Title:The 2010 Patent Landscape for Spleen Tyrosine Kinase Inhibitors+
VOLUME: 6 ISSUE: 2
Author(s):Alessandro F. Moretto, Christoph Dehnhardt, Neelu Kaila, Nikolaos Papaioannou and Atli Thorarensen
Affiliation:Inflammation and Immunology Medicinal Chemistry Pfizer, 200 Cambridgepark Drive, Cambridge MA 02140 USA.
Keywords:Anti-inflammatory pathway, non-receptor tyrosine kinase, rheumatoid arthritis, SYK, SYK inhibitor, SYK-patents
Abstract:Discovery of small molecular inhibitors for treatment of rheumatoid arthritis is a major ongoing effort within
the pharmaceutical industry. Spleen tyrosine kinase (SYK) is one of leading small molecular targets with regard to clinical
development primarlly due to efforts by Rigel and Portola. In this review, we provide a comprehensive overview of the
SYK patent landscape. The patent literature we evaluated relates to any organization that has filed applications that imply
that SYK is the intended target. The interest in SYK was initiated in the early 2000’s with many organizations, including
several large pharmaceutical companies, and has been active for years. In general, the structural theme of most of the
compounds in these applications is a traditional ATP competitive inhibitor with each organization having a different hinge
binding element. In general, the attachment to the hinge is an aryl amine that is decorated with a solubilizing group. The
other substituents are broadly variable across the numerous companies indicating that SYK has significant flexibility in its
interactions in that portion of the kinase. This overview of the SYK patent literature and the learnings of the inhibitors’
substitution patterns would be an important reference for anyone working in this area.
