3,4-二氨基-2-羟基吡啶 | 33631-02-6

• 物质功能分类: 医药中间体 - 吡啶类化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 3,4-二氨基-2-羟基吡啶
• 英文名称: 3,4-Diamino-2-hydroxypyridin
• 英文别名: 3,4-diamino-pyridin-2-ol；3,4-diamino-2-hydroxypyridine；3,4-Diaminopyridin-2-ol；3,4-diamino-1H-pyridin-2-one
• CAS: 33631-02-6
• 化学式: C₅H₇N₃O
• 分子量: 125.13
• InChiKey: BHTKBUHNIZPKSG-UHFFFAOYSA-N

物化性质

• 沸点：
  291.1±40.0 °C(Predicted)
• 密度：
  1.294±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  81.1
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• 危险品标志：
  Xi
• 海关编码：
  2933399090
• 危险性防范说明：
  P280,P305+P351+P338,P310
• 危险性描述：
  H302,H315,H319,H332,H335

反应信息

• 作为反应物：
  描述：

  3,4-二氨基-2-羟基吡啶 在 乙醇 、 钯 、 三氯氧磷 作用下， 生成 1H-咪唑[4,5-C]吡啶
  参考文献：
  名称：

  Salemink; van der Want, Recueil des Travaux Chimiques des Pays-Bas, 1949, vol. 68, p. 1013,1024

  摘要：

  DOI：
• 作为产物：
  描述：

  4-氨基-3-硝基吡啶 在 sodium sulfide 、 水 作用下， 生成 3,4-二氨基-2-羟基吡啶
  参考文献：
  名称：

  Salemink; van der Want, Recueil des Travaux Chimiques des Pays-Bas, 1949, vol. 68, p. 1013,1024

  摘要：

  DOI：

文献信息

• New substituted imidazo-pyridinones and imidazo-pyridazinones, the preparation thereof and their use as pharmaceutical compositions
  申请人：Hauel Norbert

  公开号：US20050020574A1

  公开（公告）日：2005-01-27

  The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein R 1 to R 4 are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

  本发明涉及通式所示的取代咪唑吡啶酮和咪唑吡啶酮，其中R1至R4如权利要求书中所定义，它们的互变异构体、立体异构体、混合物及其盐，具有有价值的药理特性，特别是对酶二肽基肽酶-IV（DPP-IV）活性的抑制作用。
• [EN] 3,4-DISUBSTITUTED PYRAZOLES AS CYCLIN DEPENDENT KINASES (CDK) OR AURORA KINASE OR GLYCOGEN SYNTHASE 3 (GSK-3) INHIBITORS<br/>[FR] PYRAZOLES 3,4-DISUBSTITUTES SERVANT D'INHIBITEURS DE KINASES CYCLINES DEPENDANTES (CDK), OU DE KINASES AURORA OU DE GLYCOGENE SYNTASES 3 (GSK-3)
  申请人：ASTEX TECHNOLOGY LTD

  公开号：WO2006003440A1

  公开（公告）日：2006-01-12

  The invention provides compounds of the formula (I); or salts or solvates or N-oxides thereof; wherein: Rq is selected from groups (a), (b) and (c); the asterisk denoting the point of attachment to the pyrazole ring; X is N or CR5; X' is NR4', O, S or S(O); A is a bond or -(CH2)m-(B)n-; B is C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R0 is hydrogen or, together with NRg when present, forms a group -(CH2)p- wherein p is 2 to 4; and R1 to R6b are as defined in the description. Compounds of the formula (I) have activity as inhibitors of CDK, aurora and GSK-3 kinases are useful in treating or preventing diseases such as cancers that are mediated by the said kinases.

  本发明提供式(I)的化合物；或其盐、溶剂化物或N-氧化物；其中：Rq选自基团(a)、(b)和(c)；星号表示与吡唑环的连接点；X为N或CR5；X'为NR4'、O、S或S(O)；A为键或-(CH2)m-(B)n-；B为C=O、NRg(C=O)或O(C=O)，其中Rg为氢或C1-4烃基，可选择性地被羟基或C1-4烷氧基取代；m为0、1或2；n为0或1；R0为氢，或与存在的NRg一起形成基团-( )p-，其中p为2至4；R1至R6b如说明书中所定义。式(I)的化合物作为CDK、aurora和GSK-3激酶的抑制剂，对于治疗或预防由所述激酶介导的疾病，如癌症，具有用途。
• 3,4-Disubstituted Pyrazoles as Cyclin Dependent Kinases (Cdk) or Aurora Kinase or Glycogen Synthase 3 (Gsk-3) Inhibitors
  申请人：Gill Liam Adrian

  公开号：US20080004270A1

  公开（公告）日：2008-01-03

  The invention provides compounds of the formula (I); or salts or solvates or N-oxides thereof; wherein: R q is selected from groups (a), (b) and (c); the asterisk denoting the point of attachment to the pyrazole ring; X is N or CR 5 ; X″ is NR 4 ; O, S or S(O); A is a bond or —(CH 2 ) m —(B) n —; B is C═O, NR g (C═O) or O(C═O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R 0 is hydrogen or, together with NR g when present, forms a group —(CH 2 ) p — wherein p is 2 to 4; and R 1 to R 6b are as defined in the description. Compounds of the formula (I) have activity as inhibitors of CDK, aurora and GSK-3 kinases are useful in treating or preventing diseases such as cancers that are mediated by the said kinases.

  本发明提供了式（I）的化合物；或其盐、溶剂或N-氧化物；其中：Rq选择自组（a）、（b）和（c）；星号表示与吡唑环的连接点；X为N或CR5；X″为NR4；O、S或S（O）；A为键或—（CH2）m—（B）n—；B为C═O、NRg（C═O）或O（C═O），其中Rg为氢或C1-4烃基，可选地被羟基或C1-4烷氧基取代；m为0、1或2；n为0或1；R0为氢或与NRg一起，形成—（ ）p—基团，其中p为2至4；R1至R6如描述中所定义。式（I）的化合物具有作为CDK、极光激酶和GSK-3激酶抑制剂的活性，可用于治疗或预防由该激酶介导的癌症等疾病。
• AMIDES AS PIM INHIBITORS
  申请人：AMGEN INC.

  公开号：US20150329538A1

  公开（公告）日：2015-11-19

  The invention relates to amide-containing compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

  本发明涉及公式（1）的含酰胺化合物及其盐。在某些实施例中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。在更进一步的实施例中，本发明涉及包含所述化合物的药物组合物，以及它们在预防和治疗与Pim激酶相关的疾病和病症，尤其是癌症方面的用途。
• Amides as pim inhibitors
  申请人：AMGEN INC.

  公开号：US09394297B2

  公开（公告）日：2016-07-19

  The invention relates to amide-containing compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

  本发明涉及式（1）的含酰胺化合物及其盐。在某些实施方式中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。在更进一步的实施方式中，本发明涉及包含所披露的化合物的制药组合物，以及它们在预防和治疗Pim激酶相关疾病和病症，尤其是癌症方面的用途。