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editorial
. 2014 Dec 8;6(1):19–20. doi: 10.1021/ml500480n

Novel Azaindazole Sulfonamides Inhibitors of Serum and Glucocorticoid Regulated Kinase

Gerard Rosse 1,2,*
PMCID: PMC4291733  PMID: 25589922

Title: Novel Azaindazole Sulfonamides Inhibitors of Serum and Glucocorticoid Regulated Kinase
Patent/Patent Application Number: WO 2014/140065 A1 Publication date: September 14, 2014
Priority Application: EP 2013–305283 Priority date: March 13, 2013
Inventors: Nazare, M.; Halland, N.; Schmidt, F.; Kleeman, H. W.; Weiss, T.; Saas, J.; Struebing, K.
Assignee Company: Sanofi, France
Disease Area: Degenerative joint disorders, inflammation, and cancer Biological Target: Serum and glucocorticoid regulated kinase (SGK-1)
Summary: The present application claims a series of azaindazole sulfonamides as inhibitors of SGK-1 kinase. The compounds of the invention are potentially useful in the treatment of various disease states such as cardiovascular diseases, inflammation, ostheoarthritis, diabetes, and cancer.
Important Compound Classes: graphic file with name ml-2014-00480n_0001.jpg
Key Structures: graphic file with name ml-2014-00480n_0002.jpg
Biological Assay: The enzymatic activity of the compounds was evaluated in a substrate phosphorylation assay. The cellular activity of the compounds was measured in U2OS cells overexpressing recombinant SGK-1 and GSK2beta.
Pharmacological Data: graphic file with name ml-2014-00480n_0003.jpg
Synthesis: The synthesis of 699 compounds is described.

The authors declare no competing financial interest.


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