8-cyclopropyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one

• 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: 8-cyclopropyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
• 英文别名: 8-cyclopropyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one；8-cyclopropyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one
• 化学式: C₁₉H₂₁N₇O
• 分子量: 363.422
• InChiKey: TUHDWYREOHGIHM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  86.3
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  盐酸 、 4-[6-(8-cyclopropyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)pyridin-3-yl]piperazine-1-carboxylic acid tert-butyl ester 在 二氯甲烷 、 8-cyclopropyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one 作用下， 以 二氯甲烷 为溶剂， 反应 18.0h， 以to give the desired product 8-cyclopropyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one as its hydrochloride salt (83 mg, 85%)的产率得到8-cyclopropyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
  参考文献：
  名称：

  2-(pyridin-2-ylamino)-pyrido [2,3-d]pyrimidin-7-ones

  摘要：

  本发明提供了可用于治疗细胞增殖性疾病的取代2-氨基吡啶。本发明的新型化合物是cyclin-dependent kinases 4 (cdk4)的有效抑制剂。

  公开号：

  US07208489B2
• 作为试剂：
  描述：

  盐酸 、 4-[6-(8-cyclopropyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)pyridin-3-yl]piperazine-1-carboxylic acid tert-butyl ester 在 二氯甲烷 、 8-cyclopropyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one 作用下， 以 二氯甲烷 为溶剂， 反应 18.0h， 以to give the desired product 8-cyclopropyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one as its hydrochloride salt (83 mg, 85%)的产率得到8-cyclopropyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
  参考文献：
  名称：

  2-(Pyridin-2-ylamino)-pyrido [2,3-D]pyrimidin-7-ones

  摘要：

  本发明提供了可用于治疗细胞增殖性疾病的取代的2-氨基吡啶。本发明的新型化合物是cyclin-dependent kinases 4 (cdk4)的强效抑制剂。

  公开号：

  US20050137214A1

文献信息

• 2-(Pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones
  申请人：——

  公开号：US20030149001A1

  公开（公告）日：2003-08-07

  The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (cdk4). 1

  这项发明提供了用于治疗细胞增殖性疾病的取代2-氨基吡啶。本发明的新化合物是cyclin-dependent激酶4 (cdk4)的有效抑制剂。
• 2-(PYRIDIN-2-YLAMINO)-PYRIDO [2,3 D]PYRIMIDIN-7-ONES
  申请人：Barvian Mark

  公开号：US20070179118A1

  公开（公告）日：2007-08-02

  The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (cdk4).

  本发明提供了替代2-氨基吡啶，用于治疗细胞增殖性疾病。本发明的新化合物是cyclin-dependent kinases 4 (cdk4)的有效抑制剂。
• 2-(PYRIDIN-2-YLAMINO)-PYRIDO 2,3-d]PYRIMIDIN-7-ONES
  申请人：Warner-Lambert Company LLC

  公开号：EP1470124B1

  公开（公告）日：2005-12-28
• Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, and/or a CDK 4/6 Inhibitor
  申请人：Acerta Pharma B.V.

  公开号：US20170224819A1

  公开（公告）日：2017-08-10

  Therapeutic combinations of a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the γ- and δ-isoforms and selective for both γ- and δ-isoforms (PI3K-γ,δ, PI3K-γ, and PI3K-δ, a Janus kinase-2 (JAK-2) inhibitor, a cyclin-dependent kinase-4/6 (CDK4/6) inhibitor, and/or a Bruton's tyrosine kinase (BTK) inhibitor are described. In certain embodiments, the invention includes therapeutic combinations of a cyclin-dependent kinase-4/6 (CDK4/6) inhibitor and a BTK inhibitor, a PI3K-δ inhibitor and a BTK inhibitor, a JAK-2 and a BTK inhibitor, and a JAK-2, PI3K-δ, and BTK inhibitor.
• Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, and/or a CDK4/6 Inhibitor
  申请人：Acerta Pharma B.V.

  公开号：US20180250400A1

  公开（公告）日：2018-09-06

  Therapeutic combinations of a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the γ- and δ-isoforms and selective for both γ- and δ-isoforms (PI3K-γ,δ, PI3K-γ, and PI3K-δ, a Janus kinase-2 (JAK-2) inhibitor, a cyclin-dependent kinase-4/6 (CDK4/6) inhibitor, and/or a Bruton's tyrosine kinase (BTK) inhibitor are described. In certain embodiments, the invention includes therapeutic combinations of a cyclin-dependent kinase-4/6 (CDK4/6) inhibitor and a BTK inhibitor, a PI3K-δ inhibitor and a BTK inhibitor, a JAK-2 and a BTK inhibitor, and a JAK-2, PI3K-δ, and BTK inhibitor.