(S)-7-bromo-3-chloro-5',6'-dihydrospiro[chromeno[2,3-c]pyridine-5,4'-[1,3]thiazin]-2'-amine

• 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: (S)-7-bromo-3-chloro-5',6'-dihydrospiro[chromeno[2,3-c]pyridine-5,4'-[1,3]thiazin]-2'-amine
• 英文别名: (4S)-7'-bromo-3'-chlorospiro[5,6-dihydro-1,3-thiazine-4,5'-chromeno[2,3-c]pyridine]-2-amine
• 化学式: C₁₅H₁₁BrClN₃OS
• 分子量: 396.7
• InChiKey: VDXHDNKFTCHEGL-HNNXBMFYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  22
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  85.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (S)-7-bromo-3-chloro-5',6'-dihydrospiro[chromeno[2,3-c]pyridine-5,4'-[1,3]thiazin]-2'-amine 、 、 叠氮化钠 、 、 乙醇 、 叠氮阴离子 、 在 碘化亚铜 氮气 、 乙酸乙酯 、 Brine 、 magnesium sulfate 、 crude material 作用下， 以 水 为溶剂， 反应 5.5h， 以to provide crude material of (S)-7-azido-3-chloro-5′,6′-dihydrospiro[chromeno[2,3-c]pyridine-5,4′-[1,3]thiazin]-2′-amine的产率得到(S)-7-azido-3-chloro-5',6'-dihydrospiro[chromeno[2,3-c]pyridine-5,4'-[1,3]thiazin]-2'-amine
  参考文献：
  名称：

  AMINO-OXAZINE AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE

  摘要：

  本发明涉及一种新型化合物类，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）和相关疾病。在一种实施例中，该化合物具有一般的I式，其中I式的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制备药物组合物，用于治疗与Beta-分泌酶蛋白活性相关的障碍和疾病，例如阿尔茨海默病，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/或引起的中枢神经系统疾病。本发明还包括I式的进一步实施例、中间体和制备I式化合物的有用过程。

  公开号：

  US20150307521A1

文献信息

• US9725469B2
  申请人：——

  公开号：US9725469B2

  公开（公告）日：2017-08-08
• [EN] AMINO-OXAZINE AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE<br/>[FR] COMPOSÉS D'AMINO-OXAZINE ET D'AMINO-DIHYDROTHIAZINE JOUANT LE RÔLE DE MODULATEURS DE BÊTA-SÉCRÉTASE ET PROCÉDÉS D'UTILISATION
  申请人：AMGEN INC

  公开号：WO2014078314A1

  公开（公告）日：2014-05-22

  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 A1, A2, A3, A4, A5, A6, L, R2, R7, 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.
• AMINO-OXAZINE AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
  申请人：AMGEN INC.

  公开号：US20150307521A1

  公开（公告）日：2015-10-29

  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，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）和相关疾病。在一种实施例中，该化合物具有一般的I式，其中I式的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制备药物组合物，用于治疗与Beta-分泌酶蛋白活性相关的障碍和疾病，例如阿尔茨海默病，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/或引起的中枢神经系统疾病。本发明还包括I式的进一步实施例、中间体和制备I式化合物的有用过程。