- Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360
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Starting from lead compound 4, the 1,4-oxazine headgroup was optimized to improve potency and brain penetration. Focusing at the 6-position of the 5-amino-1,4-oxazine, the insertion of a Me and a CF3 group delivered an excellent pharmacological profile wi
- Rueeger, Heinrich,Lueoend, Rainer,Machauer, Rainer,Veenstra, Siem J.,Holzer, Philipp,Hurth, Konstanze,Voegtle, Markus,Frederiksen, Mathias,Rondeau, Jean-Michel,Tintelnot-Blomley, Marina,Jacobson, Laura H.,Staufenbiel, Matthias,Laue, Grit,Neumann, Ulf
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p. 4677 - 4696
(2021/05/06)
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- NOVEL OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
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- Oxazine derivatives and their use in the treatment of neurological disorders
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The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
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- Oxazine Derivatives and their Use in the Treatment of Neurological Disorders
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The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
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- 5,6-DIHYDRO-2H-[1,4]OXAZIN-3-YL-AMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
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The present invention relates to novel 5,6-dihydro-2H-[1,4]oxazin-3-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta- amyloid.
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- OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS
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The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
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Page/Page column 27
(2011/02/18)
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