2-[4-(4-nitrophenoxy)phenyl]oxazole | 943767-52-0

• 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: 2-[4-(4-nitrophenoxy)phenyl]oxazole
• 英文别名: 2-[4-(4-nitrophenoxy)phenyl]-1,3-oxazole
• CAS: 943767-52-0
• 化学式: C₁₅H₁₀N₂O₄
• 分子量: 282.255
• InChiKey: JIKGZAVEOYQKMZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  81.1
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-[4-(4-nitrophenoxy)phenyl]oxazole 在 钯 氮 、 甲醇 作用下， 以 乙酸乙酯 、 甲醇 为溶剂， 反应 3.0h， 以to give the 2.4 g of 4-[4-(2-oxazolyl)phenoxy]benzenamine的产率得到4-[4-(2-oxazolyl)phenoxy]benzenamine
  参考文献：
  名称：

  Diamine derivatives as inhibitors of leukotriene A4 hydrolase

  摘要：

  本发明涉及化合物式(I)的化合物： 其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9如本文所述，作为单一立体异构体或立体异构体混合物，或其药学上可接受的盐，溶剂合物，包合物，多晶体，铵离子，N-氧化物或其前药；它们是白三烯A4水解酶抑制剂，因此在治疗炎症性疾病方面有用。本发明还公开了包含该化合物的药物组合物以及制备该化合物的方法。

  公开号：

  US20070155726A1
• 作为产物：
  描述：

  4-(噁唑-2-基)苯酚 、 对氟硝基苯 在 potassium tert-butylate 作用下， 以 二甲基亚砜 为溶剂， 反应 17.0h， 生成 2-[4-(4-nitrophenoxy)phenyl]oxazole
  参考文献：
  名称：

  Diamine derivatives as inhibitors of leukotriene A4 hydrolase

  摘要：

  这项发明涉及式(I)的化合物： 其中r、q、R、R2、R3、R4、R5a、R5b、R5c、R6a、R6b、R6c、R7、R8和R9如本文所述，可以是单一立体异构体或立体异构体混合物，或其药学上可接受的盐、溶剂合物、包合物、多型体、铵离子、N-氧化物或其前药；这些化合物是白三烯A4水解酶抑制剂，因此在治疗炎症性疾病中有用。还公开了包括该发明化合物的药物组合物以及制备该发明化合物的方法。

  公开号：

  US20070155726A1

文献信息

• Amide inhibitors of leukotriene A4 hydrolase
  申请人：Chen Ming

  公开号：US20070155727A1

  公开（公告）日：2007-07-05

  This invention is directed to compounds of formula (I): where r, q, R, R 2 , R 3 , R 4a , R 4b , R 4c , R 5a , R 5b , R 5c , R 6a , R 6b , R 6c , R 7 , R 8 , R 9 and R 10 are described herein, or pharmaceutically acceptable salts, solvates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A 4 hydrolase inhibitors and which are therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of using and preparing the compounds of the invention are also disclosed.

  本发明涉及的化合物的化学式为（I）：其中r、q、R、R2、R3、R4a、R4b、R4c、R5a、R5b、R5c、R6a、R6b、R6c、R7、R8、R9和R10如本文所述，或其药学上可接受的盐、溶剂化合物、多晶形、铵离子、N-氧化物或其前药；这些化合物是白三烯A4水解酶抑制剂，因此在治疗炎症性疾病方面具有用途。本发明还涉及包含所述化合物的药物组合物以及使用和制备所述化合物的方法。
• DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE
  申请人：Celtaxsys, Inc.

  公开号：US20150080382A1

  公开（公告）日：2015-03-19

  This invention is directed to compounds of formula (I): where r, q, R, R 2 , R 3 , R 4 , R 5a , R 5b , R 5c , R 6a , R 6b , R 6c , R 7 , R 8 , and R 9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A 4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

  该发明涉及式（I）的化合物：其中r、q、R、R2、R3、R4、R5a、R5b、R5c、R6a、R6b、R6c、R7、R8和R9如本文所述，作为单一立体异构体或立体异构体混合物，或其药学上可接受的盐、溶剂化合物、包合物、多晶体、铵离子、N-氧化物或其前药；这些化合物是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。本发明还公开了包含该化合物的制药组合物以及制备该化合物的方法。
• Diamine Derivatives as Inhibitors of Leukotriene A4 Hydrolase
  申请人：Arnaiz Damian

  公开号：US20100210630A1

  公开（公告）日：2010-08-19

  This invention is directed to compounds of formula (I): where r, q, R, R 2 , R 3 , R 4 , R 5a , R 5b , R 5c , R 6a , R 6b , R 6c , R 7 , R 8 , and R 9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A 4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

  本发明涉及化合物的公式(I)：其中r、q、R、R2、R3、R4、R5a、R5b、R5c、R6a、R6b、R6c、R7、R8和R9如本文所述，可以作为单一立体异构体或立体异构体混合物，或其药学上可接受的盐、溶剂合物、包合物、多晶体、铵离子、N-氧化物或前药；这些化合物是白三烯A4水解酶抑制剂，因此在治疗炎症性疾病方面有用。本发明还公开了包含该化合物的制药组合物以及制备该化合物的方法。
• INHIBITORS OF LEUKOTRIENE A4 HYDROLASE
  申请人：Celtaxsys, Inc.

  公开号：US20160068534A1

  公开（公告）日：2016-03-10

  The present invention is directed to compounds encompassed by the Formula (I), pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4 h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders.

  本发明涉及公式（I）所包含的化合物，其制药组合物，抑制LTA-4水解酶的方法，以及通过抑制LTA4h活性治疗疾病和疾病的方法和治疗疾病和疾病的方法。此类疾病和状况的非限制性示例包括炎症和自身免疫性疾病和疾病。
• Inhibitors of leukotriene A4 hydrolase
  申请人：CELTAXSYS, INC.

  公开号：US10399986B2

  公开（公告）日：2019-09-03

  The present invention is directed to compounds encompassed by the Formula (I): pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders.

  本发明涉及式 (I) 所包含的化合物： 其药物组合物、抑制LTA-4水解酶的方法，以及治疗通过抑制LTA4h活性而得到改善的疾病和紊乱的方法。此类疾病和病症的非限制性实例包括炎症性和自身免疫性疾病和病症。