Benzamide, N,N-diethyl-4-(5-hydroxyspiro(2H-1-benzopyran-2,4'-piperidin)-4-yl)- | 850305-06-5

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 新黄酮类化合物
• 英文名称: Benzamide, N,N-diethyl-4-(5-hydroxyspiro(2H-1-benzopyran-2,4'-piperidin)-4-yl)-
• 英文别名: N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide
• CAS: 850305-06-5
• 化学式: C₂₄H₂₈N₂O₃
• 分子量: 392.5
• InChiKey: OPIKUXLJQFYMSC-UHFFFAOYSA-N

物化性质

• 沸点：
  596.0±50.0 °C(Predicted)
• 密度：
  1.24±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  61.8
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] POSITIVE ALLOSTERIC MODULATORS OF THE DELTA-OPIOID RECEPTOR<br/>[FR] MODULATEURS ALLOSTÉRIQUES POSITIFS DU RÉCEPTEUR OPIOÏDE DELTA
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2016100605A1

  公开（公告）日：2016-06-23

  Described are the discovery, synthesis and pharmacological characterization of δ-opioid receptor-selective positive allosteric modulators (δ PAMs). These δ PAMs may increase the affinity and/or efficacy of the orthosteric agonists leu-enkephalin and SNC80, as measured by β-arrestin recruitment and adenylyl cyclase inhibition. The compounds may be useful pharmacological tools to probe the molecular pharmacology of the δ receptor and to explore the therapeutic potential of δ PAMs in diseases such as chronic pain and depression.

  本文描述了δ-阿片受体选择性正变构调节剂（δ PAMs）的发现、合成和药理学特征。这些δ PAMs可以通过β-阻滞素招募和腺苷酸环化酶抑制来增加正位激动剂亮-恩啡啶和SNC80的亲和力和/或功效。这些化合物可能是有用的药理学工具，用于探索δ受体的分子药理学和探索δ PAMs在慢性疼痛和抑郁等疾病的治疗潜力。
• Spirocyclic heterocyclic derivatives and methods of their use
  申请人：Dolle E. Roland

  公开号：US20050159438A1

  公开（公告）日：2005-07-21

  Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.

  本发明公开了螺环杂环衍生物、含有这些化合物的制药组合物以及它们的制药用途方法。在某些实施例中，螺环杂环衍生物是δ阿片受体的配体，可用于治疗和/或预防疼痛、焦虑、胃肠障碍和其他δ阿片受体介导的病症。
• Spirocyclic Heterocyclic Derivatives And Methods Of Their Use
  申请人：Dolle E. Roland

  公开号：US20080102031A1

  公开（公告）日：2008-05-01

  Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.

  本发明公开了螺环异杂环衍生物、含有这些化合物的制药组合物以及它们的制药用途方法。在某些实施例中，螺环异杂环衍生物是δ阿片受体的配体，可能有助于治疗和/或预防疼痛、焦虑、胃肠疾病和其他δ阿片受体介导的疾病等。
• SPIROCYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF THEIR USE
  申请人：Dolle Roland E.

  公开号：US20100029614A1

  公开（公告）日：2010-02-04

  Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.

  本发明公开了螺环杂环衍生物、含有这些化合物的制药组合物以及它们的制药用途的方法。在某些实施例中，螺环杂环衍生物是δ阿片受体的配体，并且可能有用于治疗和/或预防疼痛、焦虑、胃肠障碍和其他δ阿片受体介导的疾病等方面。
• METHODS FOR ENHANCING COGNITIVE FUNCTION
  申请人：Dolle E. Roland

  公开号：US20080119452A1

  公开（公告）日：2008-05-22

  Methods for enhancing cognitive function are disclosed. More particularly, methods are disclosed for enhancing cognitive function comprising the step of administering spirocyclic heterocyclic derivatives (including derivatives of spiro(2H-1-benzopyran-2,4′-piperidines) of the general formula IV:

  本发明揭示了增强认知功能的方法。更具体地，本发明揭示了一种增强认知功能的方法，其中包括给予螺环杂环衍生物（包括公式IV的螺(2H-1-苯并吡喃-2,4'-哌啶)衍生物）的步骤。