2-(1,2,3,4-Tetrahydroquinolin-7-yl)-1,3-benzoxazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 2-(1,2,3,4-Tetrahydroquinolin-7-yl)-1,3-benzoxazole
• 英文别名: 2-(1,2,3,4-tetrahydroquinolin-7-yl)-1,3-benzoxazole
• 化学式: C₁₆H₁₄N₂O
• 分子量: 250.29
• InChiKey: FHEOHWYGYXTQDF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  38.1
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] PYRIDINE SULFONAMIDES<br/>[FR] SULFONAMIDES DE PYRIDINE
  申请人：AMGEN INC

  公开号：WO2018017896A1

  公开（公告）日：2018-01-25

  The present invention provides compounds of Formula (I), as defined in the specification, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders, cough, or itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

  本发明提供了如规范中定义的Formula (I)的化合物，或其药用可接受的盐，这些化合物是电压门控钠通道的抑制剂，特别是Nav 1.7。这些化合物对于治疗可通过抑制钠通道治疗的疾病如疼痛障碍、咳嗽或瘙痒是有用的。还提供了含有本发明化合物的药物组合物。
• [EN] HETEROARYL AMIDES USEFUL AS KIF18A INHIBITORS<br/>[FR] AMIDES D'HÉTÉROARYLE UTILES EN TANT QU'INHIBITEURS DE KIF18A
  申请人：AMGEN INC

  公开号：WO2020132649A1

  公开（公告）日：2020-06-25

  The present invention relates to chemical compounds having a general formula (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

  本发明涉及具有通式（I）的化合物及其合成中间体，其可调节KIF18A蛋白从而影响细胞周期和细胞增殖过程以治疗癌症和癌症相关疾病。该发明还包括包括这些化合物的药物组合物，以及治疗与KIF18A活性相关的疾病状态的方法。
• [EN] KIF18A INHIBITORS<br/>[FR] INHIBITEURS DE KIF18A
  申请人：AMGEN INC

  公开号：WO2021026098A1

  公开（公告）日：2021-02-11

  Amide compounds of formula (I): and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of Kinesin Motor Protein KIF18A, such as cancer, psoriasis, atopic dermatitis, an autoimmune disorder, or inflammatory bowel disease, and the like.

  化合物的酰胺类化合物（I）的化学式：以及含有它们的组合物，以及制备这种化合物的方法。本文还提供了治疗通过抑制Kinesin Motor Protein KIF18A可治疗的疾病或疾病的方法，如癌症，牛皮癣，特应性皮炎，自身免疫性疾病或炎症性肠病等。
• [EN] PYRIDINE DERIVATIVES AS KIF18A INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIDINE EN TANT QU'INHIBITEURS DE KIF18A
  申请人：AMGEN INC

  公开号：WO2021026100A1

  公开（公告）日：2021-02-11

  Amide compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

  化合物的酰胺类似物（公式（I））：如本文所定义，并其合成中间体，能够调节KIF18A蛋白，从而影响细胞周期和细胞增殖的过程，以治疗癌症和癌症相关疾病。该发明还包括包括这些化合物的药物组合物，以及治疗与KIF18A活性相关的疾病状态的方法。
• [EN] HETEROALKYL DIHYDROQUINOLINE SULFONAMIDE COMPOUNDS<br/>[FR] COMPOSÉS DE SULFONAMIDE DE DIHYDROQUINOLÉINE D'HÉTÉROALKYLE
  申请人：AMGEN INC

  公开号：WO2021252822A1

  公开（公告）日：2021-12-16

  The present invention provides heteroalkyl dihydroquinoline sulfonamide compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

  本发明提供了Formula I的杂烷基二氢喹啉磺胺类化合物及其药学上可接受的盐，这些化合物是钠通道的抑制剂，特别是Nav1.7。这些化合物对于治疗与钠通道活性相关的疾病如疼痛障碍、咳嗽和瘙痒是有用的。还提供了含有本发明化合物的药物组合物。