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公开(公告)号：US06900223B2
公开(公告)日：2005-05-31
申请号：US10629227
申请日：2003-07-28
申请人： Neal Jeffrey Green , Steve Yikkai Tam , Jason Shaoyun Xiang , Audrey Molina Davies , Lihren Chen , Gary Paul Stack
发明人： Neal Jeffrey Green , Steve Yikkai Tam , Jason Shaoyun Xiang , Audrey Molina Davies , Lihren Chen , Gary Paul Stack
IPC分类号： C07D471/14 , A61K31/437 , A61P37/00
CPC分类号： C07D471/14
摘要： The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection, autoimmune disease or graft vs. host disease.
摘要翻译： 本发明提供式I化合物及其用于免疫治疗移植排斥反应，自身免疫性疾病或移植物抗宿主病的用途。
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公开(公告)号：US06734190B2
公开(公告)日：2004-05-11
申请号：US10629276
申请日：2003-07-28
IPC分类号： A61K31437
CPC分类号： C07D471/14 , A61K31/4745 , A61K31/55
摘要： The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection or autoimmune disease.
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![Dihydropyrazolo[3,4-d]thieno[2,3-B]pyridinone inhibitors of B7-1](/abs-image/US/2004/12/21/US06833374B2/abs.jpg.150x150.jpg)
3.发明授权Dihydropyrazolo[3,4-d]thieno[2,3-B]pyridinone inhibitors of B7-1 失效B7-1的二氢吡唑并[3,4-d]噻吩并[2,3-B]吡啶酮抑制剂公开(公告)号：US06833374B2
公开(公告)日：2004-12-21
申请号：US10629022
申请日：2003-07-28
IPC分类号： A61K314353
CPC分类号： C07D495/14 , A61K31/4745
摘要： The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection, autoimmune disease or graft vs. host disease.
摘要翻译： 本发明提供式I化合物及其用于免疫治疗移植排斥反应，自身免疫性疾病或移植物抗宿主病的用途。
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公开(公告)号：US20100029648A1
公开(公告)日：2010-02-04
申请号：US12539232
申请日：2009-08-11
申请人： Jason Shaoyun Xiang , Eddine Saiah , Steve Y. Tam , John C. McKew , Lihren Chen , Manus Ipek , Katherine Lee , Huan-Qiu Li , Jianchang Li , Wei Li , Tarek Suhayl Mansour , Vipin Suri , Richard Vargas , Yuchuan Wu , Zhao-Kui Wan , Jinbo Lee , Eva Binnun , Douglas P. Wilson
发明人： Jason Shaoyun Xiang , Eddine Saiah , Steve Y. Tam , John C. McKew , Lihren Chen , Manus Ipek , Katherine Lee , Huan-Qiu Li , Jianchang Li , Wei Li , Tarek Suhayl Mansour , Vipin Suri , Richard Vargas , Yuchuan Wu , Zhao-Kui Wan , Jinbo Lee , Eva Binnun , Douglas P. Wilson
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/4965 , A61K31/4545
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：US07632838B2
公开(公告)日：2009-12-15
申请号：US11703522
申请日：2007-02-07
申请人： Jason Shaoyun Xiang , Eddine Saiah , Steve Y. Tam , John C. Mckew , Lihren Chen , Manus Ipek , Huan-Qiu Li , Jianchang Li , Wei Li , Tarek Suhayl Mansour , Vipin Suri , Yuchuan Wu , Zhao-Kui Wan , Jinbo Lee , Eva Binnun , Douglas P. Wilson
发明人： Jason Shaoyun Xiang , Eddine Saiah , Steve Y. Tam , John C. Mckew , Lihren Chen , Manus Ipek , Huan-Qiu Li , Jianchang Li , Wei Li , Tarek Suhayl Mansour , Vipin Suri , Yuchuan Wu , Zhao-Kui Wan , Jinbo Lee , Eva Binnun , Douglas P. Wilson
IPC分类号： A61K31/4965 , C07D241/04 , C07D295/00
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：US07906548B2
公开(公告)日：2011-03-15
申请号：US12539074
申请日：2009-08-11
申请人： John C. McKew , Steve Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark L. Behnke , Baihua Hu , James D. Clark , Wei Li , Valerie Clerin , Suzana Marusic , Kevin Pong
发明人： John C. McKew , Steve Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark L. Behnke , Baihua Hu , James D. Clark , Wei Li , Valerie Clerin , Suzana Marusic , Kevin Pong
IPC分类号： A01N43/38
CPC分类号： A61K31/505 , C07D209/14 , C07D209/16 , C07D209/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/10
摘要： This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.
