2-adamantan-1-yl-N-(2-{[(3R)-3-aminopyrrolidin-1-yl]carbonyl}pyrazolo[1,5-a]pyridin-4-yl)acetamide | 1069070-30-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 英文名称: 2-adamantan-1-yl-N-(2-{[(3R)-3-aminopyrrolidin-1-yl]carbonyl}pyrazolo[1,5-a]pyridin-4-yl)acetamide
• 英文别名: Bicyclic heteroaryl amide derivative 3；2-(1-adamantyl)-N-[2-[(3R)-3-aminopyrrolidine-1-carbonyl]pyrazolo[1,5-a]pyridin-4-yl]acetamide
• CAS: 1069070-30-9
• 化学式: C₂₄H₃₁N₅O₂
• 分子量: 421.542
• InChiKey: CHANXFBBIWKIAI-ZWGBCBFGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  92.7
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• HETEROARYL AMIDE ANALOGUES AS P2X7 ANTAGONISTS
  申请人：Ihle David C.

  公开号：US20100266509A1

  公开（公告）日：2010-10-21

  Heteroaryl amide analogues are provided, of Formula (I), wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

  提供了异芳基酰胺类似物，其化学式为（I），其中变量如本文所述。这些化合物是配体，可用于体内或体外调节特定受体活性，并在治疗人类、家养伴侣动物和家畜动物的与病理受体激活相关的疾病方面特别有用。提供了用于治疗此类疾病的制药组合物和方法，以及用于受体定位研究的配体使用方法。
• Heteroaryl amide analogues as p2x7 antagonists
  申请人：H. Lundbeck A/S

  公开号：EP2592082A1

  公开（公告）日：2013-05-15

  Heteroaryl amide analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

  提供了杂芳基酰胺类似物，其分子式为 其中变量如本文所述。此类化合物是可用于调节体内或体外特异性受体活性的配体，特别适用于治疗与人类、驯养的伴侣动物和家畜的病理受体激活有关的疾病。本文提供了使用此类化合物治疗此类疾病的药物组合物和方法，以及使用此类配体进行受体定位研究的方法。
• Methods of modulating immune activity
  申请人：Flagship Pioneering Innovations V, Inc.

  公开号：US11376272B2

  公开（公告）日：2022-07-05

  In one aspect, the invention provides methods of increasing immune response by administering postcellular signaling factors produced by cells exposed to a stress condition. In one aspect, the invention provides methods of increasing immune response by administering in combination (a) a Stimulator of Interferon Genes (STING) agonist and (b) a purinergic receptor agonist. The increase in immune response may be used, for example, for treatment of infection or cancer. The invention also provides screening assays for identification of compounds that induce production of postcellular signaling factors which are also immunostimulatory agents. The invention further provides methods for identifying postcellular signaling factors with immunostimulatory activity. In another aspect, the invention provides methods of decreasing immune response by administering to a cell, tissue or subject a purinergic receptor antagonist alone or in combination with a Stimulator of Interferon Genes (STING) antagonist.

  一方面，本发明提供了通过施用暴露于应激条件下的细胞产生的细胞后信号因子来提高免疫应答的方法。在一个方面，本发明提供了通过联合施用(a)干扰素基因刺激剂（STING）激动剂和(b)嘌呤能受体激动剂来增加免疫反应的方法。免疫反应的增强可用于治疗感染或癌症等。本发明还提供了筛选测定法，用于鉴定能诱导产生细胞后信号因子的化合物，这些细胞后信号因子也是免疫刺激剂。本发明进一步提供了鉴定具有免疫刺激活性的细胞后信号因子的方法。在另一方面，本发明提供了通过向细胞、组织或受试者单独施用嘌呤能受体拮抗剂或与干扰素基因刺激剂（STING）拮抗剂联合施用来降低免疫反应的方法。
• METHODS OF MODULATING IMMUNE ACTIVITY
  申请人：Flagship Pioneering Innovations V, Inc.

  公开号：US20210299155A1

  公开（公告）日：2021-09-30

  In one aspect, the invention provides methods of increasing immune response by administering posteellular signaling factors produced by cells exposed to a stress condition. In one aspect, the invention provides methods of increasing immune response by administering in combination (a) a Stimulator of Interferon Genes (STING) agonist and (b) a purinergic receptor agonist. The increase in immune response may be used, for example, for treatment of infection or cancer. The invention also provides screening assays for identification of compounds that induce production of postcellular signaling factors which are also immunostimulatory agents. The invention further provides methods for identifying postcellular signaling factors with immunostimulatory activity. In another aspect, the invention provides methods of decreasing immune response by administering to a cell, tissue or subject a purinergic receptor antagonist alone or in combination with a Stimulator of Interferon Genes (STING) antagonist.
• US8580812B2
  申请人：——

  公开号：US8580812B2

  公开（公告）日：2013-11-12