(3R,4S)-N-ethyl-4-[[2-methoxy-5-[5-(trifluoromethyl)tetrazol-1-yl]phenyl]methylamino]-3-phenylpiperidine-1-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (3R,4S)-N-ethyl-4-[[2-methoxy-5-[5-(trifluoromethyl)tetrazol-1-yl]phenyl]methylamino]-3-phenylpiperidine-1-carboxamide
• 化学式: C₂₄H₂₈F₃N₇O₂
• 分子量: 503.5
• InChiKey: LAPDOBVFPRPNFV-PMACEKPBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  97.2
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• Piperidine derivative, process for producing the same, and use
  申请人：Ikeura Yoshinori

  公开号：US20060167052A1

  公开（公告）日：2006-07-27

  The present invention provides a compound represented by the formula: wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R 1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally lo substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R 1 is not a methyl group, and 15 when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

  本发明提供了一种化合物，其表示为以下式子：其中Ar是芳基、芳基烷基或芳香杂环基，每个基团都可以被取代，R1是氢原子、可选取代的碳氢基团、酰基或可选取代的杂环基团，X是氧原子或可选取代的亚胺基团，Z是可选取代的亚甲基团，环A是可选进一步取代的哌啶环，环B是可选取代的芳香环，但当Z是取代有氧基的亚甲基团时，R1不是甲基基团，而当Z是取代有甲基基团的亚甲基团时，环B是取代的芳香环，或其盐。该化合物是一种新型哌啶衍生物，具有优异的缓解速激肽受体拮抗作用，可用作药物，特别是用作预防和/或治疗尿频和/或尿失禁的药剂。
• PIPERIDINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1553084A1

  公开（公告）日：2005-07-13

  The present invention provides a compound represented by the formula:    wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R1 is not a methyl group, and when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

  本发明提供了一种由式表示的化合物： 其中 Ar 是芳基、芳烷基或芳香杂环基团，每个基团均可被取代；R1 是氢原子、任选取代的烃基、酰基或任选取代的杂环基团；X 是氧原子或任选取代的亚氨基；Z 是任选取代的亚甲基；环 A 是任选进一步取代的哌啶环；环 B 是任选取代的芳香环、当 Z 是被氧代基团取代的亚甲基时，R1 不是甲基；当 Z 是被甲基取代的亚甲基时，环 B 是被取代的芳香环，或其盐，这是一种新型哌啶衍生物，对快速激肽受体有很好的拮抗作用，可用作药物，特别是预防和/或治疗尿频和/或尿失禁的药物。
• US7622487B2
  申请人：——

  公开号：US7622487B2

  公开（公告）日：2009-11-24