PATENT HIGHLIGHT pubs.acs.org/acsmedchemlett
Triazolo[4,5-d]pyrimidine Derivatives as Inhibitors of GCN2 Jean-Francois Brazeau† and 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 Triazolo[4,5-d]pyrimidine Derivatives as Inhibitors of GCN2
Title:
Patent/Patent Application Number: WO 2013110309
Publication date:
August 1, 2013
Priority date:
January 28, 2012
Priority Application:
EP 2012-558
Inventors:
Dorsch, D.; Hoelzemann, G.; Schiemann, K.; Wagener, A.
Assignee Company: Disease Area:
Merck GMBH, Germany Cancer
Summary:
The present application claims a series of triazolopyrimidine analogues that inhibit the stress response of general control
Biological Target:
GCN2 protein kinase
nonderepressible 2 kinase (GCN2) and that may be useful as chemotherapeutic drugs for the treatment of cancer. Important Compound Classes:
Key Structures:
Recent Review Articles:
Ye, J.; Kumanova, M.; Hart, L. S.; Sloane, K.; Zhang, H.; De Panis, D. N.; Bobrovnikova-Marjon, E.; Diehl, J. A.; Ron, D.;
Biological Assay:
The enzyme assay was developed using serine kinase GCN2, and the cellular assay was developed using the primary antibody
Koumenis, C. EMBO J. 2010, 29, 2082. (antiphospho-elF2alpha)
Received:
r XXXX American Chemical Society
A
January 31, 2014
dx.doi.org/10.1021/ml500052f | ACS Med. Chem. Lett. XXXX, XXX, 000–000
ACS Medicinal Chemistry Letters
PATENT HIGHLIGHT
Pharmacological Data:
Synthesis: (optional)
157 compounds were prepared.
’ AUTHOR INFORMATION Corresponding Author
*E-mail:
[email protected]. Notes
The authors declare no competing financial interest.
B
dx.doi.org/10.1021/ml500052f |ACS Med. Chem. Lett. XXXX, XXX, 000–000
