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1. 发明申请

WO2003032999A1 ALKYNE MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： ALKYNE MATRIX金属蛋白酶抑制剂
公开(公告)号：WO2003032999A1
公开(公告)日：2003-04-24
申请号：PCT/IB2002/003057
申请日：2002-08-02
申请人： WARNER-LAMBERT COMPANY LLC , BUNKER, Amy, Mae , HARTER, William, Glen , HICKS, James, Lester , O'BRIEN, Patrick, Michael , PHAM, Ly, Thi , PICARD, Joseph, Armand , ROARK, William, Howard
发明人： BUNKER, Amy, Mae , HARTER, William, Glen , HICKS, James, Lester , O'BRIEN, Patrick, Michael , PHAM, Ly, Thi , PICARD, Joseph, Armand , ROARK, William, Howard
IPC分类号： A61K31/549
CPC分类号： C07D213/40 , C07C233/87 , C07C235/42 , C07C255/57 , C07C255/60 , C07C311/46 , C07C317/32 , C07D213/56 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/233 , C07D231/12 , C07D233/56 , C07D249/04 , C07D249/08 , C07D279/02 , C07D285/16 , C07D285/24 , C07D291/08 , C07D401/06 , C07D495/04 , C07D513/04 , C07D515/04
摘要： A compound of Formula (I) or a pharmaceutical acceptable salt thereof, or a tautomer thereof, wherein G 1 , G 2 , and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.
摘要翻译：式（I）化合物或其药学上可接受的盐或其互变异构体，其中G1，G2和B如本申请中所定义，是MMP-13的选择性抑制剂。该化合物可用于治疗由MMP-13介导的疾病，包括癌症和关节炎。

2. 发明申请

WO2002064599A1 BICYCLIC PYRIMIDINE MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：双相PYRIMININE MATRIX金属蛋白酶抑制剂
公开(公告)号：WO2002064599A1
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000313
申请日：2002-01-30
申请人： WARNER-LAMBERT COMPANY , DYER, Richard, Dennis , HARTER, William, Glen , HICKS, James, Lester , JOHNSON, Adam, Richard , LI, Jie, Jack , ROARK, William, Howard , SHULER, Kevon, Ray
发明人： DYER, Richard, Dennis , HARTER, William, Glen , HICKS, James, Lester , JOHNSON, Adam, Richard , LI, Jie, Jack , ROARK, William, Howard , SHULER, Kevon, Ray
IPC分类号： C07D513/04
CPC分类号： C07D487/04 , C07D513/04
摘要： Selective MMP-13 inhibitors are bicyclic pyrmidines of the formula or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen or alkyl; R 2 , R 3 , and R 4 include hydrogen, halo, alkyl, C≡C(CH 2 ) m aryl; and X is O, S, SO, SO 2 , CH 2 , C=O, CHOH, NH, OR NR 5 . A compound of the formula, or a pharmaceutically acceptable salt thereof, is useful for treating cancer or arthritis.
摘要翻译：选择性MMP-13抑制剂是下式的双环哒嗪或其药学上可接受的盐，其中R 1是氢或烷基; R 2，R 3和R 4包括氢，卤素，烷基，C（CH 2）m芳基; 并且X是O，S，SO，SO 2，CH 2，C = O，CHOH，NH或NR 5。下式的化合物或其药学上可接受的盐可用于治疗癌症或关节炎。

