N-[4-(1,3-benzodioxol-5-yl)-1,3-thiazol-2-yl]-2-(6-methoxy-1-benzofuran-3-yl)acetamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并间二氧杂环戊烯类
• 英文名称: N-[4-(1,3-benzodioxol-5-yl)-1,3-thiazol-2-yl]-2-(6-methoxy-1-benzofuran-3-yl)acetamide
• 化学式: C₂₁H₁₆N₂O₅S
• 分子量: 408.4
• InChiKey: FKZLRLSJKMKTSC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  111
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] BENZOFURAN AMIDES AND HETEROAROMATIC ANALOGUES THEREOF FOR USE IN THERAPY<br/>[FR] AMIDES DE BENZOFURANE ET LEURS ANALOGUES HÉTÉROAROMATIQUES DESTINÉS À ÊTRE UTILISÉS EN THÉRAPIE
  申请人：EUROPEAN MOLECULAR BIOLOGY LABORATORY

  公开号：WO2018229193A1

  公开（公告）日：2018-12-20

  The present invention relatesto a pharmaceutical composition comprising acompound of the formula Ias described belowor a tautomeror a pharmaceutically acceptable salt thereof; to the compound of the formula Ias described below or a tautomer or a phar- maceutically acceptable salt thereof for use as a medicament, especially for use in the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization, and to certain novel compoundsof the formula Ias described below or a tautomer or a pharmaceuti- cally acceptable salt thereof. Formula (I) wherein X1 is CR1 or N; X2 is CR2 or N; X3 is CR3 or N; X4 is CR4 or N; with the proviso that at most two of X1, X2, X3 and X4 are N; L1, L2 are a bond or a bivalent radical such as C1-C6-alkylene or C3-C8-cycloalkylene; A is 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated carbocyclic ring which may carry one or more substituents R9; or L2-A forms a group C1-C6-alkylene-OR13, C1-C6-alkylene-SR14 or C1-C6-alkylene-NR15R16; and R1, R2, R3, R4, R5, R6, R9, R13, R14, R15 and R16 are as defined in the claims and the description.

  本发明涉及一种药物组合物，包括下述的化合物I的构造或其互变异构体或药用盐；以及用作药物的下述的化合物I的构造或其互变异构体或药用盐，特别用于治疗或预防从炎症性疾病、过度增殖性疾病或紊乱、缺氧相关病理和以过度血管生成为特征的疾病中选择的疾病或紊乱；以及下述的某些新型化合物I的构造或其互变异构体或药用盐。其中，化合物(I)中X1为CR1或N；X2为CR2或N；X3为CR3或N；X4为CR4或N；但X1、X2、X3和X4中最多有两个为N；L1、L2为键或类似C1-C6-烷基或C3-C8-环烷基的二价基团；A为3-、4-、5-、6-、7-或8-成员饱和、部分不饱和或最大不饱和的碳环，可能携带一个或多个取代基R9；或L2-A形成一个基团C1-C6-烷基-OR13、C1-C6-烷基-SR14或C1-C6-烷基-NR15R16；而R1、R2、R3、R4、R5、R6、R9、R13、R14、R15和R16如权利要求和说明中所定义。
• BENZOFURAN AMIDES AND HETEROAROMATIC ANALOGUES THEREOF FOR USE IN THERAPY
  申请人：European Molecular Biology Laboratory

  公开号：EP3638664A1

  公开（公告）日：2020-04-22