trans-1-(RS)-[4-(2-aminosulfonylphenyl)]-benzylaminocarbonyl-2-(SR)-benzylaminocarbonylcyclopentane

• 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: trans-1-(RS)-[4-(2-aminosulfonylphenyl)]-benzylaminocarbonyl-2-(SR)-benzylaminocarbonylcyclopentane
• 英文别名: (1R,2R)-2-N-benzyl-1-N-[[4-(2-sulfamoylphenyl)phenyl]methyl]cyclopentane-1,2-dicarboxamide
• 化学式: C₂₇H₂₉N₃O₄S
• 分子量: 491.611
• InChiKey: HODOVVLTYYRNJA-DNQXCXABSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  35
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  127
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-溴苯磺酰氯 在 四(三苯基膦)钯 N-溴代丁二酰亚胺(NBS) 、 sodium azide 、 偶氮二异丁腈 、 potassium carbonate 、 (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate 、 1-羟基苯并三唑 、 N,N-二异丙基乙胺 、 三苯基膦 、 N,N'-羰基二咪唑 、 三氟乙酸 作用下， 以 四氢呋喃 、 乙醇 、 二氯甲烷 、 水 、 溶剂黄146 、 二甲基亚砜 、 甲苯 为溶剂， 反应 70.0h， 生成 trans-1-(RS)-[4-(2-aminosulfonylphenyl)]-benzylaminocarbonyl-2-(SR)-benzylaminocarbonylcyclopentane
  参考文献：
  名称：

  [EN] 1,2 DIAMIDO CYCLOALKYL SODIUM CHANNEL BLOCKERS
  [FR] COMPOSES 1,2 DIAMIDO CYCLOALKYLE BLOQUEURS DES CANAUX SODIQUES

  摘要：

  公开号：

  WO2003101381A3

文献信息

• FUNCTION MODIFYING NAv 1.7 ANTIBODIES
  申请人：FINNEY HELENE MARGARET

  公开号：US20110135662A1

  公开（公告）日：2011-06-09

  A Na v 1.7 binding entity that after binding functionally modifies the activity of the ion channel, in particular an anti-Na v 1.7 antibody or binding fragment thereof, pharmaceutical compositions comprising said antibodies, use of the antibodies and compositions comprising the same, in treatment, for example in the treatment/modulation of pain and processes for generating and preparing said antibodies.

  一种Nav1.7结合实体，在结合后在功能上修改离子通道的活性，特别是抗Nav1.7抗体或其结合片段，包括所述抗体的药物组合物，以及使用该抗体和包含相同的组合物进行治疗，例如用于治疗/调节疼痛的治疗，以及生成和制备该抗体的方法。
• Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain
  作者：Pengchang P. Shao、Dong Ok、Michael H. Fisher、Maria L. Garcia、Gregory J. Kaczorowski、Chunshi Li、Kathryn A. Lyons、William J. Martin、Peter T. Meinke、Birgit T. Priest、McHardy M. Smith、Matthew J. Wyvratt、Feng Ye、William H. Parsons

  DOI：10.1016/j.bmcl.2005.02.002

  日期：2005.4

  A series of new voltage-gated sodium channel blockers were prepared based on the screening lead succinic diamide BPBTS. Replacement of the succinimide linker with the more rigid cyclic 1,2-trans-diamide linker was well tolerated. N-Methylation on the biphenylsulfonamide side of the amide moiety significantly reduced the clearance rate in rat pharmacokinetic studies. (c) 2005 Elsevier Ltd. All rights reserved.
• US20140342406A1
  申请人：——

  公开号：US20140342406A1

  公开（公告）日：2014-11-20
• ANTIBODIES TO ION CHANNELS
  申请人：UCB BIOPHARMA SPRL

  公开号：US20150203571A1

  公开（公告）日：2015-07-23

  An anti-E1 ion channel antibody or binding fragment thereof, pharmaceutical compositions comprising said antibodies, use of the antibodies and compositions comprising the same, in treatment, for example in the treatment/modulation of pain and processes for generating and preparing said antibodies.
• FUNCTION MODIFYING NAv1.7 ANTIBODIES
  申请人：UCB BIOPHARMA SPRL

  公开号：US20150232553A1

  公开（公告）日：2015-08-20

  A Na v 1.7 binding entity that after binding functionally modifies the activity of the ion channel, in particular an anti-Na v 1.7 antibody or binding fragment thereof, pharmaceutical compositions comprising said antibodies, use of the antibodies and compositions comprising the same, in treatment, for example in the treatment/modulation of pain and processes for generating and preparing said antibodies.