N-[5-cyclohexylmethyl-4-(4-hydroxy-phenyl)-thiazol-2-yl]-3,4,5-trihydroxy-benzamide | 1003312-87-5

• 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: N-[5-cyclohexylmethyl-4-(4-hydroxy-phenyl)-thiazol-2-yl]-3,4,5-trihydroxy-benzamide
• 英文别名: N-[5-(cyclohexylmethyl)-4-(4-hydroxyphenyl)-1,3-thiazol-2-yl]-3,4,5-trihydroxybenzamide
• CAS: 1003312-87-5
• 化学式: C₂₃H₂₄N₂O₅S
• 分子量: 440.52
• InChiKey: IZVKRXXSLXDODF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  151
• 氢给体数：
  5
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  N-[5-cyclohexylmethyl-4-(4-hydroxy-phenyl)-thiazol-2-yl]-3,4,5-trimethoxy-benzamide 、 三溴化硼 在 crude product 、 丙酮 作用下， 以to obtain a product as a white solid in a yield of 55.8%, mp的产率得到N-[5-cyclohexylmethyl-4-(4-hydroxy-phenyl)-thiazol-2-yl]-3,4,5-trihydroxy-benzamide
  参考文献：
  名称：

  Trisubstituted thiazole compounds, preparations methods, pharmaceutical compositions and medicals uses thereof

  摘要：

  本发明涉及公式(I)的2,4,5-三取代噻唑化合物或其所有可能的异构体、前药、药学上可接受的盐、溶剂化合物或水合物，用于抑制血浆PLTP活性和/或血浆CETP活性，其中取代基如规范中所定义；一种制备公式(I)化合物的方法；包括公式(I)化合物的制药组合物以及其用于制备哺乳动物（如动脉粥样硬化、心血管疾病和周围血管疾病等）的治疗和/或预防与增加的血浆PLTP活性和/或增加的血浆CETP活性相关的疾病的药物的用途。

  公开号：

  US08053581B2

文献信息

• TRISUBSTITUTED THIAZOLE COMPOUNDS, PREPARATIONS METHODS, PHARMACEUTICAL COMPOSITIONS AND MEDICALS USES THEREOF
  申请人：Li Song

  公开号：US20090298832A1

  公开（公告）日：2009-12-03

  The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.

  本发明涉及公式（I）的2,4,5-三取代噻唑化合物或所有可能的异构体、前药、药用盐、溶剂合物或水合物，用于抑制血浆PLTP活性和/或血浆CETP活性，其中取代基如规范中定义；一种用于制备公式（I）化合物的方法；包括公式（I）化合物的药物组合物以及其用于制备治疗和/或预防与哺乳动物体内增加的血浆PLTP活性和/或增加的血浆CETP活性相关的疾病的药物的用途，如动脉粥样硬化、心血管疾病和周围血管疾病等。
• 2,4,5-trisubstituted thiazole compounds,preparation methods,pharmaceutical compositions and medical uses thereof
  申请人：Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L. A. China

  公开号：EP2772488A1

  公开（公告）日：2014-09-03

  The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.

  本发明涉及用于抑制血浆PLTP活性和/或血浆CETP活性的式(I)的2,4,5-三取代噻唑化合物或其所有可能的异构体、原药、药学上可接受的盐、溶液或水合物，其中取代基如说明书中所定义；制备式(I)化合物的工艺；一种包含式（I）化合物的药物组合物及其用于制备治疗和/或预防与哺乳动物血浆 PLTP 活性升高和/或血浆 CETP 活性升高有关的疾病（如动脉粥样硬化、心血管疾病和外周血管疾病等）的药物。
• 2,4,5-TRISUBSTITUTED THIAZOLE COMPOUNDS,PREPARATION METHODS, PHARMACEUTICAL COMPOSITIONS AND MEDICAL USES THEREOF
  申请人：Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L. A. China

  公开号：EP2042494B1

  公开（公告）日：2014-07-09
• US8053581B2
  申请人：——

  公开号：US8053581B2

  公开（公告）日：2011-11-08