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Pyridyl Isonicotinamide Inhibitors of RAF Kinase Gerard Rosse* Structure Guided Chemistry, Dart Neuroscience LLC, 7473 Lusk Boulevard, San Diego, California 92121, United States Adjunct Associate Professor, Department of Pharmacology and Physiology, College of Medicine, Drexel University, New College Building, 245 North 15th Street, Philadelphia, Pennsylvania 19102, United States Title:
Pyridyl Isonicotinamide Inhibitors of RAF Kinase
Patent/Patent Application Number:
WO 2016/038581 Al
Publication date:
March 17, 2016
Priority Application:
US 2014−62049469
Priority date:
September 12, 2014
Inventors:
Burger, M. T.; Ramurthy, S.; Taft, B. R.
Assignee Company:
Novartis AG, Switzerland
Disease Area:
Cancer
Biological 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:
Key Structures:
Recent Review Articles:
Garuti, L.; Roberti, M.; Bottegoni, G.; Ferraro, M. Diaryl Urea: A Privileged Structure in Anticancer Agents. Curr. Med. Chem. 2016, 23 (15), 1528−1548.
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
Received: November 2, 2016
© XXXX American Chemical Society
A
DOI: 10.1021/acsmedchemlett.6b00435 ACS Med. Chem. Lett. XXXX, XXX, XXX−XXX
ACS Medicinal Chemistry Letters
Patent Highlight
Pharmacological Data:
Synthesis:
■
The synthesis and biochemical activity of 18 compounds are described.
AUTHOR INFORMATION
Corresponding Author
*E-mail:
[email protected]. Notes
The author declares no competing financial interest.
B
DOI: 10.1021/acsmedchemlett.6b00435 ACS Med. Chem. Lett. XXXX, XXX, XXX−XXX
