N-hydroxy-2-{[4-(1H-indol-3-yl)-cyclohexylamino]-2-[1-(trans-3,4,5-trifluorocinnamoyl)-piperidin-4-yl]}-acetamide | 1352560-35-0

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: N-hydroxy-2-{[4-(1H-indol-3-yl)-cyclohexylamino]-2-[1-(trans-3,4,5-trifluorocinnamoyl)-piperidin-4-yl]}-acetamide
• 英文别名: N-hydroxy-2-[[4-(1H-indol-3-yl)cyclohexyl]amino]-2-[1-[(E)-3-(3,4,5-trifluorophenyl)prop-2-enoyl]piperidin-4-yl]acetamide
• CAS: 1352560-35-0
• 化学式: C₃₀H₃₃F₃N₄O₃
• 分子量: 554.612
• InChiKey: MROSHPQAEZHUGL-BJMVGYQFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  40
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  97.5
• 氢给体数：
  4
• 氢受体数：
  7

文献信息

• [EN] 4-SUBSTITUTED-CYCLOHEXYLAMINO-4-PIPERIDINYL-ACETAMIDE ANTAGONISTS OF CCR2<br/>[FR] ANTAGONISTES DE CCR2 CONSISTANT EN DES CYCLOHEXYLAMINO-4-PIPÉRIDINYL-ACÉTAMIDES SUBSTITUÉS EN POSITION 4
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2012075115A1

  公开（公告）日：2012-06-07

  The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

  本发明涉及Formula (I)的化合物，其中：R1、R2、R3、R4、X、Y和Z如规范中定义。该发明还涉及一种预防、治疗或改善综合征、紊乱或疾病的方法，其中所述综合征、紊乱或疾病是II型糖尿病、肥胖和哮喘。该发明还涉及通过给哺乳动物施用Formula (I)中至少一种化合物的治疗有效量来抑制CCR2活性的方法。
• 4-SUBSTITUTED-CYCLOHEXYLAMINO-4-PIPERIDINYL-ACETAMIDE ANTAGONISTS OF CCR2
  申请人：Lanter James C.

  公开号：US20120142733A1

  公开（公告）日：2012-06-07

  The present invention comprises compounds of Formula (I). wherein: R 1 , R 2 , R 3 , R 4 , X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

  本发明涉及式(I)的化合物。其中：R1、R2、R3、R4、X、Y和Z如规范中所定义。本发明还涉及一种预防、治疗或缓解综合症、疾病或疾病的方法，其中所述综合症、疾病或疾病为2型糖尿病、肥胖症和哮喘。本发明还涉及一种通过给哺乳动物以式(I)的至少一种化合物的治疗有效量来抑制CCR2活性的方法。
• US8921559B2
  申请人：——

  公开号：US8921559B2

  公开（公告）日：2014-12-30