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Macrocyclic Inhibitors of ERK2 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: Patent/Patent Application Number: Priority Application: Inventors: Assignee Company: Disease Area: Summary: Important Compound Classes:
Macrocyclic Inhibitors of ERK2 Kinase WO 2016/100051 Al Publication date: June 23, 2016 WO 2014-CN93858 Priority date: December 15, 2014 Siliphaivanh, P.; Sloman, D. L.; Witter, D.; Mansoor, U. F.; Kozlowski, J.; Liu, Z.; Fu, J.; Wan, Z.; Liu, W.; Qian, Y.; Huang, X. Merck Sharp and Dohme Corp., USA; MSD R&D (China) Co., Ltd. Cancer Biological Target: ERK2 Kinase The present application claims a series of pyrazolopyridine macrocyclic inhibitors of ERK2 kinase as potential treatment of cancer.
Key Structures:
Recent Review Articles: Biological Assay:
1. Yu, Z.; Ye, S.; Hu, G.; Lv, M.; Tu, Z.; Zhou, K.; Li, Q. Future Medicinal Chemistry 2015, 7 (3), 269−289. The inhibitory activity of the compounds for ERK2 kinase was determined in an IMAP-FP assay.
Received: November 2, 2016
© XXXX American Chemical Society
A
DOI: 10.1021/acsmedchemlett.6b00434 ACS Med. Chem. Lett. XXXX, XXX, XXX−XXX
ACS Medicinal Chemistry Letters
Patent Highlight
Pharmacological Data:
Synthesis:
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The synthesis and biochemical activity of fifty-eight compounds are described.
AUTHOR INFORMATION
Corresponding Author
*E-mail:
[email protected]. Notes
The author declares no competing financial interest.
B
DOI: 10.1021/acsmedchemlett.6b00434 ACS Med. Chem. Lett. XXXX, XXX, XXX−XXX
