6-(双(2-氯乙基)氨基)-6-脱氧-D-吡喃半乳糖苷 | 105618-02-8

• 物质功能分类: 原料药 - 抗肿瘤药 - 烷化剂类抗肿瘤药
• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 6-(双(2-氯乙基)氨基)-6-脱氧-D-吡喃半乳糖苷
• 中文别名: 加莫司汀
• 英文名称: Galamustine
• 英文别名: (3R,4S,5R,6R)-6-[bis(2-chloroethyl)aminomethyl]oxane-2,3,4,5-tetrol
• CAS: 105618-02-8
• 化学式: C₁₀H₁₉Cl₂NO₅
• 分子量: 304.16
• InChiKey: COKGUJJIBXWRNV-CYNREMDZSA-N

物化性质

• 溶解度：
  甲醇（微溶）、水（微溶）

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  18
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  93.4
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• NICOTINAMIDE RIBOSIDE DERIVATIVES AND THEIR USES
  申请人：GANAPATI Gangadhara

  公开号：US20180362570A1

  公开（公告）日：2018-12-20

  The disclosure provides derivatives of both the oxidized form and the reduced form of nicotinamide riboside (NR) and nicotinic acid riboside (NAR). The NR and NAR derivatives have improved stability and bioavailability compared to NR and NAR, and can increase cellular NAD + levels and improve mitochondrial function. Therefore, the NR and NAR derivatives are useful for treating mitochondrial diseases, mitochondria-related diseases and conditions, and other disorders and conditions.

  该披露提供了烟酰胺核苷酸（NR）和烟酸核苷酸（NAR）的氧化形式和还原形式的衍生物。与NR和NAR相比，NR和NAR衍生物具有更好的稳定性和生物利用度，并且可以增加细胞NAD+水平并改善线粒体功能。因此，NR和NAR衍生物对治疗线粒体疾病、与线粒体相关的疾病和症状以及其他疾病和症状具有用处。
• NICOTINYL RIBOSIDE COMPOUNDS AND THEIR USES
  申请人：MitoPower, LLC

  公开号：US20200397807A1

  公开（公告）日：2020-12-24

  The disclosure provides nicotinamide riboside (NR), the reduced form of NR (NRH), nicotinic acid riboside (NAR), the reduced form of NAR (NARH), derivatives thereof, compositions thereof and uses thereof. The NR and NAR derivatives have improved stability and bioavailability compared to NR and NAR. NR, NRH, NAR, NARH, and derivatives thereof can increase cellular NAD + levels and enhance mitochondrial and cellular function and cell viability. Therefore, NR, NRH, NAR, NARH, and derivatives thereof, whether alone or in combination with one or more additional therapeutic agents (e.g., a mitochondrial uncoupler or/and a PARP inhibitor), are useful for treating mitochondrial diseases, mitochondria-related diseases and conditions, metabolic disorders, and other disorders and conditions.

  该披露提供烟酰胺核糖苷（NR）、烟酰胺核糖苷的还原形式（NRH）、烟酸核糖苷（NAR）、烟酸核糖苷的还原形式（NARH）、以及它们的衍生物、组合物和用途。与NR和NAR相比，NR和NAR的衍生物具有更好的稳定性和生物利用度。NR、NRH、NAR、NARH和它们的衍生物可以增加细胞NAD+水平，增强线粒体和细胞功能以及细胞存活能力。因此，NR、NRH、NAR、NARH和它们的衍生物，无论是单独使用还是与一个或多个额外治疗剂（例如线粒体解耦蛋白抑制剂和/或PARP抑制剂）结合使用，都可用于治疗线粒体疾病、与线粒体相关的疾病和症状、代谢紊乱以及其他疾病和症状。
• Modulators of the megalin-mediated uptake of radiotherapeutics and/or radiodiagnostics into kidney cells and their use in therapy and diagnostics
  申请人：Schering AG

  公开号：EP1462119A1

  公开（公告）日：2004-09-29

  The present invention broadly relates to the treatment, diagnosis, and prophylactic prevention of cancer disease. More specifically, the present invention relates to methods and compositions for preventing the endocytosis of radiopharmaceutics into cells of the kidney and the subsequent radioinduced damaging of the kidney catabolism by blocking or interfering with the association or binding of radiotherapeutics and/or radiodiagnostics to the receptor megalin, a member of the LDL-receptor family. In another aspect of the present invention, the expression of megalin is altered, in order to prevent the endocytosis and cellular internalisation of radiopharmaceutics into cells of the kidney.

  本发明广泛涉及癌症疾病的治疗、诊断和预防。更具体地说，本发明涉及通过阻断或干扰放射性治疗药物和/或放射性诊断药物与受体megalin（低密度脂蛋白受体家族的成员）的结合或结合，防止放射性药物内吞进入肾脏细胞以及随后放射性诱导的肾脏分解代谢损伤的方法和组合物。本发明的另一个方面是改变megalin的表达，以防止放射性药物内吞和细胞内化到肾脏细胞中。
• COX-2-targeting, platinum-containing conjugates and their use in the treatment of tumors and cancers
  申请人：Reiley Pharmaceuticals, Inc.

  公开号：US10053478B2

  公开（公告）日：2018-08-21

  The present disclosure provides platinum-containing conjugates that selectively target and kill tumor/cancer cells. The conjugates contain a moiety that selectively targets COX-2, which is overexpressed by a broad range of tumor/cancer cells.

  本公开提供了选择性靶向和杀死肿瘤/癌细胞的含铂共轭物。这些共轭物含有选择性靶向 COX-2 的分子，COX-2 被多种肿瘤/癌细胞过度表达。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。