3-ethylsulfanyl-1-methyl-pyrrolidine-2,5-dione | 15543-05-2

• 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: 3-ethylsulfanyl-1-methyl-pyrrolidine-2,5-dione
• 英文别名: 3-Ethylsulfanyl-1-methylpyrrolidine-2,5-dione
• CAS: 15543-05-2
• 化学式: C₇H₁₁NO₂S
• 分子量: 173.236
• InChiKey: GTRBXOUAROMDFJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  62.7
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
  申请人：MEDIMMUNE LIMITED

  公开号：US20170239365A1

  公开（公告）日：2017-08-24

  A conjugate comprising a PBD dimer linked from the tether joining the two PBD units, wherein the linker is of formula (A1): (Formula (A1)) wherein R N1 is selected from H and C 1-4 alkyl; L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; Q is: (Formula (Q)), where Q x is such that Q is an amino-acid residue, a dipeptide residue or a tripeptide residue.

  一个由连接两个PBD单元的纽带相连的PBD二聚体组成的共轭物，其中连接剂的结构式为(A1)：(结构式(A1)) 其中R N1 选自H和C 1-4 烷基；L是与细胞结合剂相连的连接剂；CBA是细胞结合剂；n是0到48范围内的整数；Q是：(结构式(Q))，其中Q x 使得Q为氨基酸残基、二肽残基或三肽残基。
• [EN] HEMIASTERLIN DERIVATIVES FOR CONJUGATION AND THERAPY<br/>[FR] DÉRIVÉS D'HÉMIASTERLINE POUR CONJUGAISON ET THÉRAPIE
  申请人：SUTRO BIOPHARMA INC

  公开号：WO2016123582A1

  公开（公告）日：2016-08-04

  Provided herein are hemiasterlin derivatives, conjugates thereof, compositions comprising the derivatives or conjugates thereof, methods of producing the derivatives and conjugates thereof, and methods of using the derivatives, conjugates, and compositions for the treatment of cell proliferation. The derivatives, conjugates, and compositions are useful in methods of treatment and prevention of cell proliferation and cancer, methods of detection of cell proliferation and cancer, and methods of diagnosis of cell proliferation and cancer. In an embodiment, the hemiasterlin derivatives are according to Formula 1000: or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein Ar, L, W1, W4, W5, SG, and R are as described herein.

  本文提供了半星菱素衍生物，以及与之结合的共轭物，包含这些衍生物或共轭物的组合物，生产这些衍生物和共轭物的方法，以及利用这些衍生物、共轭物和组合物治疗细胞增殖的方法。这些衍生物、共轭物和组合物在治疗和预防细胞增殖和癌症的方法中很有用，也可用于检测细胞增殖和癌症的方法，以及诊断细胞增殖和癌症的方法。在一个实施例中，半星菱素衍生物符合公式1000：或其药用可接受的盐、溶剂化合物或互变异构体，其中Ar、L、W1、W4、W5、SG和R如本文所述。
• [EN] CONTROLLED-RELEASE CNP AGONISTS WITH LOW INITIAL NPR-B ACTIVITY<br/>[FR] AGONISTES DE CNP À LIBÉRATION CONTRÔLÉE AVEC FAIBLE ACTIVITÉ NPR-B INITIALE
  申请人：ASCENDIS PHARMA GROWTH DISORDERS AS

  公开号：WO2017118703A1

  公开（公告）日：2017-07-13

  The present invention relates to a controlled-release CNP agonist from which CNP agonist is released with a release half-life of at least 6 hours under physiological conditions and which controlled-release CNP agonist has an EC50 that is at least 20-fold higher than the EC50 of the corresponding free CNP agonist and which released CNP agonist has an EC50 that is at most 3-fold higher than the EC50 of the corresponding free CNP agonist; to pharmaceutical compositions comprising said controlled-release CNP agonist; their use; and to methods of treatment.

  本发明涉及一种受控释放的CNP激动剂，其中在生理条件下，CNP激动剂以至少6小时的释放半衰期释放，并且该受控释放的CNP激动剂的EC50至少比相应的游离CNP激动剂的EC50高20倍，并且释放的CNP激动剂的EC50至多比相应的游离CNP激动剂的EC50高3倍；以及包含所述受控释放的CNP激动剂的药物组合物；其用途；以及治疗方法。
• [EN] CONTROLLED-RELEASE CNP AGONISTS WITH REDUCED SIDE-EFFECTS<br/>[FR] AGONISTES DE CNP À LIBÉRATION CONTRÔLÉE PRÉSENTANT DES EFFETS SECONDAIRES RÉDUITS
  申请人：ASCENDIS PHARMA GROWTH DISORDERS AS

  公开号：WO2017118707A1

  公开（公告）日：2017-07-13

  The present invention relates a pharmaceutical composition comprising a controlled-release CNP agonist which reduces CNP agonist-associated side-effects, the use of such controlled-release CNP agonist and to methods of treatment.

  本发明涉及一种包含控释CNP激动剂的药物组合物，该药物组合物减少了与CNP激动剂相关的副作用，以及使用这种控释CNP激动剂和治疗方法。
• [EN] CONTROLLED-RELEASE CNP AGONISTS WITH INCREASED NEP STABILITY<br/>[FR] AGONISTES CNP À LIBÉRATION CONTRÔLÉE PRÉSENTANT UNE MEILLEURE STABILITÉ À NEP
  申请人：ASCENDIS PHARMA GROWTH DISORDERS AS

  公开号：WO2017118700A1

  公开（公告）日：2017-07-13

  The present invention relates to controlled-release CNP agonists having an at least 5-fold longer degradation half-life in an in vitro NEP degradation assay than the corresponding released CNP agonist, to pharmaceutical compositions comprising said controlled-release CNP agonist, their use and to methods of treatment.

  本发明涉及具有至少5倍长的降解半衰期的控制释放的CNP激动剂，在体外NEP降解测定中比相应释放的CNP激动剂，以及包含所述控制释放的CNP激动剂的药物组合物，它们的用途和治疗方法。