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    Tricyclic heteroaromatics and their derivatives as inhibitors of matrix metalloproteinases
    11.
    发明授权
    Tricyclic heteroaromatics and their derivatives as inhibitors of matrix metalloproteinases 失效
    三环异构体及其衍生物作为基质金属蛋白酶抑制剂

    公开(公告)号：US06350885B1

    公开(公告)日：2002-02-26

    申请号：US09719026

    申请日：2001-02-20

    申请人： Patrick Michael O'Brien ,  Joseph Armand Picard ,  Drago Robert Sliskovic

    发明人： Patrick Michael O'Brien ,  Joseph Armand Picard ,  Drago Robert Sliskovic

    IPC分类号： C07D30791

    CPC分类号： C07D209/80 ,  C07C59/86 ,  C07D209/86 ,  C07D209/94 ,  C07D233/78 ,  C07D307/91 ,  C07D333/76

    摘要： Tricyclic heteroaromatic compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, renal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

    摘要翻译： 描述了三环杂芳族化合物和衍生物以及其制备方法及其药物组合物，其可用作基质金属蛋白酶抑制剂，特别是明胶酶A，胶原酶-3和溶基质蛋白酶-1以及治疗多发性硬化，动脉粥样硬化 斑块破裂，主动脉瘤，心力衰竭，左心室扩张，再狭窄，牙周病，角膜溃疡，烧伤治疗，褥疮溃疡，伤口愈合，癌症，炎症，疼痛，关节炎，骨质疏松症，肾脏疾病或其他自身免疫性或炎症性疾病 依赖于白细胞或其他活化的迁移细胞的组织侵袭，急性和慢性神经变性疾病，包括中风，头部创伤，脊髓损伤，阿尔茨海默病，肌萎缩性侧索硬化，脑淀粉样血管病，艾滋病，帕金森病，亨廷顿病，朊病毒疾病，肌无力 重症肌无力和Duchenne肌营养不良症。

    6,5-Fused bicyclic heterocycles
    12.
    发明授权
    6,5-Fused bicyclic heterocycles 失效
    6,5-稠合双环杂环

    公开(公告)号：US06943174B2

    公开(公告)日：2005-09-13

    申请号：US10362353

    申请日：2001-05-09

    申请人： Joseph Armand Picard ,  William Howard Roark ,  Drago Robert Sliskovic

    发明人： Joseph Armand Picard ,  William Howard Roark ,  Drago Robert Sliskovic

    IPC分类号： A61K31/437 ,  A61P9/00 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D209/10 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D209/10 ,  C07D487/04

    摘要： The present invention provides compounds of Formula (I) wherein Q1, Q2, Q3, Q4, Y1, Y2, and Z are as defined in the description, and pharmaceutically acceptable salts thereof, and C1-C8 alkyl esters thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of Formula (I) and their pharmaceuticalyl acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.

    摘要翻译： 本发明提供式（I）的化合物，其中Q 1，Q 2，Q 3，Q 4， ，Y 1，Y 2和Z如说明书中所定义，及其药学上可接受的盐，和C 1 -C 3 它们可用于治疗对抑制酶15-脂肪氧合酶有响应的疾病。 因此，式（I）化合物及其药学上可接受的盐可用于治疗具有炎性成分的疾病，包括动脉粥样硬化，涉及单核细胞趋化性疾病，炎症，中风，冠状动脉疾病，哮喘，关节炎，结肠直肠癌和牛皮癣的疾病 。

    Matrix metalloproteinase inhibitors and their therapeutic uses
    14.
    发明授权
    Matrix metalloproteinase inhibitors and their therapeutic uses 失效
    基质金属蛋白酶抑制剂及其治疗用途

    公开(公告)号：US06624177B1

    公开(公告)日：2003-09-23

    申请号：US09254384

    申请日：1999-03-02

    申请人： Patrick Michael O'Brien ,  Joseph Armand Picard ,  Drago Robert Sliskovic ,  Andrew David White

    发明人： Patrick Michael O'Brien ,  Joseph Armand Picard ,  Drago Robert Sliskovic ,  Andrew David White

    IPC分类号： C07D20982

    CPC分类号： C07D307/91 ,  A61K31/343 ,  A61K31/381 ,  C07C311/19 ,  C07C2603/18 ,  C07D333/76

    摘要： The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix melatoproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.

