1,7-萘啶-6-胺 | 5912-36-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 1,7-萘啶-6-胺
• 英文名称: 1,7-naphthyridin-6-amine
• CAS: 5912-36-7
• 化学式: C₈H₇N₃
• mdl: MFCD11521588
• 分子量: 145.164
• InChiKey: LYSLEXZCMQGSBJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  51.8
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 储存条件：
  存储条件：2-8℃，请置于干燥处并密封保存。

反应信息

• 作为反应物：
  描述：

  1,7-萘啶-6-胺 在 sodium nitrite 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 生成 N-(2-chloro-5-(1,7-naphthyridin-6-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide
  参考文献：
  名称：

  Phospshoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors: Discovery and Structure–Activity Relationships of a Series of Quinoline and Quinoxaline Derivatives

  摘要：

  The phosphoinositide 3-kinase (PI3K) family catalyzes the ATP-dependent phosphorylation of the 3'-hydroxyl group of phosphatidylinositols and plays an important role in cell growth and survival. There is abundant evidence demonstrating that PI3K signaling is dysregulated in many human cancers, suggesting that therapeutics targeting the PI3K pathway may have utility for the treatment of cancer. Our efforts to identify potent, efficacious, and orally available PI3K/mammalian target of rapamycin (mTOR) dual inhibitors resulted in the discovery of a series of substituted quinolines and quinoxalines derivatives. In this report, we describe the structure-activity relationships, selectivity, and pharmacokinetic data of this series and illustrate the in vivo pharmacodynamic and efficacy data for a representative compound.

  DOI：

  10.1021/jm200386s
• 作为产物：
  描述：

  3-溴甲基-2-氰基吡啶 在 palladium on activated charcoal 、 氢溴酸 、 氢气 、 potassium carbonate 、 溶剂黄146 、 potassium hydroxide 作用下， 以 乙醇 、 水 、 乙腈 为溶剂， 20.0~50.0 ℃ 、303.99 kPa 条件下， 反应 15.0h， 生成 1,7-萘啶-6-胺
  参考文献：
  名称：

  [EN] METHODS OF USE FOR PYRIMIDINES AS FERROPORTIN INHIBITORS
  [FR] MÉTHODES D'UTILISATION DE PYRIMIDINES EN TANT QU'INHIBITEURS DE LA FERROPORTINE

  摘要：

  本文描述的主题是针对化学式(I)的铁蛋白抑制剂化合物及其药用盐，制备这些化合物的方法，包含这些化合物的药物组合物，以及用于预防和/或治疗由于缺乏肝铁蛋白或铁代谢紊乱引起的疾病的方法，特别是铁超载状态，如地中海贫血、镰状细胞病和血色病，以及肾损伤。

  公开号：

  WO2021222483A1

文献信息

• [EN] NOVEL COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS
  申请人：MISSION THERAPEUTICS LTD

  公开号：WO2016046530A1

  公开（公告）日：2016-03-31

  The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.

  本发明涉及新型化合物和制备去泛素化酶（DUBs）抑制剂的方法。具体而言，本发明涉及抑制泛素C端水解酶L1（UCHL1）。本发明进一步涉及在癌症和其他适应症治疗中使用DUB抑制剂。本发明的化合物包括具有式（I）或其药用可接受盐的化合物，其中R1至R8如本文所定义。
• [EN] QUINAZOLINE DERIVATIVES<br/>[FR] DERIVES DE QUINAZOLINE
  申请人：ASTRAZENECA AB

  公开号：WO2006040520A1

  公开（公告）日：2006-04-20

  The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.

  这项发明涉及式(I)的喹唑啉衍生物或其药用盐、溶剂化合物或前药，其中X1、p、R1、q、R2、R3、R4、R5、环A、r和R6中的每一个在描述中已定义的含义中具有任何含义；它们的制备方法，含有它们的药物组合物以及它们在制造用于治疗细胞增殖紊乱或与血管生成和/或血管通透性相关的疾病状态的药物的用途。
• [EN] CYCLOALKYL PYRIMIDINES AS FERROPORTIN INHIBITORS<br/>[FR] PYRIMIDINES CYCLOALKYLIQUES UTILISÉES EN TANT QU'INHIBITEURS DE LA FERROPORTINE
  申请人：GLOBAL BLOOD THERAPEUTICS INC

  公开号：WO2021222363A1

  公开（公告）日：2021-11-04

  The subject matter described herein is directed to ferroportin inhibitor compounds of Formula I or I' and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.

  本文描述的主题涉及Formula I或I'的铁蛋白抑制剂化合物及其药用盐，制备这些化合物的方法，包含这些化合物的药物组合物，以及用于预防和/或治疗由于缺乏肝铁蛋白或铁代谢紊乱引起的疾病的方法，特别是铁过载状态，如地中海贫血、镰状细胞病和血色病，以及肾脏损伤。
• 3-(anilinomethylene) oxindoles
  申请人：Glaxo Wellcome Inc.

  公开号：US06350747B1

  公开（公告）日：2002-02-26

  The present invention relates generally to novel amine substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways in general, and in particular in the pathological processes which involve aberrant cellular proliferation, such as tumor growth. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of tumor-related angiogenesis.

  本发明一般涉及新型胺取代的噁二酮化合物和组合物。这些化合物和组合物作为药理学药剂在治疗由于一般蛋白激酶激活的信号通路的抑制或拮抗而减轻的疾病或症状方面具有实用性，特别是在涉及异常细胞增殖的病理过程中，如肿瘤生长。具体而言，本发明涉及一系列取代的噁二酮化合物，其表现出蛋白酪氨酸激酶和蛋白丝氨酸/苏氨酸激酶抑制作用，并且在通过抑制与肿瘤相关的血管生成抑制肿瘤生长方面是有用的。
• Design and synthesis of a novel series of 4-heteroarylamino-1′-azaspiro[oxazole-5,3′-bicyclo[2.2.2]octanes as α7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR
  作者：Christiana Iwuagwu、Dalton King、Ivar M. McDonald、James Cook、F. Christopher Zusi、Matthew D. Hill、Robert A. Mate、Haiquan Fang、Ronald Knox、Lizbeth Gallagher、Debra Post-Munson Amy Easton、Regina Miller、Yulia Benitex、Judy Siuciak、Nicholas Lodge、Robert Zaczek、Daniel Morgan、Linda Bristow、John E. Macor、Richard E. Olson

  DOI：10.1016/j.bmcl.2017.01.058

  日期：2017.3

  potent partial agonists of the α7 receptor, selective against other nicotinic receptors and the serotinergic 5HT3A receptor. (1'S,3'R,4'S)-N-(6-phenylpyrimidin-4-yl)-4H-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octan]-2-amine, a potent and selective α7 nAChR partial agonist, was demonstrated to improve cognition in the mouse novel object recognition (NOR) model of episodic memory.

  如该系列以前的报告所述，含奎尼丁的螺环恶唑啉已证明可作为α7烟碱乙酰胆碱受体（α7nAChR）部分激动剂使用。在这项工作中，该化学型的SAR被扩展为包括一系列的二嗪杂环取代。许多杂环类似物是α7受体的有效部分激动剂，对其他烟碱类受体和血清素5HT3A受体具有选择性。（1'S，3'R，4'S）-N-（6-苯基嘧啶-4-基）-4H-1'-氮杂螺[恶唑-5,3'-双环[2.2.2]正辛] -2-胺，a有效和选择性的α7nAChR部分激动剂，被证明可以改善情节记忆的小鼠新对象识别（NOR）模型中的认知。