2-phenoxy-3-[3-(3-(2-hydroxyethoxy)pyridin-4-yl)propoxy]pyridine.monofumarate | 382140-83-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-phenoxy-3-[3-(3-(2-hydroxyethoxy)pyridin-4-yl)propoxy]pyridine.monofumarate
• 英文别名: (E)-but-2-enedioic acid;2-[4-[3-(2-phenoxypyridin-3-yl)oxypropyl]pyridin-3-yl]oxyethanol
• CAS: 382140-83-2
• 化学式: C₄H₄O₄*C₂₁H₂₂N₂O₄
• 分子量: 482.49
• InChiKey: INDWRRZEAWAAEE-WLHGVMLRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.36
• 重原子数：
  35
• 可旋转键数：
  12
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  148
• 氢给体数：
  3
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  2-phenoxy-3-[3-(3-hydroxypyridin-4-yl)propoxy]pyridine 、 1-溴-2-(甲氧基甲氧基)乙烷 在 盐酸 作用下， 以 乙醇 、 氯仿 、 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 生成 2-phenoxy-3-[3-(3-(2-hydroxyethoxy)pyridin-4-yl)propoxy]pyridine 、 2-phenoxy-3-[3-(3-(2-hydroxyethoxy)pyridin-4-yl)propoxy]pyridine.monofumarate
  参考文献：
  名称：

  2,3-disubstituted pyridine derivatives, process for the preparation thereof, drug compositions containing the same and intermediates for the preparation

  摘要：

  一种具有式（I）的化合物，其中A为O、S、CHR1或NR2，R1和R2为H、较低的烷基，X1和X2为H、卤素、硝基、氰基等，Y1为H、较低的烷基，Z1和Z2为H、卤素、氰基、羟基、较低的烷基等，n为2至4的整数，其药学上可接受的盐，制备该化合物的方法，含有该化合物作为活性成分的药物组合物，以及其中间体。本发明的化合物（I）显示出强大的PDE IV抑制活性以及出色的支气管扩张活性，因此，在过敏性炎症性疾病或器官炎症性疾病的治疗或预防中，特别是在伴有气道阻塞的肺部疾病（如哮喘）的治疗或预防中，它们被广泛用作PDE IV抑制剂。

  公开号：

  US06555557B1

文献信息

• PTH derivatives resistant to skin proteases
  申请人：——

  公开号：US20040023882A1

  公开（公告）日：2004-02-05

  Protease-resistant analogues of biologically active derivatives of human PTH are described. These analogs are intended for use in therapeutic preparations for the treatment of various medical conditions in which bone loss is encountered or is susceptible of being encountered. The analogs specified are hPTH(1-34) and hPTH(1-31). More particularly, protease-resistant analogs of PTH adapted for transdermal administration are described.
• US6555557B1
  申请人：——

  公开号：US6555557B1

  公开（公告）日：2003-04-29
• US6765095B2
  申请人：——

  公开号：US6765095B2

  公开（公告）日：2004-07-20
• [EN] PTH DERIVATIVES RESISTANT TO SKIN PROTEASES<br/>[FR] DERIVES DE LA PTH RESISTANTS AUX PROTEASES DE LA PEAU
  申请人：THERATECHNOLOGIES INC

  公开号：WO2003097690A2

  公开（公告）日：2003-11-27

  Protease-resistant analogues of biologically active derivatives of human PTH are described. These analogs are intended for use in therapeutic preparations for the treatment of various medical conditions in which bone loss is encountered or is susceptible of being encountered. The analogs specified are hPTH(1-34) and hPTH(1-31). More particularly, protease-resistant analogs of PTH adapted for transdermal administration are described.
• 2,3-disubstituted pyridine derivatives, process for the preparation thereof, drug compositions containing the same and intermediates for the preparation
  申请人：Dainippon Pharmaceutical Company, Limited

  公开号：US06555557B1

  公开（公告）日：2003-04-29

  A compound of the formula (I) wherein A is O, S, CHR1 or NR2, R1 and R2 are H, lower alkyl, X1 and X2 are H, halogen, nitro, cyano, etc., Y1 is H, lower alkyl, Z1 and Z2 are H, halogen, cyano, hydroxy, lower alkyl, etc., and n is an integer of 2 to 4, a pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and an intermediate therefor. The compounds (I) of the present invention show a potent PDE IV inhibitory activity as well as an excellent bronchodilating activity, and hence, they are widely useful as a PDE IV inhibitor in the treatment or prophylaxis of allergic inflammatory diseases or organ inflammatory diseases, especially in the treatment or prophylaxis of pulmonary diseases accompanied by airway obstruction such as asthma.

  一种具有式（I）的化合物，其中A为O、S、CHR1或NR2，R1和R2为H、较低的烷基，X1和X2为H、卤素、硝基、氰基等，Y1为H、较低的烷基，Z1和Z2为H、卤素、氰基、羟基、较低的烷基等，n为2至4的整数，其药学上可接受的盐，制备该化合物的方法，含有该化合物作为活性成分的药物组合物，以及其中间体。本发明的化合物（I）显示出强大的PDE IV抑制活性以及出色的支气管扩张活性，因此，在过敏性炎症性疾病或器官炎症性疾病的治疗或预防中，特别是在伴有气道阻塞的肺部疾病（如哮喘）的治疗或预防中，它们被广泛用作PDE IV抑制剂。