TTA-A2

• 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: TTA-A2
• 英文别名: (2-(4-cyclopropylphenyl)-N-((1R)-1-{5-[(2,2,2-trifluoroethyl)oxy]pyridin-2-yl}ethyl)acetamide)；2-(4-cyclopropylphenyl)-N-((1R)-1-{5-[(2,2,2-trifluoroethyl)oxo]pyridin-2-yl}ethyl)acetamide；(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide；2-(4-cyclopropylphenyl)-N-[(1R)-1-[5-(2,2,2-trifluoroethoxy)pyridin-2-yl]ethyl]acetamide
• 化学式: C₂₀H₂₁F₃N₂O₂
• 分子量: 378.394
• InChiKey: GEYDMBNDOVPFJL-CYBMUJFWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  27
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  51.2
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  3-羟基-6-甲基吡啶 在 盐酸 、 甲醇 、 N-羟基-7-氮杂苯并三氮唑 、 2,2,6,6-四甲基哌啶氧化物 、 碳酸氢钠 、 potassium carbonate 、 caesium carbonate 、 copper(II) sulfate 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 、 间氯过氧苯甲酸 、 potassium bromide 作用下， 以 甲醇 、 乙醚 、 二氯甲烷 、 氯仿 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 19.42h， 生成 TTA-A2
  参考文献：
  名称：

  Pyridyl amides as potent inhibitors of T-type calcium channels

  摘要：

  A novel series of amide T-type calcium channel antagonists were prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 led to identification of the potent and selective T-type antagonist 37 that displayed in vivo efficacy in rodent models of epilepsy and sleep. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.01.089

文献信息

• Pyridyl Amide T-Type Calcium Channel Antagonists
  申请人：Barrow James C.

  公开号：US20090275550A1

  公开（公告）日：2009-11-05

  The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

  本发明涉及对T型钙通道具有拮抗作用的吡啶酰胺化合物，其在治疗或预防与T型钙通道有关的疾病和疾病中具有用途。本发明还涉及包含这些化合物的制药组合物以及使用这些化合物和组合物预防或治疗与T型钙通道有关的疾病的用途。
• Methods for improving memory and cognition and for treating memory and cognitive disorders
  申请人：Cavion, Inc.

  公开号：US11324733B2

  公开（公告）日：2022-05-10

  This disclosure provides methods for the treatment of disease by administering pharmaceutical compounds. In particular, the disclosure relates to the treatment to improve memory or cognition, or to treat a memory or cognitive disorder, or to treat cognitive symptoms of a disease or condition by administering a T-type calcium channel antagonist.

  本公开提供了通过施用药物化合物治疗疾病的方法。特别是，本公开涉及通过给药 T 型钙通道拮抗剂来改善记忆或认知，或治疗记忆或认知障碍，或治疗疾病或病症的认知症状的治疗方法。
• WO2007/120729
  申请人：——

  公开号：——

  公开（公告）日：——
• PYRIDYL AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2010493B1

  公开（公告）日：2016-01-27
• VOLTAGE-DEPENDENT T-TYPE CALCIUM CHANNEL BLOCKER
  申请人：Nippon Chemiphar Co., Ltd.

  公开号：US20190077767A1

  公开（公告）日：2019-03-14

  A compound represented by the following General Formula (I), a tautomer or a stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, is used as a voltage-dependent T-type calcium channel blocker: wherein A represents a fused ring which may have a substituent, the fused ring being composed of a 5-membered heteroaryl group or a 5-membered or 6-membered heterocyclic ring and a benzene ring or the like, the 5-membered heteroaryl group having one to three identical or different heteroatoms as a ring-constituting element(s) having at least one substituent such as an alkoxy group having 1 to 8 carbon atoms and substituted with 1 to 5 halogen atoms; R represents a hydrogen atom or the like; B represents CR5(Q1) or NQ2, herein Q1 represents a benzimidazole group which may have a substituent; Q2 represents an alkyl group having 1 to 8 carbon atoms which may have a substituent, a heteroaryl group which may have a substituent, or the like; R0, R1, R2, R3, R4, and R5 each represent a hydrogen atom or the like; and n and m each represent 0, 1, or 2, provide that n and m are not 0 and 2 at the same time.