H-DL-Pyr-DL-Pro-DL-Ser-DL-Lys-DL-Asp-DL-Ala-DL-Phe-DL-xiIle-Gly-DL-Leu-DL-Met-NH2

• 分子结构分类: 有机化合物 - 有机聚合物 - 多肽
• 英文名称: H-DL-Pyr-DL-Pro-DL-Ser-DL-Lys-DL-Asp-DL-Ala-DL-Phe-DL-xiIle-Gly-DL-Leu-DL-Met-NH2
• 英文别名: 3-[[6-amino-2-[[3-hydroxy-2-[[1-(5-oxopyrrolidine-2-carbonyl)pyrrolidine-2-carbonyl]amino]propanoyl]amino]hexanoyl]amino]-4-[[1-[[1-[[1-[[2-[[1-[(1-amino-4-methylsulfanyl-1-oxobutan-2-yl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-oxobutanoic acid
• 化学式: C₅₄H₈₅N₁₃O₁₅S
• 分子量: 1188.4
• InChiKey: AYLPVIWBPZMVSH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.6
• 重原子数：
  83
• 可旋转键数：
  36
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  463
• 氢给体数：
  14
• 氢受体数：
  17

文献信息

• Pharmaceutical compositions of drug-oligomer conjugates and methods of treating diseases therewith
  申请人：——

  公开号：US20030069170A1

  公开（公告）日：2003-04-10

  Pharmaceutical compositions that include a drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component are present in a weight-to-weight ratio of between 1:5 and 5:1. Methods of treating diseases in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.

  描述了包括药物-寡聚物共轭物、脂肪酸成分和胆盐成分的药物组合物。药物以共价键连接到寡聚物基团上。脂肪酸成分和胆盐成分以1:5至5:1的重量比存在。还提供了利用这种药物组合物治疗需要此类治疗的受试者的方法，以及提供这种药物组合物的方法。
• Dibenzyl Amine Compounds and Derivatives
  申请人：Chang George

  公开号：US20070213371A1

  公开（公告）日：2007-09-13

  Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

  二苯基胺化合物及其衍生物，含有这种化合物的药物组合物以及使用这种化合物提高某些血浆脂质水平，包括高密度脂蛋白胆固醇，并降低其他一些血浆脂质水平，如低密度脂蛋白胆固醇和甘油三酯，并据此治疗由高密度脂蛋白胆固醇水平低和/或低密度脂蛋白胆固醇和甘油三酯水平高加重的疾病，如动脉粥样硬化和心血管疾病在某些哺乳动物，包括人类。
• [EN] THIOSEMICARBAZATES AND USES THEREOF<br/>[FR] THIOSEMICARBAZATES ET LEURS UTILISATIONS
  申请人：FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH

  公开号：WO2020227592A1

  公开（公告）日：2020-11-12

  Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

  巯酯，硫代氨基甲酸酯，硫代氨基甲酸酯，半硫代氨基甲酸酯，肽，氮代氨基酸共轭物和氮代肽；以及一种对受保护的硫代氨基甲酸酯和半硫代氨基甲酸酯进行化学选择性和位点特异性功能化的方法被描述。该方法采用三甲基脲反应特异性烷基化靠近酰硫醇基团的氮原子，使用醇生成可储存数月的受保护的单取代硫代氨基甲酸酯，在低温下使用卤化物试剂轻微条件下激活，并与其他基团正交集成以制备取代半氨基甲酸酰胺，例如，可用作氮代氨基酸共轭物，氮代肽和其他肽类模拟物的合成中间体。还描述了制备和使用尿酶，卡巴酰胺，半氨基甲酸酰胺，β-肽，氮代肽和其他肽类模拟物以及氮代肽共轭物的方法，以及尿酶，卡巴酰胺，半氨基甲酸酰胺，β-肽，氮代肽在药物发现，诊断，抑制，预防和治疗疾病中的用途。
• 1-Aryl-2-acetylamidopentanone derivatives for use as tachykinin receptor antagonists
  申请人：ELI LILLY AND COMPANY

  公开号：EP0699674A1

  公开（公告）日：1996-03-06

  This invention provides a novel series of the formula I substituted 1-aryl-2-acetamidopentanone derivatives which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.

  这项发明提供了一种新颖的公式I替代的1-芳基-2-乙酰胺基戊酮衍生物系列，这些衍生物在治疗或预防与过多的速激肽相关的生理紊乱方面是有用的。这项发明还提供了治疗这种生理紊乱的方法，以及利用这些新颖化合物的药物配方。
• Mixtures of drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
  申请人：——

  公开号：US20030228275A1

  公开（公告）日：2003-12-11

  A non-polydispersed mixture of conjugates in which each conjugate in the mixture comprises a drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may result in less inter-subject variability than polydispersed mixtures of similar conjugates.

  披露了一种非多分散混合物，其中混合物中的每个共轭物包括与包含聚乙二醇基团的寡聚物偶联的药物。该混合物可能表现出比类似共轭物的多分散混合物更高的体内活性。该混合物可能比类似共轭物的多分散混合物更有效地在体外模拟肠道消化模型中存活。该混合物可能导致比类似共轭物的多分散混合物更少的受试者间变异性。