Azine-carboxamides as anticancer agents

Abstract

Despite disappointing results with the Raf inhibitor ZM 336372, AstraZeneca claims new B-Raf kinase inhibitors with the same m-phenylenediamine core structure. The new bisamides have two distinct linker groups attached. One is a substituted aromatic carboxylic acid group that constitutes the lipophilic part of the molecule, and the other is usually a pyrimidine carboxylic acid. The new molecules are part of a series of m-phenylenediamine bisamides. The compounds are expected to have anticancer activity due to their B-Raf inhibitory activity. B-Raf is mutated in a number of cancers into a constitutively active enzyme.

Keywords::

• bisamide
• B-Raf
• carboxylic acid
• kinase inhibitor
• m-phenylendiamine
• pyrimidine

Patent Details

• Title Azine-carboxamides as anticancer agent

• Assignee AstraZeneca UK Ltd

• Inventors Aquila B, Ioannidis S, Lyne P, Pontz T

• Priority date 01/07/2004

• Filing date 29/06/2005

• Publication date 12/01/2006

• Publication no. WO2006003378

Notes