3-hydroxy-4-(4-phenylpiperazin-1-ylmethyl)-1-(toluene-4-sulfonyl)-1H-pyridin-2-one | 691013-05-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 3-hydroxy-4-(4-phenylpiperazin-1-ylmethyl)-1-(toluene-4-sulfonyl)-1H-pyridin-2-one
• 英文别名: 1-(4'-methylbenzenesulfonyl)-3-hydroxy-4-(4-phenylpiperazin-1-ylmethyl)pyridin-2(1H)-one；3-Hydroxy-1-(4-methylphenyl)sulfonyl-4-[(4-phenylpiperazin-1-yl)methyl]pyridin-2-one
• CAS: 691013-05-5
• 化学式: C₂₃H₂₅N₃O₄S
• 分子量: 439.535
• InChiKey: ZPXDJMZIOUFOQK-UHFFFAOYSA-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：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  89.5
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• PROLYL HYDROXYLASE INHIBITORS
  申请人：Gardner Joseph H.

  公开号：US20110110961A1

  公开（公告）日：2011-05-12

  Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1α), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.

  本文披露了一种可以稳定缺氧诱导因子-1α（HIF-1α）和缺氧诱导因子-2（HIF-2）的脯氨酸羟化酶抑制剂。本文还披露了包含所述化合物的一种或多种药物组合物。此外，还披露了一种用于刺激哺乳动物细胞免疫应答的方法，例如增加吞噬作用，延长吞噬细胞（包括角质细胞、中性粒细胞等）的寿命。因此，所披露的化合物提供了治疗与机体免疫应答相关疾病的方法。
• N-sulfonyl-4-methyleneamino-3-hydroxy-2-pyridones
  申请人：——

  公开号：US20040097559A1

  公开（公告）日：2004-05-20

  Compounds of Formula (I) 1 are effective in the treatment of a microbial infection.

  化合物式(I)1对治疗微生物感染有效。
• COMPOSITIONS AND METHODS FOR TREATING COLITIS
  申请人：Gardner Joseph H.

  公开号：US20110112055A1

  公开（公告）日：2011-05-12

  Disclosed herein are compositions and methods for treating colitis and other inflammatory bowel diseases, inter alia, indeterminate colitis, Crohn's disease, irritable bowel syndrome and ischemic colitis.

  本文揭示了治疗结肠炎和其他炎症性肠病的组合物和方法，包括不定性结肠炎、克罗恩病、肠易激综合征和缺血性结肠炎。
• METHODS FOR INCREASING THE STABILIZATION OF HYPOXIA INDUCIBLE FACTOR-1 ALPHA
  申请人：Shalwitz Robert

  公开号：US20110111058A1

  公开（公告）日：2011-05-12

  Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1α) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1α prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1α.

  本文披露了控制缺氧诱导转录因子1α（HIF-1α）活性及与之相关的疾病、病症或综合症的方法，包括周围血管疾病（PVD）、冠状动脉疾病（CAD）、心力衰竭、缺血和贫血等。此外，还披露了含有HIF-1α脯氨酸羟化酶抑制剂的药物组合物，可用于治疗与HIF-1α活性相关的疾病、病症和/或综合症。
• Prolyl hydroxylase inhibitors
  申请人：Aerpio Therapeutics Inc.

  公开号：EP2649998A1

  公开（公告）日：2013-10-16

  Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1α), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.

  本文公开的脯氨酰羟化酶抑制剂可以稳定缺氧诱导因子-1α（HIF-1α）以及缺氧诱导因子-2（HIF-2）。本文还公开了包含一种或多种已公开化合物的药物组合物。还进一步公开了刺激哺乳动物细胞免疫反应的方法，如增加吞噬作用，例如延长吞噬细胞（特别是角质细胞、中性粒细胞）的寿命。因此，所公开的化合物提供了治疗与机体免疫反应有关的疾病的方法。