3-methyl-3-(7-methyl-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 3-methyl-3-(7-methyl-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione
• 化学式: C₁₅H₁₆N₂O₃
• 分子量: 272.3
• InChiKey: JZIKIPVCUXKEIS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  66.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] BET BROMODOMAIN PROTEIN DEGRADERS WITH CLEAVABLE LINKERS<br/>[FR] AGENTS DE DÉGRADATION DE PROTÉINE DE BROMODOMAINE BET AVEC DES LIEURS CLIVABLES
  申请人：UNIV MICHIGAN REGENTS

  公开号：WO2019055444A1

  公开（公告）日：2019-03-21

  The present disclosure provides compounds represented by Formula (I): Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Y, =, Ar, W, L, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I)I for use to treat a condition or disorder responsive to inhibition and/or degradation of BET bromodomains such as cancer.

  本公开提供由Formula (I)表示的化合物：Formula (I)及其药用可接受的盐和溶剂，其中R1、R2a、R2b、R3a、R3b、R4、Y、=、Ar、W、L和B的定义如规范中所述。本公开还提供Formula (I)的化合物，用于治疗对BET溴结构域的抑制和/或降解敏感的疾病或疾病，如癌症。
• [EN] FUSED 1,4-DIAZEPINES AS BET PROTEIN DEGRADERS<br/>[FR] 1,4-DIAZÉPINES FUSIONNÉES EN TANT QU'AGENTS DE DÉGRADATION DE PROTÉINES BET
  申请人：UNIV MICHIGAN REGENTS

  公开号：WO2018052949A1

  公开（公告）日：2018-03-22

  The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.

  本公开提供由式I表示的化合物：I，及其药用可接受的盐、水合物和溶剂合物，其中R1、R2a、R2b、R3、R4、Ar、L、X、Y和B的定义如规范中所述。本公开还提供用于治疗对BET溴结构域降解敏感的疾病或疾病的式I化合物，如癌症。
• [EN] MONOFUNCTIONAL INTERMEDIATES FOR LIGAND-DEPENDENT TARGET PROTEIN DEGRADATION<br/>[FR] INTERMÉDIAIRES MONOFONCTIONNELS POUR LA DÉGRADATION D'UNE PROTÉINE CIBLE DÉPENDANTE DU LIGAND
  申请人：UNIV MICHIGAN REGENTS

  公开号：WO2017176958A1

  公开（公告）日：2017-10-12

  The present disclosure provides compounds represented by Formula I: and the salts or solvates thereof, wherein X, L, Y, and B are as defined in the specification. Compounds having Formula I are immunomodulators and/or monofunctional synthetic intermediates that can be used to prepare small-molecule drug conjugates.

  本公开提供了由式I表示的化合物及其盐或溶剂合物，其中X、L、Y和B如规范中所定义。具有式I的化合物是免疫调节剂和/或可用于制备小分子药物共轭物的单功能合成中间体。
• [EN] DEGRADERS THAT TARGET ALK AND THERAPEUTIC USES THEREOF<br/>[FR] AGENTS DE DÉGRADATION CIBLANT L'ALK ET LEURS UTILISATIONS THÉRAPEUTIQUES
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2020069106A1

  公开（公告）日：2020-04-02

  Disclosed are bispecific compounds (degraders) that target ALK for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat diseases and disorders characterized or mediated by aberrant ALK activity

  本发明涉及双特异性化合物（降解剂），其靶向ALK进行降解。本发明还涉及含有这些降解剂的制药组合物，以及使用这些化合物治疗由异常ALK活性特征化或介导的疾病和障碍的方法。
• 1-OXO- AND 1,3-DIOXOISOINDOLINES AND METHOD OF REDUCING INFLAMMATORY CYTOKINE LEVELS
  申请人：——

  公开号：US20010006973A1

  公开（公告）日：2001-07-05

  1-Oxo- and 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)isoindolines substituted in the 4- and/or 7-position of the isoindoline ring and optionally further substituted in the 3-position of the 2,6-dioxopiperidine ring reduce the levels of inflammatory cytokines such as TNF&agr; in a mammal. A typical embodiment is 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-4-methylisoindoline

  在异吲哚啉环的4-和/或7-位取代的1-氧代和1,3-二氧代-2-(2,6-二氧代哌啶-3-基)异吲哚啉，可选择在2,6-二氧代哌啶环的3-位进一步取代，可降低哺乳动物体内炎性细胞因子如TNFα的水平。一个典型的实施例是1,3-二氧代-2-(2,6-二氧代哌啶-3-基)-4-甲基异吲哚啉。