3-Tert-butylsulfanyl-1-methylpyrrolidine-2,5-dione

• 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-Tert-butylsulfanyl-1-methylpyrrolidine-2,5-dione
• 英文别名: 3-tert-butylsulfanyl-1-methylpyrrolidine-2,5-dione
• 化学式: C₉H₁₅NO₂S
• 分子量: 201.29
• InChiKey: WJAQCZOLQQKOKH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  62.7
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] PROGRAMMABLE POLYMERIC DRUGS<br/>[FR] MÉDICAMENTS POLYMÈRES PROGRAMMABLES
  申请人：SONY CORP

  公开号：WO2020210694A1

  公开（公告）日：2020-10-15

  Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, La, Lb, L1, L2, L3, M, m, and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

  揭示了作为生物活性化合物有用的化合物。这些化合物具有以下结构（I）：或其立体异构体、互变异构体或盐，其中R1、R2、R3、R4、R5、La、Lb、L1、L2、L3、M、m和n如本文所定义。还提供了与这些化合物的制备和使用相关的方法。
• CONJUGATES COMPRISING AN GLP-1/GLUCAGON DUAL AGONIST, A LINKER AND HYALURONIC ACID
  申请人：SANOFI

  公开号：US20180154005A1

  公开（公告）日：2018-06-07

  The present invention relates to a conjugate or a pharmaceutically acceptable salt thereof comprising an GLP-1/Glucagon receptor agonist, a linker and a hyaluronic acid hydrogel bearing -L 1 -L 2 -L-Y—R 20 groups, wherein Y represents an GLP-1/Glucagon receptor agonist moiety; and -L is a linker moiety—by formula (la), wherein the dashed line indicates the attachment to one of the amino groups of the GLP-1/Glucagon receptor agonist moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said conjugates as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by GLP-1/Glucagon receptor agonist.

  本发明涉及一种共轭物或其药用可接受盐，包括GLP-1/胰高血糖素受体激动剂、连接剂和携带-L1-L2-L-Y—R20基团的透明质酸水凝胶，其中Y代表GLP-1/胰高血糖素受体激动剂基团；而-L是连接剂基团—按照公式（la），其中虚线表示通过形成酰胺键与GLP-1/胰高血糖素受体激动剂基团的氨基之一连接。该发明还涉及包含所述共轭物的药物组合物，以及它们作为治疗或预防可通过GLP-1/胰高血糖素受体激动剂治疗的疾病或紊乱的药物的用途。
• Cytotoxic peptides and conjugates thereof
  申请人：NOVARTIS AG

  公开号：US10280139B2

  公开（公告）日：2019-05-07

  Disclosed herein are novel compounds of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel compound linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.

  本文公开了如本文所述的新型式 (I) 化合物： 本发明还描述了免疫结合剂（即抗体药物结合剂），其包含与抗原结合分子（如抗体）连接的此类新型化合物；其中此类免疫结合剂可用于治疗细胞增殖性疾病。本发明进一步提供了包含这些免疫共轭物的药物组合物、包含这些免疫共轭物与治疗共用试剂的组合物，以及使用这些免疫共轭物和组合物治疗细胞增殖障碍的方法。
• Pyrrolobenzodiazepines and targeted conjugates
  申请人：SEATTLE GENETICS, INC.

  公开号：US10328084B2

  公开（公告）日：2019-06-25

  A compound, or a pharmaceutically acceptable salt or solvate thereof, or conjugates thereof, selected from the group consisting of: wherein: (a) R10 is H, and R11 is OH, ORA, where RA is saturated C1-4 alkyl; (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is SOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation, or both M together are a divalent pharmaceutically acceptable cation.

  选自以下组别的化合物或其药学上可接受的盐或溶液，或其共轭物： 其中 (a) R10 为 H，R11 为 OH、ORA，其中 RA 为饱和 C1-4 烷基； (b) R10 和 R11 所结合的氮原子和碳原子之间形成氮碳双键；或 (c) R10 为 H，R11 为 SOzM，其中 z 为 2 或 3，M 为一价药学上可接受的阳离子，或两个 M 均为二价药学上可接受的阳离子。
• Conjugates comprising an GLP-1/glucagon dual agonist, a linker and hyaluronic acid
  申请人：SANOFI

  公开号：US10792367B2

  公开（公告）日：2020-10-06

  The present invention relates to a conjugate or a pharmaceutically acceptable salt thereof comprising an GLP-1/Glucagon receptor agonist, a linker and a hyaluronic acid hydrogel bearing -L1-L2-L-Y—R20 groups, wherein Y represents an GLP-1/Glucagon receptor agonist moiety; and -L is a linker moiety—by formula (Ia), wherein the dashed line indicates the attachment to one of the amino groups of the GLP-1/Glucagon receptor agonist moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising the conjugates as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by GLP-1/Glucagon receptor agonist.

  本发明涉及一种共轭物或其药学上可接受的盐，该共轭物或其药学上可接受的盐包含一种 GLP-1/Glucagon 受体激动剂、一种连接基团和一种带有-L1-L2-L-Y-R20 基团的透明质酸水凝胶，其中 Y 代表一种 GLP-1/Glucagon 受体激动剂分子；-L 是一种连接基团--按式 (Ia)、 其中虚线表示通过形成酰胺键连接到 GLP-1/Glucagon 受体激动剂分子的一个氨基上。本发明还涉及包含这些共轭物的药物组合物，以及它们作为治疗或预防可由 GLP-1/Glucagon 受体激动剂治疗的疾病或紊乱的药物的用途。