phenacyl (1R,2S)-2-[(2-methylpropan-2-yl)oxycarbonylamino]cyclopentane-1-carboxylate | 1071432-88-6

• 英文名称: phenacyl (1R,2S)-2-[(2-methylpropan-2-yl)oxycarbonylamino]cyclopentane-1-carboxylate
• CAS: 1071432-88-6
• 化学式: C₁₉H₂₅NO₅
• 分子量: 347.411
• InChiKey: PXJYDLVZZPJYNW-CABCVRRESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  25
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  81.7
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• ORNITHINE DERIVATIVE
  申请人：Zenkoh Tatsuya

  公开号：US20100216803A1

  公开（公告）日：2010-08-26

  Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.

  提供了一种化合物，可用作慢性肾功能不全的治疗剂和糖尿病肾病的治疗剂。本发明人对具有对EP4受体拮抗作用的鸟氨酸衍生物进行了广泛的研究，结果发现通过在本发明化合物的鸟氨酸部分的C末端引入环烷二基，可以改善其溶解性等物理化学性质，从而赋予更优选的药物特性。因此，他们完成了本发明。本发明化合物表现出良好的对EP4受体的拮抗作用，因此，可用作慢性肾功能不全和糖尿病肾病的治疗剂。
• US8030489B2
  申请人：——

  公开号：US8030489B2

  公开（公告）日：2011-10-04