5,6-Didehydro-2,3-dihydro-1-benzofuran

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧唑烯
• 英文名称: 5,6-Didehydro-2,3-dihydro-1-benzofuran
• 英文别名: 5,6-didehydro-2,3-dihydro-1-benzofuran
• 化学式: C₈H₆O
• 分子量: 118.13
• InChiKey: VCBFHVSTOUGIGH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  9.2
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• [EN] NEW 6-AMINO-QUINOLINONE COMPOUNDS AND DERIVATIVES AS BCL6 INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS 6-AMINO-QUINOLINONE ET DÉRIVÉS EN TANT QU'INHIBITEURS DE BCL6
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2018108704A1

  公开（公告）日：2018-06-21

  The present invention encompasses compounds of formula (I), wherein the groups R1 to R5, X, Y and W have the meanings given in the claims and specification, their use as inhibitors of BCL6, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

  本发明涵盖了式(I)的化合物，其中基团R1至R5、X、Y和W具有权利要求和说明中给定的含义，它们作为BCL6的抑制剂的用途，含有这种化合物的药物组合物以及它们作为药物的用途，特别是作为治疗和/或预防肿瘤疾病的药剂。
• NOVEL STING AGONISTS
  申请人：Venenum Biodesign, LLC

  公开号：US20200131209A1

  公开（公告）日：2020-04-30

  The present invention provides compounds of Formula I′: wherein , W, X, Y, Z, Z 1 , Z 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.

  本发明提供了式I′的化合物： 其中 , W, X, Y, Z, Z 1 , Z 2 , R 1 , R 2 , R 3 , R 4 和R 5 如本文所定义，或其立体异构体、互变异构体、药学上可接受的盐、前药酯或溶剂化合物形式，其中所有变量均如本文所定义。这些化合物能有效调节STING蛋白，因此可用作治疗或预防受STING激动影响的疾病的药物。
• PYRAZOLYL-CONTAINING TRICYCLIC DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF
  申请人：Jiangsu Hansoh Pharmaceutical Group Co., Ltd.

  公开号：US20200247815A1

  公开（公告）日：2020-08-06

  The present invention relates to pyrazolyl-containing tricyclic derivative, a preparation method therefor and the use thereof. In particular, the present invention relates to a compound as shown in the general formula (I), a preparation method therefor and a pharmaceutical composition containing the compound, and the use thereof as a protease such as ERK (MAPK) inhibitor in the treatment of cancers, bone diseases, inflammatory diseases, immunological diseases, nervous system diseases, metabolic diseases, respiratory diseases and heart diseases, wherein the definition of each substituent in the general formula (1) is the same as defined in the description.

  本发明涉及吡唑基含有的三环衍生物，其制备方法及其用途。具体而言，本发明涉及一种如通式(I)所示的化合物，其制备方法及含有该化合物的药物组合物，以及将其用作蛋白酶，如ERK（MAPK）抑制剂，用于治疗癌症、骨疾病、炎症性疾病、免疫疾病、神经系统疾病、代谢性疾病、呼吸系统疾病和心脏疾病，其中通式（1）中每个取代基的定义与描述中定义的相同。
• HISTONE METHYLTRANSFERASE EZH2 INHIBITOR, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
  申请人：ANCUREALL PHARMACEUTICAL (SHANGHAI) CO., LTD.

  公开号：US20190345139A1

  公开（公告）日：2019-11-14

  The invention relates to a histone methyltransferase EZH2 inhibitor, a preparation method and pharmaceutical use thereof. In particular, the invention relates to a compound represented by the general formula (I), a preparation method thereof, a pharmaceutical composition containing the same, and a use thereof as a histone methyltransferase EZH2 inhibitor for treating diseases associated with the histone methyltransferase EZH2, especially cancer. The definition of each substituents in the general formula (I) is same as the definition in the specification.

  这项发明涉及一种组蛋白甲基转移酶EZH2抑制剂，其制备方法和药用。具体而言，该发明涉及一种由通式（I）表示的化合物，其制备方法，含有该化合物的药物组合物，以及将其用作组蛋白甲基转移酶EZH2抑制剂治疗与组蛋白甲基转移酶EZH2相关的疾病，特别是癌症。通式（I）中每个取代基的定义与规范中的定义相同。
• METHOD FOR PREPARING COAGULATION FACTOR XIA INHIBITOR AND INTERMEDIATE THEREOF
  申请人：JIANGSU HENGRUI MEDICINE CO., LTD.

  公开号：US20210292279A1

  公开（公告）日：2021-09-23

  The present disclosure involves a method for preparing a coagulation factor XIa inhibitor and an intermediate thereof. Specifically, the present disclosure involves a method for preparing an oxypyridine amide derivative. The method has the advantages of high yield, good product purity, and mild reaction conditions.

  本公开涉及一种制备凝血因子XIa抑制剂及其中间体的方法。具体而言，本公开涉及一种制备氧吡啶酰胺衍生物的方法。该方法具有高产率、良好的产品纯度和温和的反应条件的优点。