    摘要翻译： 本发明涉及使用具有式IIIO的二苯并呋喃磺酰胺衍生物的化合物抑制基质金属蛋白酶的方法，本发明涉及一种治疗涉及多发性硬化症，动脉粥样硬化斑块破裂，再狭窄的基质蛋白酶的疾病的方法 ，主动脉瘤，心力衰竭，牙周病，角膜溃疡，烧伤，褥疮性溃疡，慢性溃疡或创伤，癌症转移，肿瘤血管生成，关节炎或依赖于白细胞组织侵袭的其他自身免疫性或炎性疾病。

    Fluorinated butyric acids and their derivatives as inhibitors of matrix metalloproteinases
    18.
    发明授权
    Fluorinated butyric acids and their derivatives as inhibitors of matrix metalloproteinases 失效
    氟化丁酸及其衍生物作为基质金属蛋白酶的抑制剂

    公开(公告)号：US06037361A

    公开(公告)日：2000-03-14

    申请号：US36751

    申请日：1998-03-09

    申请人： Bruce David Roth ,  Patrick Michael O'Brien ,  Drago Robert Sliskovic

    发明人： Bruce David Roth ,  Patrick Michael O'Brien ,  Drago Robert Sliskovic

    IPC分类号： A61K31/192 ,  A61K31/343 ,  A61K31/381 ,  C07C59/88 ,  C07C251/48 ,  C07C259/06 ,  C07D209/86 ,  C07D307/91 ,  C07D333/76 ,  C07D405/06 ,  A01N43/38

    CPC分类号： C07D307/91 ,  A61K31/192 ,  A61K31/343 ,  A61K31/381 ,  C07C251/48 ,  C07C259/06 ,  C07C59/88 ,  C07D209/86 ,  C07D333/76 ,  C07D405/06 ,  C07C2103/18 ,  Y10S514/825 ,  Y10S514/885 ,  Y10S514/903

    摘要： Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

    摘要翻译： 描述了氟化丁酸化合物和衍生物以及用于制备的酸法和其药物组合物，其可用作基质金属蛋白酶抑制剂，特别是明胶酶A（72kD明胶酶）和基质溶素-1，以及胶原酶，基质溶素， 和MMP-13，用于治疗多发性硬化，动脉粥样硬化斑块破裂，主动脉瘤，心力衰竭，再狭窄，牙周病，角膜溃疡，烧伤治疗，褥疮溃疡，伤口愈合，癌症，炎症，疼痛，关节炎或 依赖于白细胞或其他活化迁移细胞的组织侵袭的其它自身免疫性或炎性病症，急性和慢性神经变性疾病，包括中风，头部创伤，脊髓损伤，阿尔茨海默氏病，肌萎缩性侧索硬化，脑淀粉样血管病，艾滋病，帕金森病，亨廷顿舞蹈病 ，朊病毒疾病，重症肌无力和杜氏肌营养不良症。

    Biphenyl sulfonamides useful as matrix metalloproteinase inhibitors
    20.
    发明授权
    Biphenyl sulfonamides useful as matrix metalloproteinase inhibitors 失效
    联苯磺酰胺可用作基质金属蛋白酶抑制剂

    公开(公告)号：US06686355B2

    公开(公告)日：2004-02-03

    申请号：US10074667

    申请日：2002-02-13

    申请人： Nicole Chantel Barvian ,  Patrick Michael O'Brien ,  William Chester Patt ,  Drago Robert Sliskovic

    发明人： Nicole Chantel Barvian ,  Patrick Michael O'Brien ,  William Chester Patt ,  Drago Robert Sliskovic

    IPC分类号： C07D27912

    CPC分类号： C07D417/12 ,  C07D279/12

    摘要： Inhibitors of MMP enzymes are cyclic sulfonamides of Formula I or a pharmaceutically acceptable salt thereof, and cyclic sulfonamides of Formula III or a pharmaceutically acceptable salt thereof, wherein R1 and R2 include hydrogen, alkyl, and substituted alkyl; R3 and R4 include hydrogen, halo, and alkyl; X is OH or NHOH: Z is (CH2)n: and Y is S, SO or SO2. The compounds of Formulas I and III are useful for the treatment of diseases mediated by an MMP enzyme, including cancer, osteoarthritis, rheumatoid arthritis, heart failure, and inflammation.

    摘要翻译： MMP酶的抑制剂是式I的环状磺酰胺或其药学上可接受的盐，以及式III的环状磺酰胺或其药学上可接受的盐，其中R 1和R 2包括氢，烷基和取代的烷基; R 3和R 4包括氢，卤素和烷基; X是OH或NHOH：Z是（CH 2）n：Y是S，SO或SO 2。 式I和III的化合物可用于治疗由MMP酶介导的疾病，包括癌症，骨关节炎，类风湿性关节炎，心力衰竭和炎症。