N-[3-(4-acetyl-4-phenylpiperidin-1-yl)-1-phenylpropyl]benzenesulfonamide

• 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: N-[3-(4-acetyl-4-phenylpiperidin-1-yl)-1-phenylpropyl]benzenesulfonamide
• 化学式: C₂₈H₃₂N₂O₃S
• 分子量: 476.6
• InChiKey: RJPHUNDVRMBNRH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  34
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  74.9
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
  申请人：——

  公开号：US20040002504A1

  公开（公告）日：2004-01-01

  The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: 1 wherein, generally, Q is 2 R 1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C 1-4 alkyl or halogen, such as methyl, fluorine or bromine; R 2 is hydrogen or C 1-4 alkyl such as methyl; R 3 is phenyl; R 4 is hydrogen; R 5 is hydrogen or C 1-6 alkylcarbonyl such as methylcarbonyl; X is —SO 2 — or —C(O)N(R 2 )SO 2 — where R 2 is preferably hydrogen; Y is a bond, CH 2 or Z 1 where Z 1 is —N(R f )— in which R f is C 1-6 alkylcarbonyl such as ethylcarbonyl; and R 6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C 1-6 alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.

  本发明提供了一种治疗患有疾病（如精神分裂症）的受试者的方法，其中该疾病的治疗需要使用NK-3拮抗剂，包括向该受试者施用化合物I的治疗有效量： 1 其中，通常情况下， Q是 2 R 1 是苄基、苯基、噻吩或咪唑基，可选择地用C 1-4 烷基或卤素（如甲基、氟或溴）取代； R 2 是氢或C 1-4 烷基，如甲基； R 3 是苯基； R 4 是氢； R 5 是氢或C 1-6 烷基羰基，如甲基羰基； X是—SO 2 —或—C(O)N(R 2 )SO 2 —，其中R 2 最好是氢； Y是键、CH 2 或Z 1 ，其中Z 1 是—N(R f )—，其中R f 是C 1-6 烷基羰基，如乙基羰基；以及 R 6 是苯基、吡唑基、吡啶基、嘧啶基或苯并咪唑基，可选择地用来自C 1-6 烷基和苄基的一个或两个基团取代，如甲基、乙基和苄基； 或其药学上可接受的盐。
• N-(3-(4-Substituted-1-piperiding1)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
  申请人：Chambers Stuart Mark

  公开号：US20070117847A1

  公开（公告）日：2007-05-24

  The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R 1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C 1-4 alkyl or halogen, such as methyl, fluorine or bromine; R 2 is hydrogen or C 1-4 alkyl such as methyl; R 3 is phenyl; R 4 is hydrogen; R 5 is hydrogen or C 1-6 alkylcarbonyl such as methylcarbonyl; X is —SO 2 — or —C(O)N(R 2 )SO 2 — where R 2 is preferably hydrogen; Y is a bond, CH 2 or Z 1 where Z 1 is —N(R f )— in which R f is C 1-6 alkylcarbonyl such as ethylcarbonyl; and R 6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C 1-6 alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.

  本发明提供了一种治疗患有疾病（如精神分裂症）的受试者的方法，该疾病需要给予NK-3拮抗剂治疗，其中包括向该受试者给予化合物I的治疗有效量，化合物I的一般结构如下：其中，Q是；R1是苄基、苯基、噻吩基或咪唑基，可选地取代C1-4烷基或卤素，例如甲基、氟或溴；R2是氢或C1-4烷基，例如甲基；R3是苯基；R4是氢；R5是氢或C1-6烷基羰基，例如甲基羰基；X是-SO2-或-C（O）N（R2）SO2-，其中R2最好是氢；Y是键，CH2或Z1，其中Z1是-N（Rf）-，其中Rf是C1-6烷基羰基，例如乙酰基；R6是苯基、吡唑基、吡啶基、嘧啶基或苯并咪唑基，可选地取代一或两个来自C1-6烷基和苄基的基团，例如甲基、乙基和苄基；或其药学上可接受的盐。
• US7153868B2
  申请人：——

  公开号：US7153868B2

  公开（公告）日：2006-12-26