4-methyl-1-morpholino-pentan-3-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 4-methyl-1-morpholino-pentan-3-one
• 英文别名: 4-Methyl-1-morpholino-pentan-3-on；4-Methyl-1-morpholin-4-ylpentan-3-one
• 化学式: C₁₀H₁₉NO₂
• 分子量: 185.266
• InChiKey: BAHYLOBQEWUBPB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  3-甲基-2-丁酮 、 聚合甲醛 、 吗啡啉盐酸盐 在 乙醇 作用下， 生成 4-methyl-1-morpholino-pentan-3-one
  参考文献：
  名称：

  The Synthesis of Some Alkylated Cyclohexenones and Aromatic Compounds

  摘要：

  DOI：

  10.1021/ja01164a038

文献信息

• [EN] PRODRUGS OF THERAPEUTIC COMPOUNDS<br/>[FR] PROMÉDICAMENTS DE COMPOSÉS THÉRAPEUTIQUES
  申请人：MYREXIS INC

  公开号：WO2012148550A1

  公开（公告）日：2012-11-01

  The present invention provides compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders such as cancers.

  本发明提供了化合物、药物组合物和包含这些化合物的药物，以及在治疗癌症等疾病和疾病的方法中使用这些化合物、组合物和药物。
• BISTRIFILATE-BASED FLUOROGENIC PROBES FOR DETECTION OF SUPEROXIDE ANION RADICAL
  申请人：Yang Dan

  公开号：US20150219676A1

  公开（公告）日：2015-08-06

  The invention provides fluorogenic compounds and probes that can be used as reagents for measuring, detecting and/or screening superoxide. The fluorogenic compounds of the invention can produce fluorescence colors, such as green, yellow, red, or far-red. The invention further provides fluorogenic compounds for selectively staining superoxide in the mitochondria of living cells. The invention also provides methods that can be used to measure, directly or indirectly, the presence and/or amount of superoxide in chemical samples and biological samples such as cells and tissues in living organisms, and a high-throughput screening methods for detecting or screening superoxide or compounds that can increase or decrease the level of superoxide in chemical and biological samples.

  该发明提供了可以用作测量、检测和/或筛选超氧化物的试剂的荧光化合物和探针。该发明的荧光化合物可以产生荧光颜色，如绿色、黄色、红色或远红色。该发明进一步提供了用于选择性染色活细胞线粒体中超氧化物的荧光化合物。该发明还提供了可用于直接或间接测量化学样品和生物样品中超氧化物的存在和/或量的方法，例如生物体内的细胞和组织，以及用于检测或筛选化学和生物样品中超氧化物或可以增加或减少超氧化物水平的化合物的高通量筛选方法。
• Novel HIV reverse transcriptase inhibitors
  申请人：He Gong-Xin

  公开号：US20090075939A1

  公开（公告）日：2009-03-19

  The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

  该发明涉及以下式子的化合物（I）：或其药学上可接受的盐，溶剂化物，酯和/或膦酸酯，含有这些化合物的组合物以及包括给予这些化合物的治疗方法。
• OXIME COMPOUNDS AND THE USE THEREOF
  申请人：Matsumura Akira

  公开号：US20090298878A1

  公开（公告）日：2009-12-03

  The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO 2 , CR 3 R 4 or the like; Z is optionally substituted lower alkyl, optionally substituted aryl or the like; W is optionally substituted lower alkylene or optionally substituted lower alkenylene, R 3 and R 4 are each independently hydrogen, lower alkyl or the like; p is 0, 1, or 2 and q is 0, 1 or 2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

  本发明涉及式(I)的肟化合物及其药学上可接受的盐、前药或溶剂，其中X为氢、可选取代芳基、可选取代杂环基或类似物；Y为CO、SO2、CR3R4或类似物；Z为可选取代的低烷基、可选取代的芳基或类似物；W为可选取代的低烷基或可选取代的低烯基，R3和R4各自独立地为氢、低烷基或类似物；p为0、1或2，q为0、1或2。本发明还涉及使用式(I)的化合物来治疗、预防或改善对钙通道封锁有反应的疾病，特别是N型钙通道。本发明的化合物特别适用于治疗疼痛。
• MODIFIED DRUGS FOR USE IN LIPOSOMAL NANOPARTICLES
  申请人：Cullis Pieter

  公开号：US20120237591A1

  公开（公告）日：2012-09-20

  Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.

  本文提供了适合装载到脂质体纳米粒子载体中的药物衍生物。在一些优选方面，衍生物包括一个难溶于水的药物，其经过弱碱基团的衍生化，通过LN跨膜pH或离子梯度活性装载到LN的水内部。弱碱基团可以选择包括一个亲脂性结构域，以便将药物活性地装载到脂质体膜的内单层上。优点是，药物衍生物的LN配方相对于相应的游离药物具有改善的溶解度、降低的毒性、增强的疗效和/或其他优势。