4-Hydroxy-6-benzylpyrimidin | 16353-08-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4-Hydroxy-6-benzylpyrimidin
• 英文别名: 6-benzylpyrimidin-4-ol；6-benzyl-4-hydroxypyrimidine；6-Benzylpyrimidin-4-ol；4-benzyl-1H-pyrimidin-6-one
• CAS: 16353-08-5
• 化学式: C₁₁H₁₀N₂O
• mdl: MFCD16652724
• 分子量: 186.213
• InChiKey: JCPZGLWRQNPRGS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  41.5
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• Methods for inhibiting the transmission of HIV using topically applied substituted 6-benzyl-4-oxopyrimidines
  申请人：——

  公开号：US20030008887A1

  公开（公告）日：2003-01-09

  A method for inhibiting sexual transmission of HIV comprising topically applying to the skin or epithelial tissue of a human a composition comprising a non-nucleoside reverse transcriptase inhibitor (“NNRTI”) that is able to inhibit viral replication for periods exceeding 12, 24, or even 36 days, at concentrations below even 10 &mgr;M. In one embodiment the NNRTI is a dihydro-alkyloxy-benzyl-oxopyrimidine (DABO).

  一种抑制HIV性传播的方法，包括将一种含有非核苷类反转录酶抑制剂（“NNRTI”）的组合物局部涂抹于人体的皮肤或上皮组织上，该NNRTI能够在浓度低于10 &mgr;M的情况下抑制病毒复制，持续时间超过12、24或36天。在一种实施方式中，NNRTI是一种二氢烷氧基苯基嘧啶（DABO）。
• Beta-L-2'-deoxynucleosides for the treatment of resistant HBV strains and combination therapies
  申请人：Standring David

  公开号：US20050080034A1

  公开（公告）日：2005-04-14

  It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.

  已经发现β-L-2'-脱氧核苷可以对具有突变的耐药性乙型肝炎病毒产生活性。提供了一种治疗宿主中拉米夫定耐药性HBV（M552V）的方法，包括给予β-L-2'-脱氧核苷或其药学上可接受的盐、酯或前药。此外，提供了一种防止拉米夫定耐药性HBV（M552V）突变在未接触过的宿主中发生的方法，包括给予β-L-2'-脱氧核苷或其药学上可接受的盐、酯或前药。还提供了一种防止和/或抑制宿主中HBV双突变体（L528M / M552V）出现的方法，包括给予β-L-2'-脱氧核苷或其药学上可接受的盐、酯或前药。
• BETA-L-2' DEOXYNUCLEOSIDES FOR THE TREATMENT OF RESISTANT HBV STRAINS AND COMBINATION THERAPIES
  申请人：Standring David

  公开号：US20110172178A1

  公开（公告）日：2011-07-14

  It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.

  已经发现β-L-2'-去氧核苷可以对具有突变的耐药性乙肝病毒发挥作用。提供了一种用于治疗宿主中拉米夫定耐药性乙肝病毒（M552V）的方法，包括给予β-L-2'-去氧核苷或其药学上可接受的盐、酯或前药。此外，还提供了一种用于预防拉米夫定耐药性乙肝病毒（M552V）突变在原始宿主中发生的方法，包括给予β-L-2'-去氧核苷或其药学上可接受的盐、酯或前药。还提供了一种用于预防和/或抑制宿主中HBV双突变体（L528M/M552V）出现的方法，包括给予β-L-2'-去氧核苷或其药学上可接受的盐、酯或前药。
• QUINOLINE COMPOUNDS AND METHODS OF USE
  申请人：Gaudino John

  公开号：US20110053931A1

  公开（公告）日：2011-03-03

  Compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

  式（I）的化合物及其立体异构体、几何异构体、互变异构体、溶剂化物、代谢物、盐和药学上可接受的前药，用于抑制受体酪氨酸激酶并治疗由此介导的过度增殖性疾病。本文揭示了使用式（I）的化合物及其立体异构体、几何异构体、互变异构体、溶剂化物和药学上可接受的盐，在哺乳动物细胞中进行体外、体内和原位诊断、预防或治疗此类疾病或相关病理条件的方法。
• Process for preparing 4-hydroxypyrimidine
  申请人：UBE INDUSTRIES, LTD.

  公开号：EP0326389A2

  公开（公告）日：1989-08-02

  A process for preparing a 4-hydroxypyrimidine of Formula III: wherein R₁ and R₂ each represent a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms or an aralkyl group having 1 to 10 carbon atoms, and R₄ represents an alkyl group having 7 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms, an aralkyl group having 7 to 10 carbon atoms or an aryl group having 6 to 10 carbon atoms, which comprises subjecting a 3-amino-2-unsaturated carboxylate of Formula 1: wherein R₁ and R₂ are as defined above and R₃ represents an alkyl group having 1 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms or an aralkyl group having 7 to 10 carbon atoms, and a carboxylic acid amide of Formula II: R ₄ C O N H ₂ wherein R₄ is as defined above, to reaction with each other in the presence of a base.

  一种制备式 III 的 4-羟基嘧啶的工艺： 其中 R₁ 和 R₂ 各自代表氢原子、具有 1 至 10 个碳原子的烷基、具有 3 至 10 个碳原子的环烷基或具有 1 至 10 个碳原子的芳基，而 R₄ 代表具有 7 至 10 个碳原子的烷基、具有 3 至 10 个碳原子的环烷基、具有 7 至 10 个碳原子的芳基或具有 6 至 10 个碳原子的芳基、 其中包括将式 1 的 3-氨基-2-不饱和羧酸酯 其中 R₁ 和 R₂ 如上文所定义，R₃ 代表具有 1 至 10 个碳原子的烷基、具有 3 至 10 个碳原子的环烷基或具有 7 至 10 个碳原子的芳基、 和式 II 的羧酸酰胺： R ₄ C O N H ₂ 其中 R₄ 如上定义、 在碱存在下相互反应。