N-((5S)-2'-amino-1-fluoro-3-(5-fluoro-3-pyridinyl)-5',6'-dihydrospiro[chromeno[2,3-c]pyridine-5,4'-[1,3]thiazin]-7-yl)-5-methoxy-2-pyrazinecarboxamide | 1428633-38-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡喃吡啶类
• 英文名称: N-((5S)-2'-amino-1-fluoro-3-(5-fluoro-3-pyridinyl)-5',6'-dihydrospiro[chromeno[2,3-c]pyridine-5,4'-[1,3]thiazin]-7-yl)-5-methoxy-2-pyrazinecarboxamide
• 英文别名: N-[(4S)-2-amino-1'-fluoro-3'-(5-fluoropyridin-3-yl)spiro[5,6-dihydro-1,3-thiazine-4,5'-chromeno[2,3-c]pyridine]-7'-yl]-5-methoxypyrazine-2-carboxamide
• CAS: 1428633-38-8
• 化学式: C₂₆H₁₉F₂N₇O₃S
• 分子量: 547.545
• InChiKey: PEZGSBQHDVWHLU-SANMLTNESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  39
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  163
• 氢给体数：
  2
• 氢受体数：
  11

文献信息

• Amino-Oxazine and Amino-Dihydrothiazine Compounds as Beta-Secretase Modulators and Methods of Use
  申请人：AMGEN INC

  公开号：US20140296226A1

  公开（公告）日：2014-10-02

  The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , L, R 2 , R 7 , X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.

  本发明涉及一种新型化合物类别，用于调节β-分泌酶酶活性和治疗β-分泌酶介导的疾病，包括阿尔茨海默病（AD）和相关疾病。在一个实施例中，该化合物具有一般式I，其中式I中的A1、A2、A3、A4、A5、A6、L、R2、R7、X、Y和Z在此定义。本发明还包括将这些化合物用于治疗与β-分泌酶蛋白活性相关的障碍和疾病的药物组合物，包括阿尔茨海默病、认知缺陷、认知障碍、精神分裂症和其他与大脑斑块形成和/或沉积相关和/或由此引起的中枢神经系统疾病。本发明还包括式I的进一步实施例、中间体和用于制备式I化合物的过程。
• US9296759B2
  申请人：——

  公开号：US9296759B2

  公开（公告）日：2016-03-29
• US9777019B2
  申请人：——

  公开号：US9777019B2

  公开（公告）日：2017-10-03