4-Chloro-2-[(5-chloro-2-hydroxyphenyl)methyl]phenol;piperazine | 56186-94-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-Chloro-2-[(5-chloro-2-hydroxyphenyl)methyl]phenol;piperazine
• CAS: 56186-94-8
• 化学式: C₄H₁₀N₂*C₁₃H₁₀Cl₂O₂
• 分子量: 355.264
• InChiKey: CCYOKFIPABTJIW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.17
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  64.5
• 氢给体数：
  4
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  双氯酚 、 哌嗪 以78%的产率得到
  参考文献：
  名称：

  ZHELYAZKOV L.; TODOROVA N., TR. N.-I XIM.-FARM. IN-T, 1974, 9, 53-58

  摘要：

  DOI：

文献信息

• [EN] CYANOPYRIDINE DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE<br/>[FR] DÉRIVÉS DE CYANOPYRIDINE UTILISÉS EN TANT QU'AGONISTES DES RÉCEPTEURS BÊTA X DU FOIE, COMPOSITIONS ASSOCIÉES ET LEUR UTILISATION
  申请人：MERCK SHARP & DOHME

  公开号：WO2017083216A1

  公开（公告）日：2017-05-18

  In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

  在其多种实施方式中，本发明提供了含有化合物的替代氰基吡啶的化合物，其化学式为（I）：及其可接受的盐，其中R1、R2、R3、R4、R5、X、Y、Q和基团如本文所定义。本发明的新化合物以及包含其化合物的药学上可接受的组合物可用作肝X-β受体（LXRβ）激动剂，并且可能用于治疗或预防与之相关的病理。这些病理包括但不限于炎症性疾病和以胆固醇和脂质代谢缺陷为特征的疾病，如阿尔茨海默病。
• Cyanopyridine derivatives as liver X receptor beta agonists, compositions, and their use
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10239849B2

  公开（公告）日：2019-03-26

  In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

  在其许多实施方案中，本发明提供了含有式（I）：的取代氰基吡啶化合物及其可接受的盐，其中 R1、R2、R3、R4、R5、X、Y、Q 和基团如本文所定义。本发明的新型化合物以及包含其化合物的药学上可接受的组合物可作为肝 X-β 受体（LXRβ）激动剂，并可用于治疗或预防与之相关的病症。这些病症包括但不限于炎症性疾病和以胆固醇和脂质代谢缺陷为特征的疾病，如阿尔茨海默病。
• CYANOPYRIDINE DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP3373935A1

  公开（公告）日：2018-09-19
• Cyanopyridine Derivatives as Liver X Receptor Beta Agonists, Compositions, and Their Use
  申请人：RUDD Michael T.

  公开号：US20180327374A1

  公开（公告）日：2018-11-15

  In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.