3-(piperidin-1-yl)pyridin-4-amine | 144864-26-6

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 3-(piperidin-1-yl)pyridin-4-amine
• 英文别名: 3-piperidin-1-ylpyridin-4-amine
• CAS: 144864-26-6
• 化学式: C₁₀H₁₅N₃
• mdl: MFCD20700896
• 分子量: 177.249
• InChiKey: BKWUVVNRSKZZNU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(piperidin-1-yl)pyridin-4-amine 在 硫酸 、 硝酸 作用下， 反应 3.5h， 以12%的产率得到5-nitro-1,2,3,4-tetrahydropyrido<1',2':1,2>imidazo<5,4-c>pyridine
  参考文献：
  名称：

  New Cyclization Reactions of 3-Dialkylamino-4-aminopyridines under Conditions of Nitration

  摘要：

  Treatment of 3-dialkylamino-4-aminopyridines (1) with nitric and sulfuric acids affords imidazo[4,5-c]pyridine derivatives (2, 3 and 4) and 1,2,3-triazolo[4,5-c]pyridine 2-oxides (5) by cyclization reaction of the corresponding 4-nitroaminopyridines.

  DOI：

  10.3987/com-92-6045
• 作为产物：
  描述：

  3-溴-4-硝基吡啶-N-氧化物 在 palladium 10% on activated carbon 、 氢气 作用下， 以 乙醇 为溶剂， 反应 127.0h， 生成 3-(piperidin-1-yl)pyridin-4-amine
  参考文献：
  名称：

  Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors

  摘要：

  Proviral insertion of Moloney virus (PIM) 1, 2, and 3 kinases are serine/threonine kinases that normally function in survival and proliferation of hematopoietic cells. As high expression of PIM1, 2, and 3 is frequently observed in many human malignancies, including multiple myeloma, non Hodgkins lymphoma, and myeloid leukemias, there is interest in determining whether selective PIM1 inhibition can improve outcomes of these human cancers. Herein, we describe our efforts toward this goal. The structure guided optimization of a singleton high throughput screening hit in which the potency against all three PIM isoforms was increased >10,000 fold to yield compounds with pan PIM K(i)s < 10 pM, nanomolar cellular potency, and in vivo activity in an acute myeloid leukemia Pun dependent tumor model is described.

  DOI：

  10.1021/ml400307j

文献信息

• [EN] SMALL MOLECULE AGONISTS OF MUCOLIPIN 1 AND USES THEREOF<br/>[FR] PETITES MOLÉCULES AGONISTES DE LA MUCOLIPINE 1 ET LEURS UTILISATIONS
  申请人：UNIV MICHIGAN REGENTS

  公开号：WO2021041866A1

  公开（公告）日：2021-03-04

  This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a phenyl-sulfonic amide (or similar) structure which function as agonists of mucolipin 1 (ML1), and their use as therapeutics for the treatment of Duchenne muscular dystrophy (DMD) and related disorders.

  这项发明属于药物化学领域。特别是，该发明涉及一类新的小分子，具有苯磺酰胺（或类似）结构，作为肌球脂蛋白1（ML1）的激动剂，以及它们作为治疗杜氏肌肉萎缩症（DMD）和相关疾病的疗法的用途。
• PIM KINASE INHIBITORS AND METHODS OF THEIR USE
  申请人：Burger Matthew

  公开号：US20120208815A1

  公开（公告）日：2012-08-16

  New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

  提供了一种用于抑制人或动物主体中与肿瘤发生相关的激酶活性的新化合物、组合物和方法。在某些实施例中，这些化合物和组合物能够有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。这些新的化合物和组合物可以单独使用或与至少一种额外的药物联合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的疾病，如癌症。
• PIM kinase inhibitors and methods of their use
  申请人：Burger Matthew

  公开号：US08822497B2

  公开（公告）日：2014-09-02

  New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

  本发明提供了一种用于抑制与人或动物主体中肿瘤发生相关的激酶活性的新化合物、组合物和方法。在某些实施例中，这些化合物和组合物能够有效抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。这些新的化合物和组合物可以单独使用或与至少一种其他药物联合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的疾病，例如癌症。
• WO2008/106692
  申请人：——

  公开号：——

  公开（公告）日：——
• US8822497B2
  申请人：——

  公开号：US8822497B2

  公开（公告）日：2014-09-02