2-(2,5-Dioxopyrrolidin-1-yl)oxy-2-oxoacetic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-(2,5-Dioxopyrrolidin-1-yl)oxy-2-oxoacetic acid
• 化学式: C₆H₅NO₆
• 分子量: 187.11
• InChiKey: YHRPISBAUXFKQO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  101
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Macrocyclic compounds as inhibitors of viral replication
  申请人：Blatt M. Lawrence

  公开号：US20050267018A1

  公开（公告）日：2005-12-01

  The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

  该实施例提供了一般式I-XIX的化合物，以及包括药物组合在内的组合物，其中包括一种主体化合物。该实施例还提供了治疗方法，包括治疗黄病毒感染的方法，包括丙型肝炎病毒感染的方法和治疗肝纤维化的方法，这些方法通常涉及向需要的个体施用一种主体化合物或组合物的有效量。
• [EN] COMPSTATIN ANALOGS WITH IMPROVED POTENCY AND PHARMACOKINETIC PROPERTIES<br/>[FR] ANALOGUES DE COMPSTATINE DE PUISSANCE ET DE PROPRIÉTÉS PHARMACOCINÉTIQUES AMÉLIORÉES
  申请人：UNIV PENNSYLVANIA

  公开号：WO2015142701A1

  公开（公告）日：2015-09-24

  Compounds comprising peptides capable of binding C3 protein and inhibiting complement activation are disclosed. The compounds include a modified compstatin peptide or analog thereof, comprising an added N-terminal component that improves (1) the binding affinity of the peptide to C3, C3b or C3c and/or (2) the plasma stability and/or plasma residence time of the peptide, as compared with an unmodified compstatin peptide under equivalent conditions. Methods of improving the C3 binding of compstatin or compstatin analogs are also disclosed, as well as methods of designing compstatin analogs with improved C3 binding.

  本发明涉及包含能够结合C3蛋白并抑制补体激活的肽的化合物。这些化合物包括一种经过修改的compstatin肽或其类似物，其中包括一个添加的N-末端组分，该组分改善了肽与C3、C3b或C3c的结合亲和力和/或与未经修改的compstatin肽在等效条件下相比的血浆稳定性和/或血浆停留时间。还公开了改善compstatin或compstatin类似物的C3结合的方法，以及设计具有改善C3结合的compstatin类似物的方法。
• MACROCYCLIC COMPOUNDS AS INHIBITORS OF VIRAL REPLICATION
  申请人：BLATT LAWRENCE M.

  公开号：US20090286843A1

  公开（公告）日：2009-11-19

  The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

  该实施例提供了一般式I-XIX的化合物，以及包括药物组合物在内的组合物。该实施例还提供了治疗方法，包括治疗黄热病毒感染的方法，包括丙型肝炎病毒感染的方法和治疗肝纤维化的方法，通常涉及向需要治疗的个体施用所述化合物或组合物的有效量。
• New interferon beta-like molecules
  申请人：Maxygen Aps

  公开号：EP2080771A2

  公开（公告）日：2009-07-22

  The invention relates to a conjugate exhibiting interferon β activity and comprising at least one first non-polypeptide moiety covalently attached to an interferon β polypeptide, the amino acid sequence of which differs from that of wildtype human interferon β in at least one introduced and at least one removed amino acid residue comprising an attachment group for said first non-polypeptide moiety. The first non-polypeptide moiety is e.g. a polymer molecule or a sugar moiety. The conjugate finds particular use in therapy. The invention also relates to a glycosylated variant of a parent interferon β (IFNB) polypeptide comprising at least one in vivo glycosylation site, wherein an amino acid residue of said parent polypeptide located close to said glycosylation site has been modified to obtain the variant polypeptide having an increased glycosylation as compared to the glycosylation of the parent polypeptide.

  本发明涉及一种具有干扰素 β 活性的共轭物，该共轭物包括至少一个共价连接到干扰素 β 多肽上的第一非多肽分子，该干扰素 β 多肽的氨基酸序列与野生型人干扰素 β 的氨基酸序列至少有一个引入氨基酸残基和至少一个移除氨基酸残基不同，该氨基酸残基包含所述第一非多肽分子的连接基团。第一非多肽分子是聚合物分子或糖分子。这种共轭物特别适用于治疗。本发明还涉及一种母体干扰素β（IFNB）多肽的糖基化变体，该变体包含至少一个体内糖基化位点，其中所述母体多肽中靠近所述糖基化位点的氨基酸残基已被修饰，以获得与母体多肽的糖基化程度相比糖基化程度增加的变体多肽。
• Hyperglycosylated variants of interferon alfacon-1
  申请人：Alios Biopharma Inc.

  公开号：EP2093235A1

  公开（公告）日：2009-08-26

  The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites. The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or nonnative glycosylation sites, as well as erythropoietin and darbepoetin alfa, each of which are linked to a penetrating peptide that facilitates translocation of a substance across a biological barrier as well as pharmaceutical compositions, including oral formulations, of the same. The present invention further provides oral formulations of hyperglycosylated or protease-resistant, hyperglycosylated polypeptide variants, which polypeptide variants lack at least one protease cleavage site found in a parent polypeptide, and thus exhibit increased protease resistance compared to the parent polypeptide, which polypeptide variants further include (1) a carbohydrate moiety covalently linked to at least one non-native glycosylation site not found in the parent protein therapeutic or (2) a carbohydrate moiety covalently linked to at least one native glycosylation site found but not glycosylated in the parent protein therapeutic. The present invention further provides compositions, including oral pharmaceutical compositions, comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides containers, devices, and kits comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides therapeutic methods involving administering an effective amount of an oral pharmaceutical composition comprising a synthetic Type I interferon receptor polypeptide agonist, a hyperglycosylated polypeptide variant, or a hyperglycosylated, protease-resistant polypeptide variant to an individual in need thereof.

  本发明提供合成的I型干扰素受体多肽激动剂，包括共识或混合I型干扰素受体多肽激动剂，含有一个或多个原生或非原生糖基化位点。本发明提供合成的 I 型干扰素受体多肽激动剂，包括共识或混合 I 型干扰素受体多肽激动剂，含有一个或多个原生或非原生糖基化位点，以及促红细胞生成素和达贝胎素α，其中每一种都与促进物质通过生物屏障转运的穿透肽相连，以及药物组合物，包括其口服制剂。本发明进一步提供了高糖基化或抗蛋白酶的高糖基化多肽变体的口服制剂，这些多肽变体缺乏母体多肽中的至少一个蛋白酶裂解位点，因此与母体多肽相比表现出更强的抗蛋白酶能力、多肽变体进一步包括(1)与至少一个非原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中未发现；或(2)与至少一个原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中发现但未糖基化。本发明进一步提供了包含合成的 I 型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体的组合物，包括口服药物组合物。本发明进一步提供了包含合成 I 型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体的容器、装置和试剂盒。本发明进一步提供了治疗方法，包括向有需要的个体施用有效量的口服药物组合物，该组合物包含合成的I型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体。