Allosteric p38 kinase inhibitors

Abstract

Two applications claim N,N´-bisaryl urea derivatives as allosteric inhibitors of p38 MAPK and their use as anti-inflammatory agents. The compounds have been designed to stabilise a specific conformation of the kinase and to optimise selectivity by avoiding interactions with the ATP-binding domain of the kinase. They are the first application to describe the applicant’s p38 inhibitor programme, which is close to investigational new drug filing.

Keywords::

• IL-1
• MAPK
• p38
• rheumatoid arthritis
• TNF-α

Patent details

• Title Urea inhibitors of MAP kinases

• Assignee Locus Pharmaceuticals Inc.

• Inventors Michelotti EL, Springman EB, Nguyen D et al.

• Priority date 07/12/04

• Filing date 07/12/05

• Publication date 15/06/06

• Publication no. WO2006062982

• Title Inhibitors of protein kinases

• Assignee Locus Pharmaceuticals Inc

• Inventors Moore WR Jr, Springman E, Michelotti E.

• Priority date 07/12/04

• Filing date 07/12/05

• Publication date 15/06/06

• Publication no. WO2006062984