2-Benzyl-2,9-diazaspiro[5.5]undecane

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 2-Benzyl-2,9-diazaspiro[5.5]undecane
• 化学式: C₁₆H₂₄N₂
• 分子量: 244.38
• InChiKey: QIQMOZPPWNBFSR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2-(苯基甲基)-2,9-二氮杂螺[5.5]十一烷-8,10-二酮 在 lithium aluminium tetrahydride 、 水 作用下， 以 四氢呋喃 为溶剂， 反应 8.25h， 以72%的产率得到2-Benzyl-2,9-diazaspiro[5.5]undecane
  参考文献：
  名称：

  [EN] SUBSTITUTED DIAZA-SPIRO-[5.5]-UNDECANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS
  [FR] DERIVES DE DIAZA-SPIRO-[5.5]-UNDECANE SUBSTITUES ET LEUR UTILISATION EN TANT QU'ANTAGONISTES DE LA NEUROKININE

  摘要：

  本发明涉及替代的二氮杂螺[5.5]十一烷衍生物，具有神经激肽拮抗活性，特别是NK1拮抗活性、NK1/NK2联合拮抗活性、NK1/NK3联合拮抗活性和NK1/NK2/NK3联合拮抗活性，它们的制备、包含它们的组合物和它们作为药物的用途，特别是用于治疗和/或预防精神分裂症、恶心、焦虑和抑郁症、肠易激综合征（IBS）、昼夜节律紊乱、妊娠高血压、疼痛感知、疼痛，特别是内脏和神经病性疼痛、胰腺炎、神经源性炎症、哮喘、COPD和排尿障碍，如尿失禁。根据本发明的化合物可以用一般式（I）（I）表示，并且还包括其药用可接受的酸盐或碱盐加合物、立体化异构体形式、N-氧化物形式和前药形式，其中所有取代基的定义如权利要求1中所定义。

  公开号：

  WO2005097795A1

文献信息

• SUBSTITUTED AZASPIRO DERIVATIVES
  申请人：Xu Yuelian

  公开号：US20080247964A1

  公开（公告）日：2008-10-09

  Substituted azaspiro derivatives of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

  提供了公式中的替代的azaspiro衍生物，其中变量如本文所述。这些化合物可以用于调节组织胺H3受体在体内或体外的配体结合，并在治疗人类、家养伴侣动物和家畜动物的各种中枢神经系统（CNS）和其他疾病方面特别有用。本文提供的化合物可以单独或与一个或多个其他CNS药剂联合使用，以增强其他CNS药剂的效果。提供了用于治疗这些疾病的药物组合物和方法，以及用于检测组织胺H3受体（例如，受体定位研究）的配体的方法。
• Substituted Diaza-Spiro-[5.5]-Undecane Derivaties and Their Use as Neurokinin Antagonists
  申请人：Janssens Eduard Frans

  公开号：US20070232636A1

  公开（公告）日：2007-10-04

  This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, a combined NK 1 /NK 2 antagonistic activity, a combined NK 1 /NK 3 antagonistic activity and a combined NK 1 /NK 2 /NK 3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, COPD and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
• US7544694B2
  申请人：——

  公开号：US7544694B2

  公开（公告）日：2009-06-09
• [EN] SUBSTITUTED AZASPIRO DERIVATIVES<br/>[FR] DÉRIVÉS AZASPIRO SUBSTITUÉS
  申请人：NEUROGEN CORP

  公开号：WO2007133561A2

  公开（公告）日：2007-11-22

  [EN] Substituted azaspiro derivatives of the Formula (I) are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
  [FR] L'invention concerne des dérivés azaspiro substitués de formule (I), les variables étant telles que décrites ici. De tels composés peuvent être utilisés pour moduler la liaison de ligands aux récepteurs H3 de l'histamine de façon in vivo ou in vitro et ils sont particulièrement utiles dans le traitement d'un grand nombre de troubles du système nerveux central (SNC) et d'autres troubles chez les êtres humains, les animaux de compagnie domestiqués et les animaux d'élevage. Les composés de la présente invention peuvent être administrés seuls ou en association avec un ou plusieurs autres agents pour le SNC pour maximiser les effets du ou des autres agents pour le SNC. L'invention concerne également des compositions pharmaceutiques et des procédés servant à traiter de tels troubles, ainsi que des procédés d'utilisation de tels ligands pour détecter les récepteurs H3 de l'histamine (par exemple pour des études de localisation des récepteurs).
• [EN] SUBSTITUTED DIAZA-SPIRO-[5.5]-UNDECANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS<br/>[FR] DERIVES DE DIAZA-SPIRO-[5.5]-UNDECANE SUBSTITUES ET LEUR UTILISATION EN TANT QU'ANTAGONISTES DE LA NEUROKININE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2005097795A1

  公开（公告）日：2005-10-20

  This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, COPD and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

  本发明涉及替代的二氮杂螺[5.5]十一烷衍生物，具有神经激肽拮抗活性，特别是NK1拮抗活性、NK1/NK2联合拮抗活性、NK1/NK3联合拮抗活性和NK1/NK2/NK3联合拮抗活性，它们的制备、包含它们的组合物和它们作为药物的用途，特别是用于治疗和/或预防精神分裂症、恶心、焦虑和抑郁症、肠易激综合征（IBS）、昼夜节律紊乱、妊娠高血压、疼痛感知、疼痛，特别是内脏和神经病性疼痛、胰腺炎、神经源性炎症、哮喘、COPD和排尿障碍，如尿失禁。根据本发明的化合物可以用一般式（I）（I）表示，并且还包括其药用可接受的酸盐或碱盐加合物、立体化异构体形式、N-氧化物形式和前药形式，其中所有取代基的定义如权利要求1中所定义。