4-[(3,4-二氯苯基)乙酰基]-3-(1-吡咯烷基甲基)-1-哌嗪羧酸甲酯富马酸酯 | 126766-32-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-[(3,4-二氯苯基)乙酰基]-3-(1-吡咯烷基甲基)-1-哌嗪羧酸甲酯富马酸酯
• 英文名称: GR 89696 fumarate
• 英文别名: (E)-but-2-enedioic acid;methyl 4-[2-(3,4-dichlorophenyl)acetyl]-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate
• CAS: 126766-32-3
• 化学式: C23H29Cl2N3O7
• 分子量: 530.4
• InChiKey: ABTNETSDXZBJTE-WLHGVMLRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.62
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  128
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• Piperazine compounds
  申请人：GLAXO GROUP LIMITED

  公开号：EP0343900A2

  公开（公告）日：1989-11-29

  Compounds are disclosed of formula (I) wherein R₁ represents -COR₄, -CO₂R₄ or -COCO₂R₄ (where R₄ represents a hydrogen atom or an unsubstituted or substituted C₁₋₁₀ hydrocarbon moiety); R₂ and R₃ are the same or different and are C₁₋₆alkyl or C₃₋₆alkenyl; or -NR₂R₃ forms of 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by optionally substituted methylidene, -COR₅ (where R₅ represents C₁₋₆alkyl, -OR₆ or -NHR₆ and R₆ represents hydrogen, C₁₋₆alkyl, aryl, or ar(C₁₋₆) alkyl), or =NOR₇ (where R₇ represents C₁₋₆alkyl); X represents a direct bond, -CH₂- or -CH₂O-; Ar represents a substituted phenyl moiety; and physiologically acceptable salts thereof. The compounds are indicated as useful in the treatment of pain and cerebral ischaemia. Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.

  公开了式(I)化合物 其中 R₁ 代表 -COR₄、-CO₂R₄ 或 -CO₂R₄（其中 R₄ 代表氢原子或未取代或取代的 C₁₋₁₀ 碳氢分子）； R₂ 和 R₃ 相同或不同，并且是 C₁₋₆ 烷基或 C₃₋₆ 烯基；或-NR₂R₃形式的 5 元环（可选含有一个与氮相邻的氧原子）或 6 元环，该环可选含有一个不饱和单元，且该环未被取代或被可选取代的亚甲基取代、-COR₅（其中 R₅ 代表 C₁₋₆烷基、-OR₆或 -NHR₆，且 R₆ 代表氢、C₁₋₆烷基、芳基或 ar(C₁₋₆)烷基），或 =NOR₇（其中 R₇ 代表 C₁₋₆烷基）； X 代表直接键、-CH₂- 或 -CH₂O-； Ar 代表取代的苯基； 及其生理上可接受的盐类。 这些化合物可用于治疗疼痛和脑缺血。 此外，还公开了制备这些化合物的工艺和中间体以及含有这些化合物的药物组合物。
• Methods and compositions for treating vasomotor symptoms
  申请人：UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION

  公开号：US11083726B2

  公开（公告）日：2021-08-10

  The present disclosure is generally directed to compositions and methods for treating or limiting development of vasomotor symptoms in a subject.

  本公开总体上涉及用于治疗或限制受试者血管运动症状发展的组合物和方法。
• Methods for regulating neurotransmitter systems by inducing counteradaptations
  申请人：Michalow Alexander

  公开号：US20060069086A1

  公开（公告）日：2006-03-30

  The present invention relates to methods for regulating neurotransmitter systems by inducing a counteradaptation response. According to one embodiment of the invention, a method for regulating a neurotransmitter includes the step of repeatedly administering a ligand for a receptor in the neurotransmitter system, with a ratio of administration half-life to period between administrations of no greater than 1/2. The methods of the present invention may be used to address a whole host of undesirable mental and neurological conditions.

  本发明涉及通过诱导反适应反应来调节神经递质系统的方法。根据本发明的一个实施方案，调节神经递质的方法包括重复施用神经递质系统中受体的配体，施用半衰期与施用间隔期之比不大于1/2。本发明的方法可用于解决一系列不良的精神和神经状况。
• METHODS FOR REGULATING NEUROTRANSMITTER SYSTEMS BY INDUCING COUNTERADAPTATIONS
  申请人：Michalow, Alexander

  公开号：EP1809104A2

  公开（公告）日：2007-07-25
• EP1809104A4
  申请人：——

  公开号：EP1809104A4

  公开（公告）日：2009-04-29