2-[4-(2-oxo-1,3-oxazolidin-3-yl)phenyl]-N-[3-(trifluoromethyl)imidazo[5,1-b][1,3]thiazol-7-yl]acetamide | 1279720-80-7

• 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-(2-oxo-1,3-oxazolidin-3-yl)phenyl]-N-[3-(trifluoromethyl)imidazo[5,1-b][1,3]thiazol-7-yl]acetamide
• CAS: 1279720-80-7
• 化学式: C₁₇H₁₃F₃N₄O₃S
• 分子量: 410.376
• InChiKey: WIDKXLJIRJGSLP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  104
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  对溴苯乙酸 在 tris-(dibenzylideneacetone)dipalladium(0) 、 2-二环己基磷-2,4,6-三异丙基联苯 potassium carbonate 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 作用下， 以 2-甲基-2-丁醇 、 二氯甲烷 为溶剂， 反应 2.5h， 生成 2-[4-(2-oxo-1,3-oxazolidin-3-yl)phenyl]-N-[3-(trifluoromethyl)imidazo[5,1-b][1,3]thiazol-7-yl]acetamide
  参考文献：
  名称：

  [EN] IMIDOTHIAZOLE KINASE INHIBITORS
  [FR] INHIBITEURS IMIDAZOTHIAZOLIQUES DE KINASES

  摘要：

  本发明涉及一种新型激酶抑制剂的一般化学式(I)及其药用盐，以及将该一般化学式(I)的激酶抑制剂用于治疗涉及tau磷酸化和细胞周期调节的疾病或紊乱，如阿尔茨海默病和癌症。

  公开号：

  WO2011037780A1

文献信息

• IMIDOTHIAZOLE KINASE INHIBITORS
  申请人：Machacek Michelle R.

  公开号：US20130225591A1

  公开（公告）日：2013-08-29

  The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.

  本发明涉及一种新型激酶抑制剂，其化学式为(I)，以及其药学上可接受的盐，并且本发明涉及使用化学式(I)的激酶抑制剂治疗涉及tau磷酸化和细胞周期调节的疾病或疾病，例如阿尔茨海默病和癌症。
• COMPOSITIONS AND METHODS TO IMPROVE THE THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS INCLUDING SUBSTITUTED NAPHTHALIMIDES SUCH AS AMONAFIDE FOR THE TREATMENT OF IMMUNOLOGICAL, METABOLIC, INFECTIOUS, AND BENIGN OR NEOPLASTIC HYPERPROLIFERATIVE DISEASE CONDITIONS
  申请人：BROWN Dennis M.

  公开号：US20160067241A1

  公开（公告）日：2016-03-10

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to naphthalimides such as amonafide or analogs, derivatives, or prodrugs thereof.
• [EN] COMPOSITIONS AND METHODS TO IMPROVE THE THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS INCLUDING SUBSTITUTED NAPHTHALIMIDES SUCH AS AMONAFIDE FOR THE TREATMENT OF IMMUNOLOGICAL, METABOLIC, INFECTIOUS, AND BENIGN OR NEOPLASTIC HYPERPROLIFERATIVE DISEASE CONDITIONS<br/>[FR] COMPOSITIONS ET PROCÉDÉS PERMETTANT D'AMÉLIORER LE BÉNÉFICE THÉRAPEUTIQUE DES COMPOSÉS CHIMIQUES ADMINISTRÉS DE MANIÈRE SUBOPTIMALE COMPRENANT DES NAPHTALIMIDES SUBSTITUÉS TELS QUE L'AMONAFIDE POUR LE TRAITEMENT DES MALADIES IMMUNOLOGIQUES, MÉTABOLIQUES, INFECTIEUSES ET INFECTIEUSES OU HYPERPROLIFÉRATIVES ET NÉOPLASTIQUES.
  申请人：BROWN DENNIS M

  公开号：WO2014179528A2

  公开（公告）日：2014-11-06

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to naphthalimides such as amonafide or analogs, derivatives, or prodrugs thereof.
• [EN] IMIDOTHIAZOLE KINASE INHIBITORS<br/>[FR] INHIBITEURS IMIDAZOTHIAZOLIQUES DE KINASES
  申请人：MERCK SHARP & DOHME

  公开号：WO2011037780A1

  公开（公告）日：2011-03-31

  The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.

  本发明涉及一种新型激酶抑制剂的一般化学式(I)及其药用盐，以及将该一般化学式(I)的激酶抑制剂用于治疗涉及tau磷酸化和细胞周期调节的疾病或紊乱，如阿尔茨海默病和癌症。