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ACS Medicinal Chemistry Letters
 
ACS Med Chem Lett. 2016 December 8; 7(12): 1022–1023.
Published online 2016 November 10. doi:  10.1021/acsmedchemlett.6b00435
PMCID: PMC5151140

Pyridyl Isonicotinamide Inhibitors of RAF Kinase

Title:Pyridyl Isonicotinamide Inhibitors of RAF Kinase
Patent/Patent Application Number:WO 2016/038581 AlPublication date:March 17, 2016
Priority Application:US 2014–62049469Priority date:September 12, 2014
Inventors:Burger, M. T.; Ramurthy, S.; Taft, B. R.
Assignee Company:Novartis AG, Switzerland
Disease Area:CancerBiological Target:RAF Kinase
Summary:The present application claims a series of pyridyl isonicotinamide derivatives as inhibitors of the RAF kinase. The compounds described here are potentially useful in the treatment of ovarian cancer, nonsmall cell lung cancer, and cancers driven by RAF mutations
Important Compound Classes:
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Key Structures:
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Recent Review Articles:1. Garuti L.; Roberti M.; Bottegoni G.; Ferraro M.Diaryl Urea: A Privileged Structure in Anticancer Agents. Curr. Med. Chem. 2016, 23 (15), 1528–1548. [PubMed]
Biological Assay:The activity of the compounds was measured in an Alpha Screen assay using a truncated C-Raf protein and MEKl with an inactivating K97R ATP binding site mutation as a substrate
Pharmacological Data:
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Synthesis:The synthesis and biochemical activity of 18 compounds are described.

Notes

The author declares no competing financial interest.


Articles from ACS Medicinal Chemistry Letters are provided here courtesy of American Chemical Society