| Title: | Triazolo[4,5-d]pyrimidine Derivatives as Inhibitors of GCN2 | ||
| Patent/Patent Application Number: | WO 2013110309 | Publication date: | August 1, 2013 |
| Priority Application: | EP 2012-558 | Priority date: | January 28, 2012 |
| Inventors: | Dorsch, D.; Hoelzemann, G.; Schiemann, K.; Wagener, A. | ||
| Assignee Company: | Merck GMBH, Germany | ||
| Disease Area: | Cancer | Biological Target: | GCN2 protein kinase |
| Summary: | The present application claims a series of triazolopyrimidine analogues that inhibit the stress response of general control nonderepressible 2 kinase (GCN2) and that may be useful as chemotherapeutic drugs for the treatment of cancer. | ||
| Important Compound Classes: |  |
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| Key Structures: |  |
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| 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.; Koumenis C.. EMBO J. 2010, 29, 2082. | ||
| Biological Assay: | The enzyme assay was developed using serine kinase GCN2, and the cellular assay was developed using the primary antibody (antiphospho-elF2alpha) | ||
| Pharmacological Data: |  |
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| Synthesis: (optional) | 157 compounds were prepared. | ||
The authors declare no competing financial interest.