马来酰亚胺基酰肼盐酸盐 | 293298-33-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 马来酰亚胺基酰肼盐酸盐
• 英文名称: maleimidopropionic acid hydrazide hydrochloride
• 英文别名: 3-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanehydrazide hydrochloride；3-(2,5-dioxopyrrol-1-yl)propanehydrazide;hydrochloride
• CAS: 293298-33-6
• 化学式: C₇H₉N₃O₃*ClH
• 分子量: 219.628
• InChiKey: DWTYLPPEWBCKDA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.29
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  92.5
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H302,H317

反应信息

• 作为反应物：
  描述：

  马来酰亚胺基酰肼盐酸盐 、 以 甲醇 为溶剂， 生成
  参考文献：
  名称：

  ANTHRACYCLINS AND CONJUGATES THEREOF

  摘要：

  The invention concerns analogues of nemorubicin as well as PNU-159,682 with a range of substituents other than 2"-0Me on the morpholino ring that beneficially affected the toxicity of the toxin over the molecules with the 2"-0Me group. In addition, it was found that PNU variants with modified 2"-O-alkyl chain show enhanced tolerability in vivo. Thus, by modification of the 2"-O-alkyl group, ADCs were generated with carefully tailored potency and tolerability to improve the administered dose in patients. The invention thus concerns compounds according to structure (1) and conjugates therewith, as well as pharmaceutical compositions and methods of targeting tumour cells and treating cancer.

  公开号：

  WO2024038065A1

文献信息

• TRANSMUCOSAL DELIVERY OF PHARMACEUTICAL ACTIVE SUBSTANCES
  申请人：JON Sangyong

  公开号：US20070292387A1

  公开（公告）日：2007-12-20

  Provided is a conjugate including a pharmacologically active substance covalently bound to chitosan or its derivative and a method for transmucosal delivery of a pharmacologically active substance using the same. Specifically, a conjugate includes a pharmacologically active substance covalently bound via a linker to chitosan; and a pharmaceutical composition for transmucosal administration of a drug includes the aforementioned conjugate and a pharmaceutically acceptable carrier. Further provided is a method for in vivo delivery of a pharmacologically active substance via a transmucosal route, by covalent binding of the active substance with chitosan or its derivative via a linker. The conjugate in accordance with the present invention exhibits excellent absorption rate and biocompatibility in biological mucous membranes, particularly mucous membranes of the alimentary canal (especially the gastrointestinal tract), in vivo degradability, and superior bioavailability even with oral administration, thus enabling treatment of diseases via oral administration of a drug.

  提供的是一个包括药理活性物质与壳聚糖或其衍生物共价结合的共轭物，以及使用该共轭物进行药理活性物质经粘膜途径传递的方法。具体来说，该共轭物包括通过连接剂与壳聚糖共价结合的药理活性物质；以及用于经粘膜途径给药的药物组合物包括上述共轭物和药学上可接受的载体。此外，提供了一种通过药理活性物质与壳聚糖或其衍生物通过连接剂共价结合的方式，经粘膜途径在体内传递药理活性物质的方法。根据本发明的共轭物在生物粘膜，特别是消化道（尤其是胃肠道）的粘膜中表现出优异的吸收速率和生物相容性，在体内可降解性，以及即使口服也具有优越的生物利用度，从而使得通过口服给药治疗疾病成为可能。
• DRUG DELIVERY CARRIER
  申请人：Kwon, Soon-Chang

  公开号：EP2319503A2

  公开（公告）日：2011-05-11

  The present disclosure relates to a drug delivery carrier including: (a) a biocompatible polymer; and (b) a hydrophobic group conjugated to the polymer. The drug delivery carrier according to the present disclosure having the hydrophobic group conjugated to the biocompatible polymer may be useful for adsorption of synthetic drugs having very low solubility in water. Further, it may regulate discharge rate of adsorbed drugs by regulating a portion of hydrophobic groups conjugated to the polymeric material. Thus, the present disclosure provides a broad-spectrum platform technology applicable to new hydrophobic synthetic drugs to be developed in the future as well as those that have been developed already but face difficulties due to low bioavailability. The disclosed drug delivery carrier may provide considerable therapeutic convenience for patients by combining stained-release characteristics with the ability for adsorption of a hydrophobic drug having low bioavailability. The drug delivery carrier according to the present disclosure may also be applied to protein therapeutics. For patent-expired first-generation protein drugs requiring daily or once-in-two-or-three-days injection, the present disclosure improves convenience by allowing second-generation injection formulations that are administered once a week or once or twice a month. As used herein, a "first-generation protein drug" refers to a biomedicine based on a natural protein prepared by a gene recombination technique and a "second-generation protein drug" refers to a biopharmaceutical improvement of a first-generation protein drug through formulation or modification of molecular structure for increasing half-life or extending treatment period through sustained release. The present disclosure provides a strong tool capable of achieving the desired effect simply by mixing with or adsorbing to the drug delivery carrier, unlike known techniques requiring modification or introduction of a special molecular structure to the first-generation or second-generation protein drug. Thus, application of the disclosed drug delivery carrier will shorten development time of next-generation protein drugs and will effectively contribute to increasing use of hydrophobic synthetic drugs. Ultimately, the disclosed drug delivery carrier will be useful for development of competitive new medicines such as sustained-release proteins and synthetic pharmaceuticals.

  本公开涉及一种药物输送载体，包括：(a) 生物相容性聚合物；(b) 与聚合物共轭的疏水基团。根据本公开的给药载体，其疏水基团与生物相容性聚合物共轭，可用于吸附在水中溶解度极低的合成药物。此外，它还可以通过调节与聚合物材料共轭的部分疏水基团来调节吸附药物的释放速率。因此，本公开提供了一种广谱平台技术，适用于未来将要开发的新型疏水性合成药物以及已经开发但由于生物利用度低而面临困难的药物。本发明公开的给药载体结合了染色释放特性和低生物利用度疏水性药物的吸附能力，可为患者提供极大的治疗便利。 本公开的给药载体还可用于蛋白质治疗。对于专利过期的第一代蛋白质药物，需要每天或两天或三天注射一次，而本公开的第二代注射制剂可以每周或每月注射一次或两次，从而提高了方便性。本文所用的 "第一代蛋白质药物 "是指基于基因重组技术制备的天然蛋白质的生物医药，"第二代蛋白质药物 "是指通过配方或分子结构修饰对第一代蛋白质药物进行生物制药改进，通过持续释放延长半衰期或延长治疗期。与需要对第一代或第二代蛋白质药物进行改性或引入特殊分子结构的已知技术不同，本公开提供了一种强有力的工具，只需与给药载体混合或吸附到给药载体上，就能达到预期效果。因此，公开的给药载体的应用将缩短下一代蛋白质药物的开发时间，并将有效促进疏水性合成药物的使用。最终，所公开的给药载体将有助于开发具有竞争力的新药，如缓释蛋白质和合成药物。