3-benzyl-1-methyl-6-(3-phenylprop-1-ynyl)-4H-quinazolin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 3-benzyl-1-methyl-6-(3-phenylprop-1-ynyl)-4H-quinazolin-2-one
• 化学式: C₂₅H₂₂N₂O
• 分子量: 366.5
• InChiKey: IOYBAWXPEPFCHJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.16
• 拓扑面积：
  23.6
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• 5,6-Fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
  申请人：——

  公开号：US20040043986A1

  公开（公告）日：2004-03-04

  This invention provides compounds defined by Formula I 1 or a pharmaceutically acceptable salt thereof, wherein R 1 , Q, Y 3 , Y 4 , Y 5 , Y 6 , Y 8 , R 2 , and R 4 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.

  该发明提供了由公式I1定义的化合物或其药学上可接受的盐，其中R1、Q、Y3、Y4、Y5、Y6、Y8、R2和R4如规范中所定义。该发明还提供了包含公式I中的化合物或其药学上可接受的盐的制药组合物，以及与药学上可接受的载体、稀释剂或辅料一起使用的制药组合物。该发明还提供了抑制动物中MMP-13酶的方法，包括向动物投与公式I中的化合物或其药学上可接受的盐。该发明还提供了治疗由MMP-13酶介导的疾病的方法，包括向患者投与公式I中的化合物或其药学上可接受的盐，可以单独使用或与其他药物组合使用。该发明还提供了治疗心脏病、多发性硬化、骨关节炎和类风湿性关节炎、除骨关节炎或类风湿性关节炎外的其他关节炎、心力衰竭、炎症性肠病、心力衰竭、年龄相关性黄斑变性、慢性阻塞性肺病、哮喘、牙周病、银屑病、动脉粥样硬化和骨质疏松症的方法，包括向患者投与公式I中的化合物或其药学上可接受的盐，可以单独使用或与其他药物组合使用。该发明还提供了包括公式I中的化合物或其药学上可接受的盐和规范中描述的另一个药物活性成分的组合物。
• [EN] 5,6-FUSED 3,4-DIHYDROPYRIMIDINE-2-ONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS<br/>[FR] DERIVES DE 3,4-DIHYDROPYRIMIDINE-2-ONE 5,6-FONDUE, UTILISE COMME INHIBITEURS DE METALLOPROTEINASE MATRICIELLE
  申请人：WARNER LAMBERT CO

  公开号：WO2004014869A2

  公开（公告）日：2004-02-19

  This invention provides compounds defined by Formula I or a pharmaceuticafy acceptable salt theme, wherein R1, Q, Y3, Y4, Y5, Y6, Y8, R2, and R4 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compounnd of Formula I and the use of the compounds of Formula I as matrix metalloproteinase inhibitors.