(4S)-2'-(((1S)-2,2-difluorocyclopropyl)methoxy)-7'-(5-pyrimidinyl)spiro[1,3-oxazole-4,9'-xanthen]-2-amine | 1215865-30-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: (4S)-2'-(((1S)-2,2-difluorocyclopropyl)methoxy)-7'-(5-pyrimidinyl)spiro[1,3-oxazole-4,9'-xanthen]-2-amine
• 英文别名: (4S)-2'-[[(1S)-2,2-difluorocyclopropyl]methoxy]-7'-pyrimidin-5-ylspiro[5H-1,3-oxazole-4,9'-xanthene]-2-amine
• CAS: 1215865-30-7
• 化学式: C₂₃H₁₈F₂N₄O₃
• 分子量: 436.418
• InChiKey: YPYQVGSLDNKUFZ-NYHFZMIOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  32
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  91.8
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• SPIRO-TRICYCLIC RING COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
  申请人：White Ryan

  公开号：US20100087429A1

  公开（公告）日：2010-04-08

  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 , T 1 , T 2 , W, 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.

  本发明涉及一类新化合物，可用于调节Beta-分泌酶酶活性和治疗Beta-分泌酶介导的疾病，包括阿尔茨海默病（AD）和相关病症。其中，一种实施方式是化合物具有通式I，其中通式I中的A1、A2、A3、A4、A5、A6、T1、T2、W、X、Y和Z的定义在此。本发明还包括这些化合物在制备用于治疗与beta-分泌酶蛋白活性相关的疾病和病症的药物组合物中的使用，包括阿尔茨海默病、认知障碍、认知损伤、精神分裂症和其他与大脑斑块的形成和/或沉积相关和/或由此引起的中枢神经系统病症。本发明还包括通式I的进一步实施方式、中间体和制备通式I化合物的有用过程。
• SPIRO-TETRACYCLIC RING COMPOUNDS AS BETASECRETASE MODULATORS AND METHODS OF USE
  申请人：Amgen Inc.

  公开号：EP2328903B1

  公开（公告）日：2014-03-05
• US8426447B2
  申请人：——

  公开号：US8426447B2

  公开（公告）日：2013-04-23