1-(吡啶基-3-y甲基)哌啶基-4-胺 | 160357-88-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 1-(吡啶基-3-y甲基)哌啶基-4-胺
• 中文别名: 1-(吡啶基-3-Y甲基)哌啶基-4-胺
• 英文名称: 1-(pyridin-3-ylmethyl)piperidin-4-amine
• 英文别名: 4-amino-1-(pyridin-3-ylmethyl)piperidine；1-(3-pyridylmethyl)-4-aminopiperidine；4-amino-N-(pyridin-3-ylmethyl)piperidine；4-amino-1-(3-pyridinylmethyl)piperidine；4-amino-1-(3-pyridylmethyl)piperidine；4-amino-N-(3-pyridylmethyl)piperidine
• CAS: 160357-88-0
• 化学式: C₁₁H₁₇N₃
• mdl: MFCD08059920
• 分子量: 191.276
• InChiKey: MSXJQLZTWITCEC-UHFFFAOYSA-N

物化性质

• 沸点：
  305.0±37.0 °C(Predicted)
• 密度：
  1.082±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.545
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 危险等级：
  IRRITANT
• 危险品标志：
  Xi
• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  1-(吡啶基-3-y甲基)哌啶基-4-胺 、 3-氯丙炔 在 碳酸氢钠 作用下， 以 乙醇 为溶剂， 反应 3.0h， 以32%的产率得到
  参考文献：
  名称：

  Design and synthesis of novel triazolo-lapatinib hybrids as inhibitors of breast cancer cells

  摘要：

  A series of triazolo-lapatinib hybrids were synthesized via copper (II)-oxide nanoparticle (Cu2O-NP)-catalyzed azide-alkyne cycloaddition. The ability of these compounds to reduce the viability of breast cancer SKBR3 and SUM159 cells and stem cell-like KG-1a leukemia cells was subsequently evaluated. Compared with lapatinib, compounds 6c-f were more potent than lapatinib against the three cell lines. Next, the toxicity of compounds 6c-f was assessed in zebrafish. Compound 6d had comparable toxicity with lapatinib at 200M (mortality rate=10 vs. 10%), and compound 6e had lower toxicity than lapatinib at 200M (mortality rate=0 vs. 10%). Thus, compound 6e is a promising lead compound worthy of further investigation.[GRAPHICS].

  DOI：

  10.1007/s00044-018-2247-0
• 作为产物：
  描述：

  2,2,2-trifluoro-N-[1-(3-pyridylmethyl)4-piperidyl]acetamide 在 sodium borohydrid 作用下， 以 1,4-二氧六环 、 乙醇 、 水 为溶剂， 以11.2 g (88%)的产率得到1-(吡啶基-3-y甲基)哌啶基-4-胺
  参考文献：
  名称：

  4-(biphenylcarbonylamino)piperidine derivatives as mtp inhibitors

  摘要：

  本发明涉及式(I)的化合物：其中：Z代表二苯基，可选地在2'、3'、4'、5'和6'位上用三卤甲基和三卤甲氧基中的一种或多种取代基取代；Het代表喹啉基、喹喔啉基或吡啶基，可选地用卤素、氰基、硝基、(C1-C6)烷基、(C6-C12)芳基、(C1-C6)烷氧基、羟基、(C1-C6)硫代烷氧基、羧基和(C1-C6)烷氧羰基中的一种或多种取代基取代，或其药学上可接受的盐。这些化合物可用作微粒体三酸甘油酯转移蛋白的抑制剂和B载脂蛋白分泌的抑制剂。

  公开号：

  US20040034028A1

文献信息

• 6-(4-Hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
  申请人：SANOFI

  公开号：US20130150340A1

  公开（公告）日：2013-06-13

  The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, in which R 1 , R 2 , R 3 and R 4 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的1H-吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3和R4如下所示。式I的化合物是激酶抑制剂，对于治疗与糖尿病及糖尿病并发症相关的疾病，如糖尿病肾病、糖尿病神经病变和糖尿病视网膜病变等，具有用处。此外，本发明还涉及将式I的化合物用作药物中的活性成分，以及包含它们的药物组合物。
• [EN] 6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS D'AMIDE DE L'ACIDE 6-(4-HYDROXY-PHÉNYL)-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIQUE EN TANT QU'INHIBITEURS DE KINASES
  申请人：SANOFI SA

  公开号：WO2013060636A1

  公开（公告）日：2013-05-02

  The present invention relates to 1 H-pyrazolo[3,4-b]pyridine compounds of the formula (I) in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are protein kinase C (PKC) inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式(I)的1H-吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3和R4的定义如下所示。式I的化合物是蛋白激酶C（PKC）抑制剂，对于治疗与糖尿病及糖尿病并发症相关的疾病，如糖尿病肾病、糖尿病神经病变和糖尿病视网膜病变等，具有益处。此外，本发明还涉及利用该式化合物，特别是作为药物中的活性成分以及包含它们的药物组合物。
• [EN] 2-PHENYL-3H-IMIDAZO[4,5-B]PYRIDINE DERIVATES USEFUL AS INHIBITORS OF MAMMALIAN TYROSINE KINASE ROR1 ACTIVITY<br/>[FR] DÉRIVÉS DE 2-PHÉNYL-3H-IMIDAZO[4,5-B]PYRIDINE UTILISÉS COMME INHIBITEURS DE L'ACTIVITÉ DE LA TYROSINE KINASE DE MAMMIFÈRE ROR1
  申请人：KANCERA AB

  公开号：WO2016124553A1

  公开（公告）日：2016-08-11

  A compound of formula (I´) or (I´´) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of mammalian kinase enzyme activity, including ROR1 tyrosine kinase activity and may be used in the treatment of disorders associated with such activity.

  化合物的化学式（I´）或（I´´）或其药学上可接受的盐。该化合物是哺乳动物激酶酶活性的抑制剂，包括ROR1酪氨酸激酶活性，并可用于治疗与该活性相关的疾病。
• 4-Piperidinealkanamine derivatives
  申请人：FABRICA ESPANOLA DE PRODUCTOS QUIMICOS Y FARMACEUTICOS, S.A.

  公开号：EP0343307A1

  公开（公告）日：1989-11-29

  Compounds of general formula I (Z=O) are prepared by react­ing 4-piperidinealkanamines with carboxylic acids or reactive der­ivatives thereof, such as the esters of lower aliphatic alcohols or acid halides. Compounds of general formula I (Z=CONH) are likewise obtained by means of the reaction between 4-piperidinealcan­amines and isocyanates. The compounds of general formula I thus obtained, and the pharmaceutically acceptable salts thereof are of a great therapeutic utility, given their activity as specific antagonists of histamine H₁ receptors.

  通式I（Z=O）的化合物是通过将4-哌啶烷基胺与羧酸或其反应衍生物（如低碳醇酯或酸卤化物）反应制备而成的。通式I（Z=CONH）的化合物同样是通过4-哌啶烷胺和异氰酸酯之间的反应获得的。这样获得的通式I的化合物及其药用可接受的盐在治疗上具有极大的用途，因为它们作为组织胺H₁受体的特异拮抗剂而具有活性。
• [EN] INHIBITORS OF SARM1<br/>[FR] INHIBITEURS DE SARM1
  申请人：DISARM THERAPEUTICS INC

  公开号：WO2021050913A1

  公开（公告）日：2021-03-18

  The present disclosure provides compounds and methods useful for inhibiting SARM1 and/or treating and/or preventing axonal degeneration.

  本公开提供了化合物和方法，用于抑制SARM1和/或治疗和/或预防轴突退化。