6-chlorofuro[3,2-b]pyridin-3(2H)-one | 1400683-14-8

• 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: 6-chlorofuro[3,2-b]pyridin-3(2H)-one
• 英文别名: 6-chloro-furo[3,2-b]pyridin-3-one；6-chlorofuro[3,2-b]pyridin-3-one
• CAS: 1400683-14-8
• 化学式: C₇H₄ClNO₂
• 分子量: 169.567
• InChiKey: NJMJNAUPSVMWIC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  39.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  ethyl 6-chloro-3-hydroxyfuro[3,2-b]pyridine-2-carboxylate 在 盐酸 、 水 、 碳酸氢钠 作用下， 以 水 为溶剂， 反应 3.0h， 以73.1%的产率得到6-chlorofuro[3,2-b]pyridin-3(2H)-one
  参考文献：
  名称：

  [EN] 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS
  [FR] 1,4-OXAZÉPINES UTILISABLES EN TANT QU'INHIBITEURS DE BACE1 ET/OU BACE2

  摘要：

  本发明涉及具有BACE1和/或BACE2抑制活性的式I的1,4-噁唑啉，它们的制备，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗例如阿尔茨海默病和2型糖尿病方面是有用的。

  公开号：

  WO2012126791A1

文献信息

• [EN] PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE<br/>[FR] COMPOSÉS À BASE DE 1,3-OXAZIN-2-AMINE FUSIONNÉE AVEC DU CYCLOPROPYLE PERFLUORÉ UTILISABLES EN TANT QU'INHIBITEURS DE LA BÊTA-SÉCRÉTASE ET LEURS PROCÉDÉS D'UTILISATION
  申请人：AMGEN INC

  公开号：WO2014138484A1

  公开（公告）日：2014-09-12

  PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE ABSTRACT OF THE DISCLOSURE The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: INSERT STRUCTURE HERE} I wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

  本发明提供了一类新的化合物，用于调节β-分泌酶（BACE）活性。这些化合物具有一般的化学式I：在此插入结构} I，其中变量A4、A5、A6、A8，以及化学式I中的每个Ra、Rb、R1、R2、R3和R7，在本文中分别定义。该发明还提供了包含这些化合物的药物组合物，以及用于治疗与A-beta斑块形成和沉积相关的疾病和/或症状的化合物和组合物的用途，这些疾病和症状是由BACE的生物活性引起的。这种由BACE介导的疾病包括阿尔茨海默病、认知缺陷、认知障碍、精神分裂症和其他中枢神经系统疾病。该发明还提供了化学式II和III的化合物，以及其亚式化合物、中间体和制备本发明化合物的方法。
• 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS
  申请人：Gabellieri Emanuele

  公开号：US20120238548A1

  公开（公告）日：2012-09-20

  The present invention relates to 1,4-Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明涉及具有BACE1和/或BACE2抑制活性的式I的1,4-噁唑啉，其制备方法，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗例如阿尔茨海默病和2型糖尿病方面是有用的。
• Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
  申请人：AMGEN INC.

  公开号：US09085576B2

  公开（公告）日：2015-07-21

  The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

  本发明提供了一种新的化合物类别，用于调节β-分泌酶酶（BACE）活性。该化合物具有一般式I：其中变量A4、A5、A6、A8，以及式I中的每个Ra、Rb、R1、R2、R3和R7，在此独立地定义。该发明还提供了包含该化合物的药物组合物，并且该化合物和组合物的用途包括治疗与A-beta斑块形成和沉积相关的疾病和/或症状，这是由BACE的生物活性引起的。这种BACE介导的疾病包括阿尔茨海默病、认知缺陷、认知障碍、精神分裂症和其他中枢神经系统疾病。该发明还提供了式II和式III的化合物，以及其子式实施例，中间体和制备该发明化合物的方法。
• 1,4-oxazepines as BACE1 and/or BACE2 inhibitors
  申请人：Gabellieri Emanuele

  公开号：US08748418B2

  公开（公告）日：2014-06-10

  The present invention relates to 1,4-Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明涉及具有BACE1和/或BACE2抑制活性的1,4-噁唑烷的公式I，它们的制造，包含它们的制药组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗例如阿尔茨海默病和2型糖尿病方面有用。
• PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
  申请人：AMGEN INC.

  公开号：US20150252011A1

  公开（公告）日：2015-09-10

  The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A 4 , A 5 , A 6 , A 8 , each of R a , R b , R 1 , R 2 , R 3 and R 7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

  本发明提供了一类新的化合物，可用于调节β-分泌酶(BACE)的活性。这些化合物具有通式I： 其中，变量A4、A5、A6、A8，以及通式I中的每个Ra、Rb、R1、R2、R3和R7，在此独立地定义。本发明还提供了包含这些化合物的药物组合物，并将这些化合物和组合物用于治疗与A-beta斑块形成和沉积有关的疾病和/或症状，这是由BACE的生物活性导致的。这样的BACE介导的疾病包括阿尔茨海默病、认知缺陷、认知障碍、精神分裂症和其他中枢神经系统疾病。本发明还提供了通式II和III的化合物，以及它们的亚式化合物、中间体和制备本发明化合物的方法。