| Title: | Pyrrolopyridines-quinazolines Inhibitors of PKR-Like ER Kinase | ||
| Patent/Patent Application Number: | WO 2014/161808 A1 | Publication date: | October 9, 2014 |
| Priority Application: | EP 2013–162362 | Priority date: | April 4, 2013 |
| Inventors: | Stansfield, I.; Ligny, Y. A. E.; Amblard, N. C., I.; Versele, M. L. A. | ||
| Assignee Company: | Janssen Pharmaceutica NV, Belgium | ||
| Disease Area: | Cancer, diabetes, and neurodegenerative diseases | Biological Target: | PKR-like ER kinase (PERK) |
| Summary: | The present application claims pyrrolopyridines-quinazolines analogues as inhibitors of PERK kinase. The compounds of the invention are potentially useful in the treatment of a wide range of disorders such as cancer, diabetes, ocular disease, stroke, inflammation, viral infections, and neurodegenerative diseases. | ||
| Important Compound Classes: |  |
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| Definitions: | A = CH or N | ||
| Key Structures: |  |
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| Biological Assay: | The enzymatic activity of the compounds was evaluated in a PERK kinase assay using LanthaScreen technology and in a cell-based TR-FRET assay in HEK293 cells. | ||
| Pharmacological Data: |  |
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| Synthesis: | The synthesis of 153 compounds is described. | ||
The authors declare no competing financial interest.