb 23, 2001
• Grant date: Mar 25, 2003
• Expiry date: Feb 23, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D239/28
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds of formula 1 are effective modulators of p38 MAP kinase. wherein R1 is H, lower alkyl, or OR5, where R5 is aryl, heterocyclyl, acyl, N—R6-4-piperidinyl, N—R6-4-piperidinylmethyl, or N—R6-4-pipelidinylethyl, where aryl and heterocyclyl are substituted with 1-3 R6 substituents selected from the group consisting of H, lower alkyl, lower alkenyl, OH, NO2, NH2, halo, trihalomethyl, —CN, SH, SO, SO2, SO3H, —OR, —COR, —COOR, —CONHR, —OCOR, and —NCOR, where R is lower alkyl; R2 is H or lower alkyl; R3 is aryl substituted with 1-3 R6 substituents; R4 is H, lower alkyl, aryl, aralkyl, —OH, —NH2, —NHR, or —OR, where R is lower alkyl or aryl-lower alkyl; and A is —CH— or —N—; and pharmaceutically acceptable salts thereof.