(1-Hydroxy-2,5-dioxopyrrolidin-1-ium-1-yl) 4-formylbenzoate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (1-Hydroxy-2,5-dioxopyrrolidin-1-ium-1-yl) 4-formylbenzoate
• 英文别名: (1-hydroxy-2,5-dioxopyrrolidin-1-ium-1-yl) 4-formylbenzoate
• 化学式: C12H10NO6+
• 分子量: 264.21
• InChiKey: GXTILYGNELJNJX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  97.7
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• [EN] ERYTHROPOIETIN CONJUGATES HAVING ORAL BIOAVAILABILITY<br/>[FR] CONJUGUÉS D'ÉRYTHROPOÏÉTINE PRÉSENTANT UNE BIODISPONIBILITÉ ORALE
  申请人：LEK PHARMACEUTICALS

  公开号：WO2015032981A1

  公开（公告）日：2015-03-12

  The present invention relates to erythropoietin (EPO) conjugates having a high bioavailability and efficacy, especially when administered perorally. Also provided are methods for preparing the EPO conjugates, their use for treating various diseases, and pharmaceutical compositions comprising said EPO conjugates, alone or in combination with absorption enhancers and/or coating polymers.

  本发明涉及具有高生物利用度和疗效的红细胞生成素（EPO）共轭物，特别是在口服给药时。还提供了制备EPO共轭物的方法，其用于治疗各种疾病，以及包括所述EPO共轭物的药物组合物，单独或与吸收增强剂和/或包衣聚合物结合使用。
• [EN] THERAPEUTIC CONJUGATES WITH SULFATED DENDRIMERS FOR INTRACELLULAR TARGETING<br/>[FR] CONJUGUÉS THÉRAPEUTIQUES COMPORTANT DES DENDRIMÈRES SULFATÉS POUR CIBLAGE INTRACELLULAIRE
  申请人：IC DISCOVERY GMBH

  公开号：WO2015177279A1

  公开（公告）日：2015-11-26

  The present invention relates to novel dendrimer conjugates, methods for their preparation and their use for treatment of diseases. The invention discloses a new method for the delivery of dendrimer conjugates with therapeutically active molecules into the cell by utilizing transmembrane solute carrier proteins enabling uptake of the inventive dendrimer conjugates. Particular subject-matter of the present invention is a conjugate of the formula E-[G-L- D(OSO3-M+)n]m,wherein E is a therapeutic or diagnostic effector molecule, wherein D(OSO3-M+)n is a dendrimer D carrying a number n of sulfate groups OSO3-M+, wherein the number n of sulfate groups is selected from 6 to 96, wherein M is a cationic inorganic or organic counter ion to the anionic sulfate group, wherein L is a linker or spacer between D and E, wherein G is a connecting functional group forming the attachment between L and E, and wherein m is an integer from 1 to 20.

  本发明涉及新型树状分子共轭物、其制备方法以及用于治疗疾病的方法。该发明揭示了一种新的方法，通过利用跨膜溶质载体蛋白，使创新的树状分子共轭物能够进入细胞，从而传递治疗活性分子。本发明的特定主题是公式E-[G-L-D（OSO3-M+）n]m的共轭物，其中E是治疗或诊断效应分子，D（OSO3-M+）n是携带n个硫酸酯基团OSO3-M+的树状分子D，硫酸酯基团的数量n选自6到96，其中M是阳离子无机或有机对阴离子硫酸酯基团的反离子，L是D和E之间的连接剂或间隔物，G是连接L和E的连接功能基团，m是1到20的整数。
• Factor VIII Conjugates
  申请人：NOVO NORDISK A/S

  公开号：US20150224203A1

  公开（公告）日：2015-08-13

  The present invention relates to FVIII conjugated to heparosan (HEP) polymers, methods for the manufacture thereof and uses of such conjugates. The resultant conjugates may be used in the treatment or prevention of bleeding disorders such as haemophilia.

  本发明涉及到与肝素硫酸聚合物（HEP）共轭的FVIII，其制造方法以及这种共轭物的用途。得到的共轭物可以用于治疗或预防出血性疾病，例如血友病。
• Therapeutic conjugates with sulfated dendrimers for intracellular targeting
  申请人：IC DISCOVERY GMBH

  公开号：US11045560B2

  公开（公告）日：2021-06-29

  The present invention relates to novel dendrimer conjugates, methods for their preparation and their use for treatment of diseases. The invention discloses a new method for the delivery of dendrimer conjugates with therapeutically active molecules into the cell by utilizing transmembrane solute carrier proteins enabling uptake of the inventive dendrimer conjugates. Particular subject-matter of the present invention is a conjugate of the formula E-[G-L-D(OSO3−M+)n]m, wherein E is a therapeutic or diagnostic effector molecule, wherein D(OSO3−M+)n is a dendrimer D carrying a number n of sulfate groups OSO3−M+, wherein the number n of sulfate groups is selected from 6 to 96, wherein M is a cationic inorganic or organic counter ion to the anionic sulfate group, wherein L is a linker or spacer between D and E, wherein G is a connecting functional group forming the attachment between L and E, and wherein m is an integer from 1 to 20.

  本发明涉及新型树枝状聚合物共轭物、其制备方法及其用于治疗疾病的用途。本发明公开了一种新方法，通过利用跨膜溶质载体蛋白使本发明的树枝状聚合物共轭物被吸收，从而将具有治疗活性分子的树枝状聚合物共轭物输送到细胞中。本发明的特定主题是式 E-[G-L-D(OSO3-M+)n]m的共轭物，其中 E 是治疗或诊断效应分子，D(OSO3-M+)n 是携带 n 个硫酸基团 OSO3-M+ 的树枝状聚合物 D，其中硫酸基团的数目 n 选自 6 至 96、其中 M 是阴离子硫酸基团的阳离子无机或有机反离子，其中 L 是 D 和 E 之间的连接物或间隔物，其中 G 是在 L 和 E 之间形成连接的连接官能团，其中 m 是 1 至 20 的整数。
• THERAPEUTIC CONJUGATES WITH SULFATED DENDRIMERS FOR INTRACELLULAR TARGETING
  申请人：IC Discovery GmbH

  公开号：EP3145984A1

  公开（公告）日：2017-03-29