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    • 9. 发明申请
    • CHROMONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS
    • CHROMONE衍生物作为基质金属蛋白酶抑制剂
    • WO2004014880A1
    • 2004-02-19
    • PCT/IB2003/003541
    • 2003-08-04
    • WARNER-LAMBERT COMPANY LLCORTWINE, Daniel, Fred
    • ORTWINE, Daniel, Fred
    • C07D265/22
    • C07D311/22C07D265/22
    • This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R 1 , Q, y 2 , y 3 , Y 4 , U 5 , U 6 , U 8 , 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 10 acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MW-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 MNIP 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.
    • 本发明提供由式I定义的化合物或其药学上可接受的盐,其中R 1,Q,y 2,y 3,Y 4,U 5,U 6, 8>和R2如说明书中所定义。 本发明还提供药物组合物,其包含本说明书中定义的式I化合物或其药学上可接受的盐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中抑制MW-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由患者中的MNIP13酶介导的疾病的方法,包括单独或在药物组合物中向患者施用式I化合物或其药学上可接受的盐。 本发明还提供了治疗诸如心脏病,多发性硬化,骨关节炎和类风湿性关节炎,除了骨关节炎或类风湿性关节炎之外的关节炎,心功能不全,炎性肠病,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,牛皮癣,动脉粥样硬化和骨质疏松症,包括单独或在药物组合物中向患者施用式I化合物或其药学上可接受的盐。 本发明还提供了包含式I化合物或其药学上可接受的盐以及说明书中描述的另一种药物活性成分的组合。
    • 10. 发明申请
    • 5,6-FUSED 3,4-DIHYDROPYRIMIDINE-2-ONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS
    • 作为基质金属蛋白酶抑制剂的5,6-FUSED 3,4-二羟基嘧啶-2-酮衍生物
    • WO2004014869A2
    • 2004-02-19
    • PCT/IB2003/003534
    • 2003-08-04
    • WARNER-LAMBERT COMPANY LLCNAHRA, JoeO'BRIEN, Patrick, MichaelORTWINE, Daniel, Fred
    • NAHRA, JoeO'BRIEN, Patrick, MichaelORTWINE, Daniel, Fred
    • C07D239/00
    • C07D231/12C07D233/56C07D239/74C07D239/80C07D249/08C07D401/06C07D401/12C07D403/06C07D405/06C07D471/04
    • This invention provides compounds defined by Formula (I), 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
    • 本发明提供式(I)所定义的化合物或其药学上可接受的盐,其中R 1,Q,Y 3,Y 4,Y 5 Y 6,Y 8, R 2和R 4如说明书中所定义。 本发明还提供包含本说明书中定义的式(I)化合物或其药学上可接受的盐以及药学上可接受的载体,稀释剂或赋形剂的药物组合物。 本发明还提供了在动物中抑制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中由MMP-13酶介导的疾病的方法,其包括向患者施用单独或药物组合物中的式(I)化合物或其药学上可接受的盐。 本发明还提供了治疗诸如心脏病,多发性硬化,骨关节炎和类风湿性关节炎,除了骨关节炎或类风湿性关节炎之外的关节炎,心功能不全,炎性肠病,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,牛皮癣,动脉粥样硬化和骨质疏松症,其包括向患者单独或在药物组合物中给予式(I)化合物或其药学上可接受的盐。 本发明还提供组合,其包含式(I)化合物或其药学上可接受的盐以及如说明书中所述的另一种药物活性成分