申请人:——
公开号:US20040224951A1
公开(公告)日:2004-11-11
This invention provides compounds defined by Formula I
1
or a pharmaceutically acceptable salt thereof,
wherein R
1
, Q, Y
5
, Y
6
, Y
8
, R
2
, R
4
, and R
7
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.
本发明提供了由公式I1定义的化合物或其药学上可接受的盐,其中R1、Q、Y5、Y6、Y8、R2、R4和R7如规范中所定义。本发明还提供了包括公式I中定义的化合物或其药学上可接受的盐的制药组合物,以及药学上可接受的载体、稀释剂或赋形剂。本发明还提供了在动物体内抑制MMP-13酶的方法,包括向动物体内给予公式I中定义的化合物或其药学上可接受的盐。本发明还提供了治疗由MMP-13酶介导的疾病的方法,包括向患者体内给予公式I中定义的化合物或其药学上可接受的盐,单独或与制药组合物一起。本发明还提供了治疗心脏病、多发性硬化症、骨关节炎、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、慢性阻塞性肺疾病、哮喘、牙周疾病、银屑病、动脉粥样硬化和骨质疏松症的方法,包括向患者体内给予公式I中定义的化合物或其药学上可接受的盐,单独或与制药组合物一起。本发明还提供了包括公式I中定义的化合物或其药学上可接受的盐和规范中描述的另一种药学活性成分的组合物。