6-(3-phenylprop-2-ynyl)-3-(pyridin-4-ylmethyl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 6-(3-phenylprop-2-ynyl)-3-(pyridin-4-ylmethyl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-one
• 化学式: C₂₂H₂₀N₄O
• 分子量: 356.4
• InChiKey: HMZVPXGDCOLQEA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  48.8
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Fused tetrahydropyridine derivatives as matrix metalloproteinase inhibitors
  申请人：——

  公开号：US20040038960A1

  公开（公告）日：2004-02-26

  This invention provides compounds defined by Formula I 1 or a pharmaceutically acceptable salt thereof, wherein R 1 , Q, Y 1 , Y 2 , Y 3 , and R 2 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.

  本发明提供了由式 I 定义的化合物 1 或其药学上可接受的盐、 其中 R 1 、Q、Y 1 , Y 2 , Y 3 和 R 2 如说明书中所定义。本发明还提供了药物组合物，其包含式 I 的化合物或其药学上可接受的盐，如说明书中所定义，以及药学上可接受的载体、稀释剂或赋形剂。本发明还提供了抑制动物体内 MMP-13 酶的方法，包括向动物施用式 I 化合物或其药学上可接受的盐。本发明还提供了治疗患者体内由 MMP-13 酶介导的疾病的方法，包括向患者单独或在药物组合物中施用式 I 化合物或其药学上可接受的盐。本发明还提供了组合物，包括向患者单独或在药物组合物中施用式 I 化合物或其药学上可接受的盐。本发明还提供了组合物，包括式 I 化合物或其药学上可接受的盐，以及说明书中所述的另一种药学活性成分。
• US6869958B2
  申请人：——

  公开号：US6869958B2

  公开（公告）日：2005-03-22
• [EN] FUSED TETRAHYDROPYRIDINE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS<br/>[FR] DERIVES FUSIONNES DE LA TETRAHYDROPYRIDINE INHIBITEURS DE LA METALLOPROTEASE MATRICIELLE
  申请人：WARNER LAMBERT CO

  公开号：WO2004014909A1

  公开（公告）日：2004-02-19

  This invention provides compounds defined by Formula (I) or a pharmaceutically acceptable salt thereof, wherein Rl, Q, Yl, Y2, Y3, and R2 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.