| Title: | Quinalozinones as Inhibitors of Class I PI3K Kinases | ||
| Patent/Patent Application Number: | WO 2014/128612 A1 | Publication date: | August 8, 2014 |
| Priority Application: | US 2013-61766920 | Priority date: | February 20, 2013 |
| Inventors: | Guibourdenche, C.; Hintermann, S.; Hurth, K.; Jacquier, S.; Kalis, C.; Moebitz, H.; Soldermann, N. | ||
| Assignee Company: | Novartis, Inc. | ||
| Disease Area: | Autoimmune, inflammatory disorders, cancer therapy, and parasitic infections | Biological Target: | Phosphoinositide-3 kinases (PI3K) |
| Summary: | The present application discloses a series of quinalozinones as inhibitors of class I PI3K kinases. The compounds of the invention show a certain level of selectivity for PI3Kδ, PI3Kβ, and PI3Kγ over the PI3Kα isoform. The compounds claimed here are potentially useful in the treatment of a wide range of disorders such as autoimmune, inflammatory and allergic diseases, asthma, COPD, parasitic infections, and cancer. | ||
| Important Compound Classes: |  |
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| Key Structures: |  |
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| Recent Review Articles: | Zhou H.; Huang S.. Adv. Anticancer Agents Med. Chem. 2013, 1, 72–106. | ||
| Biological Assay: | The enzymatic activity of the compounds was evaluated using a TR-FRET inhibition assay. The cellular inhibition activity of the compounds was tested by monitoring PI3K-mediated Akt 1/2 (S473) phosphorylation in rate cells. | ||
| Pharmacological Data: |  |
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| Synthesis: | The synthesis of 182 compounds is described. | ||
The authors declare no competing financial interest.