3-methyl-6-[1-(6-methyl-2-pyridinyl)-1H-pyrazol-5-yl]-4(3H)-quinazolinone | 1378524-25-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-methyl-6-[1-(6-methyl-2-pyridinyl)-1H-pyrazol-5-yl]-4(3H)-quinazolinone
• 英文别名: PF-03671148；3-methyl-6-[2-(6-methylpyridin-2-yl)pyrazol-3-yl]quinazolin-4-one
• CAS: 1378524-25-4
• 化学式: C₁₈H₁₅N₅O
• 分子量: 317.35
• InChiKey: OWIYYKSTVQMPLM-UHFFFAOYSA-N

物化性质

• 沸点：
  567.6±60.0 °C(Predicted)
• 密度：
  1.32±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  63.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  3-methyl-4-oxo-3,4-dihydroquinazoline-6-carboxylic acid 在 N,N'-羰基二咪唑 作用下， 以 四氢呋喃 、 溶剂黄146 、 N,N-二甲基甲酰胺 为溶剂， 反应 5.0h， 生成 3-methyl-6-[1-(6-methyl-2-pyridinyl)-1H-pyrazol-5-yl]-4(3H)-quinazolinone 、
  参考文献：
  名称：

  Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring

  摘要：

  A series of 2-(1H-pyrazol-1-yl)pyridines are described as inhibitors of ALK5 (TGF beta receptor I kinase). Modeling compounds in the ALK5 kinase domain enabled some optimization of potency via substitutions on the pyrazole core. One of these compounds PF-03671148 gave a dose dependent reduction in TGF beta induced fibrotic gene expression in human fibroblasts. A similar reduction in fibrotic gene expression was observed when PF-03671148 was applied topically in a rat wound repair model. Thus these compounds have potential utility for the prevention of dermal scarring. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.04.013

文献信息

• 1,5-DIHYDRO-2H-PYRROL-2-ONE COMPOUNDS AND METHODS OF USING SAME
  申请人：Frequency Therapeutics, Inc.

  公开号：US20180214458A1

  公开（公告）日：2018-08-02

  The present invention relates to 1,5-dihydro-2H-pyrrol-2-one compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.

  本发明涉及1,5-二氢-2H-吡咯-2-酮化合物及其使用方法，用于诱导干/祖细胞支持细胞的自我更新，包括诱导干/祖细胞增殖同时保持子细胞中分化为组织细胞的能力。
• 1,2-DIHYDRO-3H-PYRAZOL-3-ONE COMPOUNDS AND METHODS OF USING SAME
  申请人：Frequency Therapeutics, Inc.

  公开号：US20200316089A1

  公开（公告）日：2020-10-08

  The present disclosure relates to 1,2-dihydro-3H-pyrazol-3-one compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.

  本公开涉及1,2-二氢-3H-吡唑-3-酮化合物及其使用方法，用于诱导干/祖细胞支持细胞的自我更新，包括诱导干/祖细胞增殖，同时维持子细胞中分化成组织细胞的能力。
• 1,5-dihydro-2H-pyrrol-2-one compounds and methods of using same
  申请人：Frequency Therapeutics, Inc.

  公开号：US10383881B2

  公开（公告）日：2019-08-20

  The present invention relates to 1,5-dihydro-2H-pyrrol-2-one compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.

  本发明涉及1,5-二氢-2H-吡咯-2-酮化合物以及使用它们诱导干/祖支持细胞自我更新的方法，包括诱导干/祖细胞增殖，同时保持子细胞分化成组织细胞的能力。
• 1H-pyrrole-2,5-dione compounds and methods of using same
  申请人：Frequency Therapeutics, Inc.

  公开号：US11066419B2

  公开（公告）日：2021-07-20

  The present invention relates to 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.

  本发明涉及 1H-吡咯-2,5-二酮化合物和使用它们诱导干/祖支持细胞自我更新的方法，包括诱导干/祖细胞增殖，同时保持子细胞分化成组织细胞的能力。
• METHODS FOR CONTROLLED PROLIFERATION OF VESTIBULAR STEM CELLS / GENERATING INNER EAR HAIR CELLS USING WNT AND TGF-BETA INHIBITION
  申请人：Frequency Therapeutics, Inc.

  公开号：EP3423069A2

  公开（公告）日：2019-01-09