3. 发明申请

WO2004092132A1 [B]-FUSED BICYCLIC PROLINE DERIVATIVES AND THEIR USE FOR TREATING ARTHRITIC CONDITIONS 审中-公开
标题翻译： [B] - 双体双酚A衍生物及其用于治疗ARTHRITIC条件的用途
公开(公告)号：WO2004092132A1
公开(公告)日：2004-10-28
申请号：PCT/IB2004/001206
申请日：2004-04-05
申请人： WARNER-LAMBERT COMPANY LLC , BARVIAN, Nicole, Chantel , CONNOLLY, Cleo, J., Chivikas , GUZZO, Peter, Robert , HAMBY, James, Marino , HICKS, James, Lester , JOHNSON, Matthew, Robert , LE, Van-Duc , MITCHELL, Lorna, Helen , ROARK, William, Howard
发明人： BARVIAN, Nicole, Chantel , CONNOLLY, Cleo, J., Chivikas , GUZZO, Peter, Robert , HAMBY, James, Marino , HICKS, James, Lester , JOHNSON, Matthew, Robert , LE, Van-Duc , MITCHELL, Lorna, Helen , ROARK, William, Howard
IPC分类号： C07D209/12
CPC分类号： C07D495/04 , C07D209/12 , C07D209/14 , C07D403/04 , C07D413/04 , C07D417/02
摘要： The invention relates to a compound which is [b]-fused bicyclic proline derivative, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising the compound or the salt thereof, and methods of treating diseases, including, but not limited to, methods of preventing or inhibiting joint cartilage damage and preventing or treating diseases characterized by joint cartilage damage, joint inflammation, or joint pain. The [b]-fused bicyclic proline derivatives are compounds of Formula I as described above. Diseases characterized by joint cartilage damage or joint pain include, for example, osteoarthritis and rheumatoid arthritis. Rheumatoid arthritis is also characterized by joint inflammation. This invention also relates to methods of synthesizing and preparing the [b]-fused bicyclic proline derivatives, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及[b]双环脯氨酸衍生物或其药学上可接受的盐的化合物; 包含该化合物或其盐的药物组合物和治疗疾病的方法，包括但不限于预防或抑制关节软骨损伤和预防或治疗以关节软骨损伤，关节炎症或关节疼痛为特征的疾病的方法。 [b]引发的双环脯氨酸衍生物是如上所述的式I化合物。以关节软骨损伤或关节疼痛为特征的疾病包括例如骨关节炎和类风湿性关节炎。类风湿性关节炎的特征还在于关节炎。本发明还涉及合成和制备[b] - 双环脯氨酸衍生物或其药学上可接受的盐的方法。

4. 发明申请

WO2004014868A2 PYRIMIDINE-2,4-DIONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：嘧啶-2,4-二酮衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2004014868A2
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003525
申请日：2003-08-04
申请人： WARNER-LAMBERT COMPANY LLC , HICKS, James, Lester , ROARK, William, Howard
发明人： HICKS, James, Lester , ROARK, William, Howard
IPC分类号： C07D239/00
CPC分类号： C07D401/12 , C07D239/60 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R l , Q, R 2 , R 3 , 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：本发明提供了由式I定义的化合物或其药学上可接受的盐，其中R 1，Q，R 2，R 4， 3和R 4如说明书中所定义。本发明还提供了药物组合物，其包含如说明书中所定义的式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。本发明还提供了抑制动物中MMP-13酶的方法，包括给动物施用式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，包括向患者单独或在药物组合物中给予患者式I化合物或其药学上可接受的盐。本发明还提供治疗诸如心脏病，多发性硬化症，骨关节炎和类风湿性关节炎，除骨关节炎或类风湿性关节炎以外的关节炎，心功能不全，炎性肠病，心力衰竭，年龄相关性黄斑变性，慢性阻塞性肺病疾病，哮喘，牙周病，牛皮癣，动脉粥样硬化和骨质疏松症的方法，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学活性组分的组合。

5. 发明申请

WO2004014388A1 6,6-FUSED HETEROARYL DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：作为基质金属蛋白酶抑制剂的6,6-融合异构体衍生物
公开(公告)号：WO2004014388A1
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003494
申请日：2003-08-04
申请人： WARNER-LAMBERT COMPANY LLC , HICKS, James, Lester , ROARK, William, Howard
发明人： HICKS, James, Lester , ROARK, William, Howard
IPC分类号： A61K31/5415
CPC分类号： C07D279/02
摘要： This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein Rl, Q, Yl, Y2, Y3, R 2a, 0, Rs, and n 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 NIMP-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：本发明提供由式I定义的化合物或其药学上可接受的盐，其中R1，Q，Y1，Y2，Y3，R 2a，O，R和n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。本发明还提供了抑制动物中NIMP-13酶的方法，其包括向动物施用式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。

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