2-chloro-4-(2-methylpyridin-3-yloxy)pyridine | 1043022-76-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-chloro-4-(2-methylpyridin-3-yloxy)pyridine
• 英文别名: 3-(2-chloropyridin-4-yloxy)-2-methylpyridine；2-Chloro-4-(2-methylpyridin-3-yl)oxy-pyridine；2-chloro-4-(2-methylpyridin-3-yl)oxypyridine
• CAS: 1043022-76-9
• 化学式: C₁₁H₉ClN₂O
• 分子量: 220.658
• InChiKey: ZECXEHGXTCPYDI-UHFFFAOYSA-N

物化性质

• 沸点：
  328.3±42.0 °C(Predicted)
• 密度：
  1.263±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  35
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  氨基甲酸叔丁酯 、 2-chloro-4-(2-methylpyridin-3-yloxy)pyridine 在 tris-(dibenzylideneacetone)dipalladium(0) 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 potassium phosphate 作用下， 以 水 、 甲苯 为溶剂， 反应 72.0h， 以59%的产率得到tert-butyl 4-(2-methylpyridin-3-yloxy)pyridin-2-ylcarbamate
  参考文献：
  名称：

  WO2008/91770

  摘要：

  公开号：
• 作为产物：
  描述：

  3-羟基-2-甲基吡啶 、 2,4-二氯吡啶 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 以82%的产率得到2-chloro-4-(2-methylpyridin-3-yloxy)pyridine
  参考文献：
  名称：

  Rapid Generation of a High Quality Lead for Transforming Growth Factor-β (TGF-β) Type I Receptor (ALK5)

  摘要：

  A novel class of 4-pyridinoxy-2-anilinopyridine-based TGF-beta type I receptor (also known as activin-like kinase 5 or ALK5) inhibitors is reported. The binding mode of this scaffold was successfully predicted by analyzing possible docked binding modes of literature inhibitors and novel synthetic ideas. Compounds such as 19 are potent ALK5 inhibitors with good physicochemical and pharmacokinetic properties and thus represent high quality leads for further optimization.

  DOI：

  10.1021/jm900807w

文献信息

• CHEMICAL COMPOUNDS-821
  申请人：Finlay Maurice Raymond

  公开号：US20090048269A1

  公开（公告）日：2009-02-19

  The invention relates to chemical compounds of the formula (I), or pharmaceutically acceptable salts thereof, which possess ALK5 (TGFβR1) inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal such as man.

  该发明涉及化学式(I)的化合物，或其药学上可接受的盐，具有ALK5（TGFβR1）抑制活性，因此在抗癌活性方面有用，从而在治疗人体或动物体的方法中有用。该发明还涉及制造上述化学化合物的方法，含有它们的药物组合物，以及它们在制造用于在温血动物（如人）中产生抗癌效果的药物中的使用。
• [EN] UREA COMPOUNDS AS GKA ACTIVATORS<br/>[FR] COMPOSÉS D'URÉE EN TANT QU'ACTIVATEURS DE LA GKA
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2013086397A1

  公开（公告）日：2013-06-13

  The present invention relates to compounds, to pharmaceutical compositions comprising the compounds, to a process for making the compounds and to the use of the compounds in therapy. More particularly, it relates to certain glucokinase activators of Formulas 1 and 1a, useful in the treatment of diseases and disorders that would benefit from activation of glucokinase.

  本发明涉及化合物，包括含有该化合物的药物组合物，制备该化合物的方法以及在治疗中使用该化合物。更具体地，涉及到某些葡萄糖激酶激活剂的1和1a式，可用于治疗需要激活葡萄糖激酶的疾病和障碍。
• 2-AMINOPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS
  申请人：Aicher Thomas Daniel

  公开号：US20100099713A1

  公开（公告）日：2010-04-22

  Provided are compounds having the Formula I or salts thereof, wherein R 2 , L, R 3 , R 11 , D 2 and R 13 are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

  提供的化合物具有I式或其盐，其中R2、L、R3、R11、D2和R13的定义如本文所述，可用于治疗和/或预防由葡萄糖激酶活性不足引起的疾病，如糖尿病。还提供了治疗或预防由葡萄糖激酶活性不足或可以通过激活葡萄糖激酶治疗的疾病和疾病的方法。
• 2-aminopyridine derivatives as glucokinase activators
  申请人：Aicher Thomas Daniel

  公开号：US08431713B2

  公开（公告）日：2013-04-30

  Provided are compounds having the Formula I or salts thereof, wherein R2, L, R3, R11, D2 and R13 are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

  提供了具有公式I或其盐的化合物，其中R2、L、R3、R11、D2和R13的定义如本文所述，这些化合物在治疗和/或预防由葡萄糖激酶活性不足介导的疾病，如糖尿病等方面是有用的。还提供了治疗或预防由葡萄糖激酶活性不足或可以通过激活葡萄糖激酶治疗的疾病和疾病的方法。
• US8431713B2
  申请人：——

  公开号：US8431713B2

  公开（公告）日：2013-04-30