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editorial
. 2014 Feb 13;5(4):278–279. doi: 10.1021/ml500047f

Phenyl Carboxamide Analogues as Spleen Tyrosine Kinase (Syk) Inhibitors

Jean-Francois Brazeau , Gerard Rosse †,‡,*
PMCID: PMC4027592  PMID: 24900823

Title: Phenyl Carboxamide Analogues as Spleen Tyrosine Kinase (Syk) Inhibitors
Patent/Patent Application Number: WO 2013052391 Publication date: April 11, 2013
Priority Application: US 2011/61543542 Priority date: October 5, 2011
Inventors: Altman, M. D.; Di Francesco, M. E.; Ellis, J. M.; Knowles, S. L.; Northrup, A. B.
Assignee Company: Merck Sharp & Dohme Corp., USA
Disease Area: Inflammatory, allergic, and autoimmune diseases Biological Target: Syk kinase
Summary: The present application claims a series of phenyl carboxamide compounds that demonstrate activity against Syk kinase protein. Such compounds could potentially be used for the treatment of conditions or disorders associated with inappropriate Syk activity such as inflammatory, allergic, and autoimmune diseases (rheumatoid arthritis, asthma, etc.).
Important Compound Classes: graphic file with name ml-2014-00047f_0001.jpg
Key Structures: graphic file with name ml-2014-00047f_0002.jpg
Recent Review Articles: Efremov D. G.; Laurenti L.. Expert Opin. Invest. Drugs 2011, 20, 623.
Biological Assay: Compound efficacy was evaluated using a HTRF assay for the recombinant human Syk enzyme.
Pharmacological Data: graphic file with name ml-2014-00047f_0006.jpg
Synthesis: 18 compounds were synthesized.

The authors declare no competing financial interest.


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