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公开(公告)号:US20050143422A1
公开(公告)日:2005-06-30
申请号:US11001589
申请日:2004-12-01
申请人: Jeremy Levin , Thomas Rush , Frank Lovering , Yonghan Hu , Jianchang Li , Wei Li , Jun Wu , Rajeev Hotchandani , Jason Xiang , Xuemei Du , Derek Cole , Steve Tam
发明人: Jeremy Levin , Thomas Rush , Frank Lovering , Yonghan Hu , Jianchang Li , Wei Li , Jun Wu , Rajeev Hotchandani , Jason Xiang , Xuemei Du , Derek Cole , Steve Tam
IPC分类号: C07D209/42 , C07D231/14 , C07D235/12 , C07D235/24 , C07D261/18 , C07D263/58 , C07D277/56 , C07D277/64 , C07D277/68 , C07D285/00 , C07D285/01 , C07D307/68 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/85 , C07D307/92 , C07D333/34 , C07D333/70 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D491/06 , C07D495/04 , A61K31/445 , A61K31/4025 , A61K31/4178 , C07D43/14 , C07D49/14
CPC分类号: C07D235/24 , C07D209/42 , C07D231/14 , C07D235/12 , C07D261/18 , C07D263/58 , C07D277/56 , C07D277/64 , C07D277/68 , C07D285/01 , C07D307/68 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/85 , C07D307/92 , C07D333/34 , C07D333/70 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D491/06 , C07D495/04
摘要: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
摘要翻译: 本发明涉及联芳基磺酰胺及其作为例如金属蛋白酶抑制剂的用途。
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公开(公告)号:US20070225327A1
公开(公告)日:2007-09-27
申请号:US11756253
申请日:2007-05-31
申请人: Jason Xiang , Steve Tam , Yonghan Hu , Phaik-Eng Sum , David How , Darrin Hopper , Matthew Vera , Joshua Sabatini , Thomas Rush , Elisabeth Morris , Katy Georgiadis
发明人: Jason Xiang , Steve Tam , Yonghan Hu , Phaik-Eng Sum , David How , Darrin Hopper , Matthew Vera , Joshua Sabatini , Thomas Rush , Elisabeth Morris , Katy Georgiadis
IPC分类号: A61K31/197 , A61K31/47
CPC分类号: C07D213/30 , A61K31/4188 , A61K31/424 , A61K31/429 , C07C311/29 , C07C311/46 , C07C2601/08 , C07C2602/10 , C07D213/64 , C07D213/643 , C07D215/14 , C07D215/227 , C07D215/233 , C07D217/18 , C07D235/12 , C07D239/34 , C07D239/60 , C07D261/14 , C07D263/22 , C07D263/58 , C07D277/64 , C07D277/68 , C07D295/096 , C07D295/192 , C07D307/79 , C07D307/80 , C07D307/82 , C07D307/84 , C07D319/18 , C07D321/10 , C07D333/20 , C07D333/36 , C07D333/66
摘要: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
摘要翻译: 本发明涉及联芳基磺酰胺及其作为例如金属蛋白酶抑制剂的用途。
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公开(公告)号:US20050130973A1
公开(公告)日:2005-06-16
申请号:US11000711
申请日:2004-12-01
申请人: Jason Xiang , Steve Tam , Yonghan Hu , Phaik-Eng Sum , David How , Darrin Hopper , Matthew Vera , Joshua Sabatini , Thomas Rush , Elisabeth Morris , Katy Georgiadis
发明人: Jason Xiang , Steve Tam , Yonghan Hu , Phaik-Eng Sum , David How , Darrin Hopper , Matthew Vera , Joshua Sabatini , Thomas Rush , Elisabeth Morris , Katy Georgiadis
IPC分类号: C07C311/29 , C07C311/46 , C07D213/30 , C07D213/64 , C07D213/643 , C07D215/14 , C07D215/22 , C07D215/227 , C07D215/233 , C07D217/18 , C07D235/12 , C07D239/34 , C07D239/60 , C07D261/14 , C07D263/22 , C07D263/58 , C07D277/64 , C07D277/68 , C07D295/096 , C07D295/192 , C07D307/79 , C07D307/80 , C07D307/82 , C07D307/84 , C07D319/18 , C07D321/10 , C07D333/20 , C07D333/36 , C07D333/66 , A61K31/50 , A61K31/47 , A61K31/4965 , A61K31/505
CPC分类号: C07D213/30 , A61K31/4188 , A61K31/424 , A61K31/429 , C07C311/29 , C07C311/46 , C07C2601/08 , C07C2602/10 , C07D213/64 , C07D213/643 , C07D215/14 , C07D215/227 , C07D215/233 , C07D217/18 , C07D235/12 , C07D239/34 , C07D239/60 , C07D261/14 , C07D263/22 , C07D263/58 , C07D277/64 , C07D277/68 , C07D295/096 , C07D295/192 , C07D307/79 , C07D307/80 , C07D307/82 , C07D307/84 , C07D319/18 , C07D321/10 , C07D333/20 , C07D333/36 , C07D333/66
摘要: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
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公开(公告)号:US20070219198A1
公开(公告)日:2007-09-20
申请号:US11703522
申请日:2007-02-07
申请人: Jason Xiang , Eddine Saiah , Steve Tam , John Mckew , Lihren Chen , Manus Ipek , Katherine Lee , Huan-Qiu Li , Jianchang Li , Wei Li , Tarek Mansour , Vipin Suri , Richard Vargas , Yuchuan Wu , Zhao-Kui Wan , Jinbo Lee , Eva Binnun , Douglas Wilson
发明人: Jason Xiang , Eddine Saiah , Steve Tam , John Mckew , Lihren Chen , Manus Ipek , Katherine Lee , Huan-Qiu Li , Jianchang Li , Wei Li , Tarek Mansour , Vipin Suri , Richard Vargas , Yuchuan Wu , Zhao-Kui Wan , Jinbo Lee , Eva Binnun , Douglas Wilson
IPC分类号: A61K31/5377 , A61K31/497 , A61K31/496 , C07D413/02 , C07D403/02 , C07D409/02
CPC分类号: C07D211/96 , C07D295/26 , C07D401/04 , C07D403/02 , C07D409/02 , C07D413/02
摘要: This invention relates to inhibiting 11βHSD1.
