发明申请
US20130109683A1 5,6-DIHYDRO-2H-[1,4]OXAZIN-3-YL-AMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
审中-公开
作为β-分泌酶(BACE)的抑制剂有用的5,6-二氢-2H- [1,4]氧杂-3-氨基胺衍生物
- 专利标题: 5,6-DIHYDRO-2H-[1,4]OXAZIN-3-YL-AMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
- 专利标题(中): 作为β-分泌酶(BACE)的抑制剂有用的5,6-二氢-2H- [1,4]氧杂-3-氨基胺衍生物
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申请号: US13703199申请日: 2011-06-08
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公开(公告)号: US20130109683A1公开(公告)日: 2013-05-02
- 发明人: Andrés Avelino Trabanco-Suárez , Frederik Jan Rita Rombouts , Gary John Tresadern , Michiel Luc Maria Van Gool , Gregor James MacDonald , Carolina Martinez Lamenca , Henricus Jacobus Maria Gijsen
- 申请人: Andrés Avelino Trabanco-Suárez , Frederik Jan Rita Rombouts , Gary John Tresadern , Michiel Luc Maria Van Gool , Gregor James MacDonald , Carolina Martinez Lamenca , Henricus Jacobus Maria Gijsen
- 申请人地址: US NJ New Brunswick
- 专利权人: JANSSEN PHARMACEUTICA NV
- 当前专利权人: JANSSEN PHARMACEUTICA NV
- 当前专利权人地址: US NJ New Brunswick
- 优先权: EP10165335.0 20100609; EP11152314.8 20110127; EP11157765.6 20110310; EP11164999.2 20110505
- 国际申请: PCT/EP2011/059441 WO 20110608
- 主分类号: C07D413/10
- IPC分类号: C07D413/10 ; C07D265/30
摘要:
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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