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    THIENO'2,3-D PYRIMIDINDIONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS
    5.
    发明申请
    THIENO'2,3-D PYRIMIDINDIONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
    THIENO'2,3-D吡啶衍生物作为基质金属蛋白酶抑制剂

    公开(公告)号：WO2002064598A1

    公开(公告)日：2002-08-22

    申请号：PCT/IB2002/000204

    申请日：2002-01-18

    申请人： WARNER-LAMBERT COMPANY ,  HARTER, William, Glen ,  LI, Jie, Jack ,  ORTWINE, Daniel, Fred ,  SHULER, Kevon, Ray ,  YUE, Wen-Song

    发明人： HARTER, William, Glen ,  LI, Jie, Jack ,  ORTWINE, Daniel, Fred ,  SHULER, Kevon, Ray ,  YUE, Wen-Song

    IPC分类号： C07D495/04

    CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D491/04 ,  C07D495/04

    摘要： Selective MMP-13 inhibitors are fused pyrimidinones of the formula or a pharmaceutically acceptable salt thereof, wherein: W, together with the carbon atoms to which it is attached, form a 5-membered ring diradical Y is O, S, SO, SO 2 , NR 5 , or CH¿2, ?A is-C-or S-; B is O or NR 5 ; or A and B are taken together to form -C≡C-; R 1 , R 4 , and R 5 are hydrogen, alkyl, alkenyl, alkynyl, (CH 2 ) n aryl, (CH 2 ) n cycloalkyl, C 1 C 6 alkanoyl, or (CH 2 ) n heteroaryl; R 2 and R 3 are hydrogen, alkyl, alkenyl, alkynyl CN, NO 2 , NR 4 R 5 , (CH 2 ) n cycloalkyl, (CH 2 ) n aryl, or (CH 2 ) n heteroaryl; R 2 may further be halo; n is an integer of from 0 to 5; and R 4 and R 5 when taken together with the nitrogen to which they are attached complete a 3-to 8-membered ring containing carbon atoms and optionally containing O, S, or N, and substituted or unsubstituted; with the proviso that R?1 ¿and R 3 are not both selected from hydrogen and C 1- C 6 alkyl.

    摘要翻译： 选择性MMP-13抑制剂是下式的稠合嘧啶酮或其药学上可接受的盐，其中：W与其连接的碳原子一起形成5元环双基Y是O，S，SO，SO 2， NR 5，或CH 2，A是-C-或S-; B是O或NR 5; 或A和B一起形成-CC-; R 1，R 4和R 5是氢，烷基，烯基，炔基，（CH 2）n芳基，（CH 2）n环烷基，C 1 -C 6烷酰基或（CH 2）n杂芳基; R 2和R 3是氢，烷基，烯基，炔基CN，NO 2，NR 4 R 5，（CH 2）n环烷基，（CH 2）n芳基或（CH 2）n杂芳基; R 2还可以是卤素; n为0〜5的整数。 和R 4和R 5与它们所连接的氮原子一起形成含有碳原子的3-8元环，任选地含有O，S或N以及取代或未取代的; 条件是R 1和R 3不都选自氢和C 1 -C 6烷基。

    CHROMONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS
    9.
    发明申请
    CHROMONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
    CHROMONE衍生物作为基质金属蛋白酶抑制剂

    公开(公告)号：WO2004014880A1

    公开(公告)日：2004-02-19

    申请号：PCT/IB2003/003541

    申请日：2003-08-04

    申请人： WARNER-LAMBERT COMPANY LLC ,  ORTWINE, Daniel, Fred

    发明人： ORTWINE, Daniel, Fred

    IPC分类号： C07D265/22

    CPC分类号： C07D311/22 ,  C07D265/22

    摘要： 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.

    摘要翻译： 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。

    5,6-FUSED 3,4-DIHYDROPYRIMIDINE-2-ONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS
    10.
    发明申请
    5,6-FUSED 3,4-DIHYDROPYRIMIDINE-2-ONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
    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

    公开(公告)号：WO2004014869A2

    公开(公告)日：2004-02-19

    申请号：PCT/IB2003/003534

    申请日：2003-08-04

    申请人： WARNER-LAMBERT COMPANY LLC ,  NAHRA, Joe ,  O'BRIEN, Patrick, Michael ,  ORTWINE, Daniel, Fred

    发明人： NAHRA, Joe ,  O'BRIEN, Patrick, Michael ,  ORTWINE, Daniel, Fred

    IPC分类号： C07D239/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D239/74 ,  C07D239/80 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D471/04

    摘要： 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

    摘要翻译： 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