摘要翻译: 本发明涉及抑制11betaHSD1。
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公开(公告)号:US20060025445A1
公开(公告)日:2006-02-02
申请号:US11196643
申请日:2005-08-02
申请人: Jason Xiang , John McKew , Steve Tam , Manus Ipek , Vipin Suri , Tarek Mansour
发明人: Jason Xiang , John McKew , Steve Tam , Manus Ipek , Vipin Suri , Tarek Mansour
IPC分类号: A61K31/445 , A61K31/40 , A61K31/381
CPC分类号: C07C311/16 , C07C311/03 , C07C311/29 , C07D233/84 , C07D261/10 , C07D307/64 , C07D333/22 , C07D333/34
摘要: This invention relates to inhibiting 11-beta HSD1.
摘要翻译: 本发明涉及抑制11-βHSD1。
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公开(公告)号:US20070043066A1
公开(公告)日:2007-02-22
申请号:US11484005
申请日:2006-07-11
申请人: Phaik-Eng Sum , David How , Joshua Sabatini , Jason Xiang , Manus Ipek , Eric Feyfant
发明人: Phaik-Eng Sum , David How , Joshua Sabatini , Jason Xiang , Manus Ipek , Eric Feyfant
IPC分类号: A61K31/505 , A61K31/44 , A61K31/381 , A61K31/34 , A61K31/198 , A61K31/165
CPC分类号: C07D213/82 , C07B2200/07 , C07C231/16 , C07C233/83 , C07C235/84 , C07C237/22 , C07C237/42 , C07C259/06 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2603/18 , C07C2603/74 , C07D213/38 , C07D239/26 , C07D239/42 , C07D277/30 , C07D307/52 , C07D307/68 , C07D307/79 , C07D307/85 , C07D317/58 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/38 , C07D409/04
摘要: The present invention relates to modulators of metalloproteinase activity.
摘要翻译: 本发明涉及金属蛋白酶活性的调节剂。
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公开(公告)号:US20060004066A1
公开(公告)日:2006-01-05
申请号:US10983981
申请日:2004-11-08
申请人: Elisabeth Morris , Sonya Glasson , Jason Xiang
发明人: Elisabeth Morris , Sonya Glasson , Jason Xiang
IPC分类号: A61K31/429 , A61K31/424 , A61K31/4188
CPC分类号: C07D213/30 , A61K31/4188 , A61K31/424 , A61K31/429 , C07C311/29 , C07C311/46 , C07C2601/08 , C07C2602/10 , C07D213/64 , C07D213/643 , C07D215/14 , C07D215/227 , C07D215/233 , C07D217/18 , C07D235/12 , C07D239/34 , C07D239/60 , C07D261/14 , C07D263/22 , C07D263/58 , C07D277/64 , C07D277/68 , C07D295/096 , C07D295/192 , C07D307/79 , C07D307/80 , C07D307/82 , C07D307/84 , C07D319/18 , C07D321/10 , C07D333/20 , C07D333/36 , C07D333/66
摘要: The present invention relates to methods of treating ADAMTS-5-associated diseases and particularly osteoarthritis comprising administering an agent capable of modulating ADMATS-5 activity to a subject afflicted with the disease. The agent is preferably a biaryl sulfonamide compound. The invention is based, in part, on the discovery that transgenic animals that do not express functional ADAMTS-5 show a reduction in the degree of osteoarthritis after the induction of osteoarthritis as compared to WT animals. Furthermore, the ADAMTS-5 transgenic animals have reduced aggrecanase activity in articular tissue as compared to WT animals. These animals are good models for ADAMTS-5-associated diseases, and for screening of drugs useful in the treatment and/or prevention of these diseases. There are no other animal models in which the deletion of the activity of a single gene is capable of abrogating the course of osteoarthritis. Accordingly, these animals also show that osteoarthritis can be prevented and/or treated by administering to a subject an ADAMTS-5 inhibitory agent and particularly an agent capable of inhibiting the aggrecanase activity of ADAMTS-5.
摘要翻译: 本发明涉及治疗ADAMTS-5相关疾病,特别是骨关节炎的方法,其包括将能够将ADMATS-5活性调节至患有该疾病的受试者的药剂。 该试剂优选为联芳基磺酰胺化合物。 本发明部分地基于以下发现:与WT动物相比,不表达功能性ADAMTS-5的转基因动物在诱导骨关节炎之后表现出降低骨关节炎的程度。 此外,ADAMTS-5转基因动物与WT动物相比降低了关节组织中的聚集蛋白聚糖蛋白聚糖酶活性。 这些动物是ADAMTS-5相关疾病的良好模型,并且用于筛选可用于治疗和/或预防这些疾病的药物。 没有其他动物模型,其中单个基因的活性的缺失能够消除骨关节炎的过程。 因此,这些动物还显示可以通过向受试者施用ADAMTS-5抑制剂,特别是能够抑制ADAMTS-5的聚集蛋白聚糖酶活性的试剂来预防和/或治疗骨关节炎。
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