(R)-N-[2-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-2-methanesulphonyloxy-N-methyl-2-phenyl-acetamide | 251292-11-2

• 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: (R)-N-[2-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-2-methanesulphonyloxy-N-methyl-2-phenyl-acetamide
• 英文别名: [(1R)-2-[2-[3,5-bis(trifluoromethyl)phenyl]ethyl-methylamino]-2-oxo-1-phenylethyl] methanesulfonate
• CAS: 251292-11-2
• 化学式: C₂₀H₁₉F₆NO₄S
• 分子量: 483.432
• InChiKey: FLSFYGIFJUNVSK-QGZVFWFLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  72.1
• 氢给体数：
  0
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  (R)-N-[2-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-2-methanesulphonyloxy-N-methyl-2-phenyl-acetamide 、 扁桃酸 生成 N-[2-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-2-[4-(2-hydroxy-1-hydroxymethyl-ethylamino)-piperidin-1-yl]-N-methyl-2-phenylacetamide
  参考文献：
  名称：

  Neurokinin antagonists

  摘要：

  该发明涉及新的化合物I1的公式或其药学上可接受的盐，其中R1代表3-羟基丙基，1,3-二羟基丙-2-基或C3-C6-环烷基甲基，而R2、R3、R4和Ar的含义如规范中所述，以及其制备和使用。这些新化合物是有价值的神经激肽（速激肽）拮抗剂。

  公开号：

  US20020147219A1

文献信息

• Pharmaceutical compositions based on anticholinergics and NK1-receptor antagonists
  申请人：——

  公开号：US20020169181A1

  公开（公告）日：2002-11-14

  The present invention relates to novel pharmaceutical compositions based on anticholinergics and NK 1 -receptor antagonists, processes for preparing them and their use in the treatment of respiratory tract diseases.

  本发明涉及基于抗胆碱药物和NK1受体拮抗剂的新型药物组合物，以及其制备过程和在治疗呼吸道疾病中的应用。
• Pharmaceutical compositions based on anticholinergics and additional active ingredients
  申请人：Pairet Michel

  公开号：US20050148562A1

  公开（公告）日：2005-07-07

  A pharmaceutical composition comprising an anticholinergic and at least one additional active ingredient selected from among corticosteroids, dopamine agonistes, PDE-IV inhibitors, NK1-antagonists, endothelin antagonists, antihistamines, and EGFR-kinase inhibitors, processes for preparing them and their use in the treatment of respiratory diseases.

  一种包括抗胆碱药物和至少一种额外活性成分的制药组合物，所述额外活性成分从皮质类固醇、多巴胺激动剂、PDE-IV抑制剂、NK1拮抗剂、内皮素拮抗剂、抗组胺药和EGFR激酶抑制剂中选择，以及制备它们的方法及其在治疗呼吸系统疾病中的用途。
• Method for the treatment or prevention of atopic dermatitis
  申请人：Boehringer Ingelheim International GmbH

  公开号：US20030100565A1

  公开（公告）日：2003-05-29

  The invention relates to a method for the treatment or prevention of atopic dermatitis, which comprises the administration of an effective amount of an NK-1 receptor antagonist to a patient in need of such treatment, wherein said NK1 receptor antagonist is effective in inhibiting the substance P (SP-)induced scratching in mice and/or guinea pigs.

  这项发明涉及一种治疗或预防特应性皮炎的方法，包括向需要该治疗的患者施用有效量的NK-1受体拮抗剂，其中所述的NK-1受体拮抗剂能够有效抑制小鼠和/或豚鼠中由P物质（SP）诱导的搔抓行为。
• Method for the treatment of prevention of atopic dermatitis
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP1295599A1

  公开（公告）日：2003-03-26

  The invention relates to a method for the treatment or prevention of atopic dermatitis, which comprises the administration of an effective amount of an NK-1 receptor antagonist to a patient in need of such treatment, wherein said NK1 receptor antagonist is effective in inhibiting the substance P (SP-)induced scratching in mice.

  这项发明涉及一种治疗或预防特应性皮炎的方法，包括向需要该治疗的患者施用有效量的NK-1受体拮抗剂，其中所述NK1受体拮抗剂有效地抑制小鼠中由P物质（SP）引起的搔抓行为。
• Processes and intermediate compounds for preparing guanidine and amidine derivatives
  申请人：——

  公开号：US20020010173A1

  公开（公告）日：2002-01-24

  The invention relates to new compounds of general formula I 1 or the pharmaceutically acceptable salts thereof, wherein X=N-R 3 or CH-R 4 , Y=CH 2 or (CH 2 ) 2 , Z=O or H 2 ; and R 1 , R 2 , R 3 , R 4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.

  本发明涉及一种新的化合物，其一般式为I1或其药学上可接受的盐，其中X＝N-R3或CH-R4，Y＝CH2或(CH2)2，Z＝O或H2；R1、R2、R3、R4和Ar的含义如说明书中所给出的，并且本发明还涉及其制备和使用。这些新化合物是有价值的神经激肽（快速激肽）拮抗剂。