6-甲基-1,5-萘啶-2(1H)-酮 | 764717-60-4

• 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: 6-甲基-1,5-萘啶-2(1H)-酮
• 英文名称: 6-methyl-1H-[1,5]naphthyridin-2-one
• 英文别名: 6-Methyl-1H-[1,5]naphthyridin-2-on；6-methyl-1,5-naphthyridin-2(1H)-one；6-methyl-1H-1,5-naphthyridin-2-one
• CAS: 764717-60-4
• 化学式: C₉H₈N₂O
• mdl: MFCD09038142
• 分子量: 160.175
• InChiKey: VVEGURRPTDBLHJ-UHFFFAOYSA-N

物化性质

• 熔点：
  260 °C
• 沸点：
  369.5±42.0 °C(Predicted)
• 密度：
  1.217±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.111
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  6-甲基-1,5-萘啶-2(1H)-酮 在 氢氧化钾 、 钯 、 三氯氧磷 作用下， 生成 2-甲基-1,5-萘啶
  参考文献：
  名称：

  Miyaki, Yakugaku Zasshi/Journal of the Pharmaceutical Society of Japan, 1942, vol. 62, p. 257,265; dtsch. Ref. S. 66

  摘要：

  DOI：
• 作为产物：
  描述：

  5-amino-2-hydroxypyridine 在 盐酸 、 乙醛 作用下， 生成 6-甲基-1,5-萘啶-2(1H)-酮
  参考文献：
  名称：

  249. 1：5-萘啶的某些衍生物

  摘要：

  DOI：

  10.1039/jr9490001157

文献信息

• SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME
  申请人：BlinkBio, Inc.

  公开号：US20170202970A1

  公开（公告）日：2017-07-20

  Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.

  本文描述了基于硅的共轭物，能够将一个或多个有效载荷基团传递到靶细胞或组织。考虑到的共轭物可能包括一个硅-杂原子核心，一个或多个可选的催化基团，一个定位基团，允许共轭物在靶细胞或组织内积累，一个或多个有效载荷基团（例如，治疗剂或成像剂），以及与硅-杂原子核心共价结合的两个或更多个不干扰基团。
• Identification of 1,5-Naphthyridine Derivatives as a Novel Series of Potent and Selective TGF-β Type I Receptor Inhibitors
  作者：Françoise Gellibert、James Woolven、Marie-Hélène Fouchet、Neil Mathews、Helen Goodland、Victoria Lovegrove、Alain Laroze、Van-Loc Nguyen、Stéphane Sautet、Ruolan Wang、Cheryl Janson、Ward Smith、Gaël Krysa、Valérie Boullay、Anne-Charlotte de Gouville、Stéphane Huet、David Hartley

  DOI：10.1021/jm0400247

  日期：2004.8.1

  Optimization of the screening hit 1 led to the identification of novel 1,5-naphthyridine aminothiazole and pyrazole derivatives, which are potent and selective inhibitors of the transforming growth factor-beta type I receptor, ALK5. Compounds 15 and 19, which inhibited ALK5 autophosphorylation with IC50 = 6 and 4 nM, respectively, showed potent activities in both binding and cellular assays and exhibited

  筛选命中1的优化导致鉴定了新型1,5-萘啶氨基噻唑和吡唑衍生物，它们是转化生长因子βI型受体ALK5的有效抑制剂。分别以IC50 = 6和4 nM抑制ALK5自磷酸化的化合物15和19在结合和细胞分析中均显示出强大的活性，并显示出超过p38促分裂原活化蛋白激酶的选择性。描述了与人ALK5结合的19的X射线晶体结构，证实了对接研究提出的结合模式。
• Bicyclic aromatic substituted pyridone derivative
  申请人：Sakuraba Shunji

  公开号：US20090264426A1

  公开（公告）日：2009-10-22

  Disclosed is a compound represented by the formula (I): Wherein R 1 and R 2 independently represent a hydrogen atom, a lower alkyl group or the like; X 1 , X 2 and X 3 independently represent a methine group or a nitrogen atom; Y 1 and Y 3 independently represent a single bond, —O— or the like; Y 2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z 1 and Z 2 independently represent a single bond, a C 1-4 alkylene group or the like; Ar 1 represents an aromatic carbocyclic ring or the like; and Ar 2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.

  本发明揭示了一种化合物，其化学式为（I）：其中R1和R2分别代表氢原子、低碳烷基或类似物；X1、X2和X3分别代表亚甲基基团或氮原子；Y1和Y3分别代表单键、—O—或类似物；Y2代表低碳烷基基团或类似物；W1至W4独立地代表单键、亚甲基基团或类似物；L代表单键、亚甲基基团或类似物；Z1和Z2独立地代表单键、C1-4烷基基团或类似物；Ar1代表芳香环烷基环或类似物；Ar2代表双环芳香环烷基环或类似物。该化合物可用作治疗中枢疾病、心血管疾病或代谢性疾病的药物。
• BICYCLIC AROMATIC SUBSTITUTED PYRIDONE DERIVATIVE
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP1939194A1

  公开（公告）日：2008-07-02

  Disclosed is a compound represented by the formula (I): Wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like; X1 , X2 and X3 independently represent a methine group or a nitrogen atom; Y1 and Y3 independently represent a single bond, -O- or the like; Y2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z1 and Z2 independently represent a single bond, a C1-4 alkylene group or the like; Ar1 represents an aromatic carbocyclic ring or the like; and Ar2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.

  本发明公开了一种由式 (I) 表示的化合物： 其中 R1 和 R2 独立地代表氢原子、低级烷基或类似物；X1、X2 和 X3 独立地代表甲基或氮原子；Y1 和 Y3 独立地代表单键、-O- 或类似物；Y2 代表低级亚烷基或类似物；W1 至 W4 独立地代表单键、亚甲基或类似物；L 代表单键、亚甲基或类似物；Z1 和 Z2 独立地代表单键、C1-4 亚烷基或类似物；Ar1 代表芳香碳环或类似物；Ar2 代表双环芳香碳环或类似物。该化合物可用作治疗中枢疾病、心血管疾病或代谢疾病的药物。
• DE507637
  申请人：——

  公开号：——

  公开（公告）日：——