| Title: | Dihydrooxazines As Inhibitors of BACE-1 or BACE-2 | ||
| Patent/Patent Application Number: | WO 2013/027188 A1 | Publication Date: | February 28, 2013 |
| Priority Application: | Priority Date: | August 23, 2012 | |
| Inventors: | Lueoend, R. M.; Machauer, R.; Rueeger, H.; Veenstra, S. J. | ||
| Assignee Company: | Novartis AG, Basel, Switzerland | ||
| Disease Area: | Alzheimer’s disease, mild cognitive impairment, insulin intolerance, type 2 diabetes, obesity | Biological Target: | BACE-1, BACE-2 |
| Summary: | The patent application claims dihydrooxazine derivatives as inhibitors for the treatment of Alzheimer’s disease or diabetes. | ||
| Important Compound Classes: |  |
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| Key Structures: |  |
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| Biological Assays: | Thirty-seven compounds described in this invention were evaluated for their inhibition properties against human BACE-1, BACE-2, and cellular release of amyloid peptide 1–40. Seven compounds were tested in vivo for their ability to lower Abeta in rat brain and CSF. | ||
| Pharmacological Data: | Inhibition of BACE-1, BACE-2, or cellular
release of amyloid peptide 1–40. 
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| Synthesis: | Synthesis of 37 examples is described. | ||
The author declares no competing financial interest.
Author Present Address
† Adjunct Associate Professor, Department of Pharmacology and Physiology, Drexel University, College of Medicine, New College Building, 245 N. 15th Street, Philadelphia, PA 19102.