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公开(公告)号:US20100035957A1
公开(公告)日:2010-02-11
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: A61K31/405 , A61P9/10 , A61P25/28
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: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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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:US08329675B2
公开(公告)日:2012-12-11
申请号:US13049779
申请日:2011-03-16
申请人: Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
摘要: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
摘要翻译: 本发明提供由式(I),(II)或(III)包含的化合物及其药物组合物。 本发明还提供了通过向患者施用治疗有效量的所提供的式(I),(II)或(III)化合物或其药物组合物来治疗FAAH介导的疾病,病症或病症的方法。 需要它。 此外,本发明提供了通过向有需要的患者施用治疗有效量的式(I),(II)或(III)化合物或其药物组合物来抑制患者的FAAH的方法。
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公开(公告)号:US20110224171A1
公开(公告)日:2011-09-15
申请号:US13049779
申请日:2011-03-16
申请人: Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号: A61K31/69 , A61P29/00 , A61P37/00 , A61P25/24 , A61P25/02 , A61P25/00 , A61P27/06 , A61P9/00 , A61P25/06
摘要: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
摘要翻译: 本发明提供由式(I),(II)或(III)包含的化合物及其药物组合物。 本发明还提供了通过向患者施用治疗有效量的所提供的式(I),(II)或(III)化合物或其药物组合物来治疗FAAH介导的疾病,病症或病症的方法。 需要它。 此外,本发明提供了通过向有需要的患者施用治疗有效量的式(I),(II)或(III)化合物或其药物组合物来抑制患者的FAAH的方法。
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公开(公告)号:US20110034437A1
公开(公告)日:2011-02-10
申请号:US12782658
申请日:2010-05-18
申请人: Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号: A61K31/55 , C07D261/20 , A61K31/42 , A61K31/438 , C07D498/10 , A61P25/00 , A61P3/00 , A61P9/00 , A61P1/08 , A61P25/28 , A61P25/30 , A61P25/20 , A61P3/04
CPC分类号: C07D498/10 , A61K31/42 , A61K31/438 , A61K31/55 , C07D261/20 , C07D498/04
摘要: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient.The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
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公开(公告)号:US20110028482A1
公开(公告)日:2011-02-03
申请号:US12782655
申请日:2010-05-18
申请人: Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号: A61K31/498 , C07D413/04 , A61K31/42 , C07D417/14 , A61K31/4439 , C07D401/14 , A61K31/506 , A61K31/427 , C07D401/04 , A61K31/454 , C07D413/06 , A61K31/496 , C07D417/10 , A61K31/428 , C07D403/10 , C07D401/10 , A61K31/4709 , A61P1/00 , A61P3/00 , A61P9/00 , A61P17/00 , A61P25/00 , A61P27/06 , A61P29/00
CPC分类号: C07D413/04 , C07D261/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient.The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
摘要翻译: 本发明提供式(I)的异恶唑啉FAAH抑制剂或其药学上可接受的形式,其中G,Ra,Rb,Rc和Rd各自如本文所定义。 本发明还提供包含式(I)化合物或其药学上可接受的形式的药物组合物和药学上可接受的赋形剂。 本发明还提供了治疗FAAH介导的病症的方法,包括向有需要的受试者施用治疗有效量的式(I)化合物或其药学上可接受的形式。
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公开(公告)号:US20090099131A1
公开(公告)日:2009-04-16
申请号:US11870130
申请日:2007-10-10
申请人: Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
摘要: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
摘要翻译: 本发明提供由式(I),(II)或(III)包含的化合物及其药物组合物。 本发明还提供了通过向患者施用治疗有效量的所提供的式(I),(II)或(III)化合物或其药物组合物来治疗FAAH介导的疾病,病症或病症的方法。 需要它。 此外,本发明提供了通过向有需要的患者施用治疗有效量的式(I),(II)或(III)化合物或其药物组合物来抑制患者的FAAH的方法。
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公开(公告)号:US08927551B2
公开(公告)日:2015-01-06
申请号:US12782655
申请日:2010-05-18
申请人: Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号: A61K31/498 , C07D413/04 , A61K31/4439 , C07D401/14 , A61K31/506 , A61K31/424 , C07D401/04 , A61K31/454 , C07D413/06 , A61K31/496 , C07D403/10 , C07D401/10 , C07D417/04 , C07D417/14 , C07D413/14 , C07D261/04
CPC分类号: C07D413/04 , C07D261/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient.The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
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公开(公告)号:US08785635B2
公开(公告)日:2014-07-22
申请号:US12199689
申请日:2008-08-27
申请人: Brian Austad , Mark L. Behnke , Alfredo C. Castro , Michael J. Grogan , Somarajannair Janardanannair , Andre Lescarbeau , Stephane Peluso , Martin Tremblay
发明人: Brian Austad , Mark L. Behnke , Alfredo C. Castro , Michael J. Grogan , Somarajannair Janardanannair , Andre Lescarbeau , Stephane Peluso , Martin Tremblay
IPC分类号: C07D211/00 , C07D401/00 , C07D491/02 , A61K31/196 , A61K45/06 , A61K31/4355 , C07D491/04 , A61K31/198 , A61K31/704 , A61K31/664 , A61K38/21 , A61K31/7076 , C07D491/107 , A61K31/58 , A61K31/17 , A61K31/4745 , A61K31/573 , A61K31/454 , A61K31/56 , C07D491/10 , C07J69/00 , C07D491/048 , A61K31/69 , A61K31/519 , A61K31/7068
CPC分类号: A61K31/4355 , A61K9/0014 , A61K31/17 , A61K31/196 , A61K31/198 , A61K31/454 , A61K31/4745 , A61K31/519 , A61K31/56 , A61K31/573 , A61K31/58 , A61K31/664 , A61K31/69 , A61K31/704 , A61K31/7068 , A61K31/7076 , A61K38/21 , A61K45/06 , A61N5/10 , C07D307/94 , C07D471/04 , C07D471/10 , C07D491/04 , C07D491/048 , C07D491/10 , C07D491/107 , C07J69/00
摘要: The invention provides novel derivatives of cyclopamine having the following formula:
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