4-[5-(5-benzylcarbamoyl-6-oxo-6H-pyridazin-1-yl)tetrazol-2-yl]benzoic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-[5-(5-benzylcarbamoyl-6-oxo-6H-pyridazin-1-yl)tetrazol-2-yl]benzoic acid
• 英文别名: 4-[5-[5-(Benzylcarbamoyl)-6-oxopyridazin-1-yl]tetrazol-2-yl]benzoic acid
• 化学式: C₂₀H₁₅N₇O₄
• 分子量: 417.384
• InChiKey: WROKSGJAVRSHTA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  31
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  143
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• Monocyclic derivatives as matrix metalloproteinase inhibitors
  申请人：——

  公开号：US20040043979A1

  公开（公告）日：2004-03-04

  This invention provides compounds defined by Formula I R 1 -Q-D-(V 1 ) m —R 2 I or a pharmaceutically acceptable salt thereof, wherein R 1 , Q, D, V 1 , m, 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 R 1 -Q-D-(V 1 ) m -R 2 I 或其药学上可接受的盐、 其中 R 1 、Q、D、V 1 m 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，连同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。
• MONOCYCLIC DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS
  申请人：Warner-Lambert Company LLC

  公开号：EP1537098A1

  公开（公告）日：2005-06-08
• US7132424B2
  申请人：——

  公开号：US7132424B2

  公开（公告）日：2006-11-07
• [EN] MONOCYCLIC DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS<br/>[FR] DERIVES MONOCYCLIQUES EN TANT QU'INHIBITEURS DE METALLOPROTEINASES MATRICIELLES
  申请人：WARNER LAMBERT CO

  公开号：WO2004014892A1

  公开（公告）日：2004-02-19

  This invention provides compounds defined by Formula (I) or a pharmaceutically acceptable salt thereof, wherein R', Q, D, V', m, 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.