2-chloropyrido[3,2-d]pyrimidin-4-amine | 874493-60-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 2-chloropyrido[3,2-d]pyrimidin-4-amine
• 英文别名: 2-chloro-pyrido[3,2-d]pyrimidin-4-ylamine；2-Chlor-pyrido[3,2-d]pyrimidin-4-ylamin；2-Chloro-pyrido[3,2-d]pyrimidin-4-amine
• CAS: 874493-60-4
• 化学式: C₇H₅ClN₄
• 分子量: 180.596
• InChiKey: OEEWKKRJLNRBQV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  64.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-chloropyrido[3,2-d]pyrimidin-4-amine 在 盐酸 、 N,N-二异丙基乙胺 作用下， 以 1,4-二氧六环 、 正丁醇 为溶剂， 反应 21.0h， 生成 (3S)-4-(4-aminopyrido[3,2-d]pyrimidin-2-yl)-N-(4-methoxy-2-methylphenyl)-3-methylpiperazine-1-carboxamide
  参考文献：
  名称：

  [EN] FUSED PYRIDINE DERIVATIVES AS KINASE INHIBITORS
  [FR] DÉRIVÉS DE PYRIDINE CONDENSÉS EN TANT QU'INHIBITEURS DE KINASES

  摘要：

  一系列经取代的嘧啶并[3,2-d]嘧啶和1,5-萘啶衍生物的化学式(I)，如本文所定义，是选择性抑制磷脂酰肌醇-4-激酶IIIβ（PI4KIIIβ）活性的药物，在治疗和/或预防各种人类疾病方面具有益处，包括炎症、自身免疫和肿瘤性疾病；病毒性疾病和疟疾；以及器官和细胞移植排斥反应。

  公开号：

  WO2017055306A1
• 作为产物：
  描述：

  2,4-二氯吡啶并[3,2-d]嘧啶 在 氨 作用下， 生成 2-chloropyrido[3,2-d]pyrimidin-4-amine
  参考文献：
  名称：

  Oakes et al., Journal of the Chemical Society, 1956, p. 1045,1053

  摘要：

  DOI：

文献信息

• Cyclopropyl Fused Thiazin-2-Amine Compounds as Beta-Secretase Inhibitors and Methods of Use
  申请人：AMGEN INC.

  公开号：US20160046618A1

  公开（公告）日：2016-02-18

  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 , and 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）活性。该化合物具有通式I：其中变量A4、A5、A6、A8和通式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该化合物的药物组合物，并且提供了使用该化合物和组合物治疗与A-beta斑块形成和沉积相关的疾病和/或病况，这是由BACE的生物活性引起的。这种BACE介导的疾病包括，例如，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，以及其子式实施例、中间体和制备本发明化合物的方法。
• TOLL-LIKE RECEPTOR MODULATING 4,6-DIAMINO-PYRIDO[3,2-D]PYRIMIDINE COMPOUNDS
  申请人：Gilead Sciences, Inc.

  公开号：EP3722297A1

  公开（公告）日：2020-10-14

  The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D] pyrimidine compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them.

  本公开总体上涉及类收费受体调节剂化合物，如二氨基吡啶并[3,2 D]嘧啶化合物和药物组合物，除其他外，它们可调节类收费受体（如 TLR-8），以及制造和使用它们的方法。
• Studies on Condensed Pyrimidine Systems. XIV. Some Pyrido [3,2-d]pyrimidines
  作者：Roland K. Robins、George H. Hitchings

  DOI：10.1021/ja01586a026

  日期：1956.3
• FUSED PYRIDINE DERIVATIVES AS KINASE INHIBITORS
  申请人：UCB Biopharma SPRL

  公开号：EP3356365A1

  公开（公告）日：2018-08-08
• CYCLOPROPYL FUSED THIAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
  申请人：AMGEN INC.

  公开号：US20170267673A1

  公开（公告）日：2017-09-21

  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 A 4 , A 5 , A 6 , A 8 , and 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.