The 2-oxindole chemotype and patent activity inspired by the SU5416 franchise

Abstract

Indol-2-ones or 2-oxoindole-based tyrosine kinase inhibitors (TKIs) were originally identified in the late 1980s by researchers in Japan and Italy. Interest in this series of TKIs increased significantly following the disclosure of SU5416, a clinical candidate from Sugen for the treatment of cancer. During the clinical development of SU5416, there was a significant increase in patent filings related to TKIs containing 2-oxindole groups, both inside and outside of Sugen. This review will look at the patent activity inspired by the 2-oxoindole kinase inhibitors from the late 1980s to applications published through April of 2003.

• indolones
• kinase inhibitors
• oxindole
• semaxanib
• SU5416
• SU6668
• SU11248