2-[2-(2-Oxo-pyrrolidin-1-yl)-ethyl]-isoindole-1,3-dione | 84598-47-0

• 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: 2-[2-(2-Oxo-pyrrolidin-1-yl)-ethyl]-isoindole-1,3-dione
• 英文别名: 2-(2-(2-Oxopyrrolidin-1-yl)ethyl)isoindoline-1,3-dione；2-[2-(2-oxopyrrolidin-1-yl)ethyl]isoindole-1,3-dione
• CAS: 84598-47-0
• 化学式: C₁₄H₁₄N₂O₃
• 分子量: 258.277
• InChiKey: ZGOLWMXTVMBZBL-UHFFFAOYSA-N

物化性质

• 熔点：
  99.5-101.5 °C
• 沸点：
  460.8±28.0 °C(Predicted)
• 密度：
  1.341±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  57.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-[2-(2-Oxo-pyrrolidin-1-yl)-ethyl]-isoindole-1,3-dione 以8%的产率得到
  参考文献：
  名称：

  MACHIDA, MINORU;TAKECHI, HARUKO;SHISHIDO, YOKO;KANAOKA, YUICHI, SYNTHESIS, BRD, 1982, N 12, 1078-1080

  摘要：

  DOI：
• 作为产物：
  描述：

  2-吡咯烷酮 、 sodium;hydride 、 N-(2-溴乙基)邻苯二甲酰亚胺 在 氩 、 水 、 magnesium sulfate 、 Ethyl acetate hexane methylene-chloride 作用下， 以 N,N-二甲基甲酰胺 、 乙酸乙酯 为溶剂， 反应 21.0h， 以Flash chromatography of the resulting crude oil with a solvent gradient of 40:10:50, 50:10:40, 60:10:30, and 70:10:20 EtOAc-CH2Cl2-Hexane afforded the title compound as a golden yellow oil的产率得到2-[2-(2-Oxo-pyrrolidin-1-yl)-ethyl]-isoindole-1,3-dione
  参考文献：
  名称：

  Aryl nitrogen-containing bicyclic compounds and methods of use

  摘要：

  本发明涉及一种新的化合物类别，对蛋白激酶介导的疾病，包括炎症、癌症和相关疾病的预防和治疗有用。该化合物具有一般的式子I，其中A1、A2、A3、B、R1、R2、R3和R4在此定义。因此，本发明还涉及包含本发明化合物的制药组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及用于制备本发明化合物的中间体和过程。

  公开号：

  US20070054916A1

文献信息

• Modulators of G-protein coupled receptors
  申请人：Carmot Therapeutics, Inc.

  公开号：US11535660B1

  公开（公告）日：2022-12-27

  This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize or partially agonize or antagonize) glucagon?like peptide?1 receptor (“GLP?1R”) and/or the gastric inhibitory polypeptide receptor (“GIPR”). The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which modulation (e.g., agonism, partial agonism or antagonism) of GLP?1R and/or GIPR activities is beneficial for the treatment or prevention of the underlying pathology and/or symptoms and/or progression of the disease, disorder, or condition. In some embodiments, the modulation results in an enhancement of (e.g., an increase in) existing levels (e.g., normal or below normal levels) of GLP?1R and/or GIPR activity (e.g., signaling). In some embodiments, the chemical entities described herein further modulate (e.g., attenuate, uncouple)-arrestin signaling relative to what is observed with the native ligand. This disclosure also features compositions as well as other methods of using and making the said chemical entities.

  本公开的化学实体（如化合物或该化合物的药学上可接受的盐和/或水合物和/或原药）可调节（如激动或部分激动或拮抗）胰高血糖素样肽1受体（"GLP?1R"）和/或胃抑制多肽受体（"GIPR"）。这些化学实体是有用的，例如，用于治疗患有疾病、失调或病症的受试者（例如人类），在这种情况下，调节（例如，激动、部分激动或拮抗）GLP?1R 和/或 GIPR 的活性有利于治疗或预防潜在的病理和/或症状和/或疾病、失调或病症的进展。在一些实施方案中，调节的结果是增强（如增加）现有水平（如正常或低于正常水平）的GLP?1R和/或GIPR活性（如信号传导）。在某些实施方案中，本文所述的化学实体可进一步调节（如减弱、解除耦合）--相对于原生配体的信号转导。本公开还包括组合物以及使用和制造所述化学实体的其他方法。
• Photochemical Synthesis of Multicyclic Fused Imidazolidines, Hydropyrazines, and Hydro-1,4-diazepines
  作者：Minoru Machida、Haruko Takechi、Yoko Shishido、Yuichi Kanaoka

  DOI：10.1055/s-1982-30075

  日期：——
• ARYL NITROGEN-CONTAINING BICYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS
  申请人：AMGEN INC.

  公开号：EP1836174A2

  公开（公告）日：2007-09-26
• [EN] ARYL NITROGEN-CONTAINING BICYCLIC COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSES BICYCLIQUES AZOTES D'ARYLE ET LEURS PROCEDES D'UTILISATION
  申请人：AMGEN INC

  公开号：WO2006039718A2

  公开（公告）日：2006-04-13

  The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I, wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
• [EN] MODULATORS OF G-PROTEIN COUPLED RECEPTORS<br/>[FR] MODULATEURS DE RÉCEPTEURS COUPLÉS À LA PROTÉINE
  申请人：CARMOT THERAPEUTICS INC

  公开号：WO2019183577A1

  公开（公告）日：2019-09-26

  This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize or partially agonize or antagonize) glucagon?like peptide?1 receptor ("GLP?1R") and/or the gastric inhibitory polypeptide receptor ("GIPR"). The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which modulation (e.g., agonism, partial agonism or antagonism) of GLP?1R and/or GIPR activities is benficial for the treatment or prevention of the underlying pathology and/or symptoms and/or progression of the disease, disorder, or condition. In some embodiments, the modulation results in an enhancment of (e.g., an increase in) existing levels (e.g., normal or below normal levels) of GLP?1R and/or GIPR activity (e.g., signaling). In some embodiments, the chemical entities described herein further modulate (e.g., attenuate, uncouple) -arrestin signaling relative to what is observed with the native ligand. This disclosure also features compositions as well as other methods of using and making the said chemical entities.