2-chloro-N-(5-methyl-1H-pyrazol-3-yl)pyrido[2,3-d]pyrimidine-4-amine | 896464-11-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 2-chloro-N-(5-methyl-1H-pyrazol-3-yl)pyrido[2,3-d]pyrimidine-4-amine
• 英文别名: 2-chloro-N-(3-methyl-1H-pyrazol-5-yl)pyrido[2,3-d]pyrimidine-4-amine；2-chloro-N-(5-methyl-1H-pyrazol-3-yl)pyrido[2,3-d]pyrimidin-4-amine
• CAS: 896464-11-2
• 化学式: C₁₁H₉ClN₆
• 分子量: 260.686
• InChiKey: BTGPJJGXNJEUGB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  79.4
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-chloro-N-(5-methyl-1H-pyrazol-3-yl)pyrido[2,3-d]pyrimidine-4-amine 在 盐酸 作用下， 以 1,4-二氧六环 、 正丁醇 为溶剂， 反应 5.75h， 生成 3-((3-exo)-3-((4-((5-methyl-1H-pyrazol-3-yl)amino)pyrido[2,3-d]pyrimidin-2-yl)amino)-8-azabicyclo[3.2.1]oct-8-yl)propionitrile
  参考文献：
  名称：

  EP3889152

  摘要：

  公开号：
• 作为产物：
  描述：

  2,4-二氯吡咯并[2,3-D]嘧啶 、 3-氨基-5-甲基吡唑 在 三乙胺 、 N,N-二异丙基乙胺 作用下， 以 乙醇 为溶剂， 反应 13.5h， 以71%的产率得到2-chloro-N-(5-methyl-1H-pyrazol-3-yl)pyrido[2,3-d]pyrimidine-4-amine
  参考文献：
  名称：

  EP3889152

  摘要：

  公开号：

文献信息

• Pyrazole compounds useful as protein kinase inhibitors
  申请人：Bebbington David

  公开号：US20070270444A1

  公开（公告）日：2007-11-22

  This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R x and R y are independently selected from T-R 3 , or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R 2 , R 2′ , T, and R 3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

  该发明描述了式IV的新型吡唑化合物： 其中环D为从芳基，杂芳基，杂环基或碳环基中选择的5-7成员单环或8-10成员双环；Rx和Ry独立地选择自T-R3，或者与它们之间的原子结合形成融合的、不饱和的或部分不饱和的、具有1-3个环杂原子的5-8成员环；而R2，R2'，T和R3如说明书所述。这些化合物可用作蛋白激酶抑制剂，特别是作为aurora-2和GSK-3的抑制剂，用于治疗癌症、糖尿病和阿尔茨海默病等疾病。
• HETEROAROMATIC DERIVATIVES USEFUL AS ANTICANCER AGENTS
  申请人：Bhattacharya Samit Kumar

  公开号：US20090281073A1

  公开（公告）日：2009-11-12

  This invention relates to compounds of Formula (I), and to pharmaceutically acceptable salts and solvates thereof, wherein Z, W, X, Y, V, R 1 , R 2 , and R 3 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula (I) and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula (I). The invention also relates to methods of preparing the compounds of Formula (I).

  本发明涉及公式(I)的化合物，以及其药学上可接受的盐和溶剂化物，其中Z，W，X，Y，V，R1，R2和R3的定义如本文所述。该发明还涉及通过给予公式(I)的化合物来治疗哺乳动物中的异常细胞生长的方法，以及含有公式(I)的化合物用于治疗这种疾病的药物组合物。该发明还涉及制备公式(I)的化合物的方法。
• TRIAZOLE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
  申请人：Bebbington David

  公开号：US20120071657A1

  公开（公告）日：2012-03-22

  This invention describes novel triazole compounds of formula IX: wherein Z 1 is nitrogen or CR 9 and Z 2 is nitrogen or CH, provided that at least one of Z 1 and Z 2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R 1 ; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R x and R y are independently selected from T-R 3 , or R x and R y are taken together with their intervening atoms to form a fused ring; R 1 , R 3 , and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.

  该发明描述了式IX的新型三唑类化合物：其中Z1是氮或CR9，Z2是氮或CH，但至少其中一个为氮；G是环C或环D；环C选自苯基、吡啶基、嘧啶基、吡嗪基、吡咯基或1,2,4-三嗪基环，其中所述的环C具有一个或两个独立选择自-R1的邻位取代基；环D是选自芳基、杂芳基、杂环基或碳环基的5-7成员单环或8-10成员双环环；Rx和Ry独立选择自T-R3，或Rx和Ry与它们之间的原子结合形成螺合环；R1、R3和T如说明书所述。该化合物可用作蛋白激酶抑制剂，特别是GSK-3和Aurora的抑制剂，用于治疗糖尿病、癌症和阿尔茨海默病等疾病。
• PYRAZOLE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
  申请人：Bebbington David

  公开号：US20100256170A1

  公开（公告）日：2010-10-07

  This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R x and R y are independently selected from T-R 3 , or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R 2 , R 2′ , T, and R 3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

  本发明描述了式IV的新型吡唑化合物：其中环D为5-7成员单环或8-10成员双环，选自芳基，杂芳基，杂环基或碳环基；Rx和Ry分别选自T-R3，或与其之间的原子结合形成融合的、不饱和或部分不饱和的5-8成员环，其中有1-3个选自氧、硫或氮的环杂原子；R2、R2'、T和R3如说明书所述。这些化合物可用作蛋白激酶抑制剂，特别是aurora-2和GSK-3的抑制剂，用于治疗癌症、糖尿病和阿尔茨海默病等疾病。
• HETEROAROMATIC DERIVATIVES FOR USE AS REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
  申请人：Jiangsu Hansoh Pharmaceutical Group Co., Ltd.

  公开号：EP3889152A1

  公开（公告）日：2021-10-06

  The present invention relates to heteroaromatic derivatives for use as a regulator, a preparation method therefor and a use thereof. In particular, disclosed are compounds represented by general formula (I), preparation methods therefor, pharmaceutical compositions comprising said compounds, and a use thereof as Janus kinase inhibitors in treating inflammatory diseases and tumor-related diseases.

  本发明涉及用作调节剂的杂芳香族衍生物、其制备方法及其用途。特别是，本发明公开了通式（I）代表的化合物、其制备方法、包含所述化合物的药物组合物，以及其作为 Janus 激酶抑制剂在治疗炎症性疾病和肿瘤相关疾病中的用途。