摘要翻译： 本发明提供了使用通式的取代的吲哚化合物及其药学上可接受的盐形式的方法。 本发明提供了使用化合物作为各种磷脂酶，特别是磷脂酶A2酶的活性的抑制剂的方法，以及用于医学治疗，预防和抑制疾病和病症，包括哮喘，中风，动脉粥样硬化，多发性硬化，帕金森病， 关节炎疾病，风湿病，中风引起的中枢神经系统损伤，由缺血引起的中枢神经系统损伤，由创伤引起的中枢神经系统损伤，由前列腺素引起或增强的炎症，由白细胞三烯引起或增强的炎症，血小板引起或增强的炎症 活化因子，由前列腺素引起或增强的疼痛，由白三烯引起或加剧的疼痛，以及血小板激活因子引起或增强的疼痛。
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公开(公告)号：US20060014759A1
公开(公告)日：2006-01-19
申请号：US11140390
申请日：2005-05-27
申请人： John McKew , Steven Tam , Katherine Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James Clark , Wei Li , Valerie Clerin , Suzana Marusic , Kevin Pong
发明人： John McKew , Steven Tam , Katherine Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James Clark , Wei Li , Valerie Clerin , Suzana Marusic , Kevin Pong
IPC分类号： A61K31/505 , C07D239/02
CPC分类号： A61K31/505 , C07D209/14 , C07D209/16 , C07D209/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/10
摘要： This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.
摘要翻译： 本发明提供了使用通式的取代的吲哚化合物及其药学上可接受的盐形式的方法。 本发明提供了使用化合物作为各种磷脂酶，特别是磷脂酶2酶的活性抑制剂的方法，以及用于治疗，预防和抑制疾病和病症的方法，包括哮喘，中风， 动脉粥样硬化，多发性硬化，帕金森病，关节炎疾病，风湿病，由中风引起的中枢神经系统损伤，由缺血引起的中枢神经系统损伤，由创伤引起的中枢神经系统损伤，由前列腺素引起或增强的炎症，由...引起或增强的炎症 白细胞三烯，血小板活化因子引起或增强的炎症，前列腺素引起或加剧的疼痛，白细胞三烯引起或增强的疼痛，以及血小板激活因子引起或增强的疼痛。
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公开(公告)号：US06797708B2
公开(公告)日：2004-09-28
申请号：US10302636
申请日：2002-11-22
申请人： John C. McKew , Steven Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James D. Clark
发明人： John C. McKew , Steven Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James D. Clark
IPC分类号： C07D40106
CPC分类号： C07D209/14 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/10
摘要： This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.
摘要翻译： 本发明提供以下通式的取代的吲哚化合物及其药学上可接受的盐形式，以及使用该化合物作为各种磷脂酶，特别是磷脂酶A2酶的活性抑制剂以及用于治疗，预防和抑制疼痛的方法 和炎症。
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公开(公告)号：US08283373B2
公开(公告)日：2012-10-09
申请号：US12488182
申请日：2009-06-19
申请人： John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
发明人： John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
IPC分类号： A61K31/404
CPC分类号： C07D209/14 , C07D209/18
摘要： This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLA2α). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.
摘要翻译： 本发明提供各种磷脂酶，特别是细胞溶质磷脂酶A2酶（cPLA2）的活性的化学抑制剂，更具体地包括胞浆磷脂酶A2α酶（cPLA2α）的抑制剂。 在一些实施方案中，抑制剂具有式I：其中组成变量如本文所定义。
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公开(公告)号：US07605156B2
公开(公告)日：2009-10-20
申请号：US11140390
申请日：2005-05-27
申请人： John C. McKew , Steve Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark L. Behnke , Baihua Hu , James D. Clark , Wei Li , Valerie Clerin , Suzana Marusic , Kevin Pong
发明人： John C. McKew , Steve Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark L. Behnke , Baihua Hu , James D. Clark , Wei Li , Valerie Clerin , Suzana Marusic , Kevin Pong
IPC分类号： A61K31/54
CPC分类号： A61K31/505 , C07D209/14 , C07D209/16 , C07D209/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/10
摘要： This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.
摘要翻译： 本发明提供了使用通式的取代的吲哚化合物及其药学上可接受的盐形式的方法。 本发明提供了使用化合物作为各种磷脂酶，特别是磷脂酶A2酶的活性的抑制剂的方法，以及用于医学治疗，预防和抑制疾病和病症，包括哮喘，中风，动脉粥样硬化，多发性硬化，帕金森病， 关节炎疾病，风湿病，中风引起的中枢神经系统损伤，由缺血引起的中枢神经系统损伤，由创伤引起的中枢神经系统损伤，由前列腺素引起或增强的炎症，由白细胞三烯引起或增强的炎症，血小板引起或增强的炎症 活化因子，由前列腺素引起或增强的疼痛，由白三烯引起或加剧的疼痛，以及血小板激活因子引起或增强的疼痛。
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