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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
Applicant: 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
Inventor： 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: A01N43/38
CPC classification number: 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
Abstract: 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.
Abstract translation: 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：US06797708B2
公开(公告)日：2004-09-28
申请号：US10302636
申请日：2002-11-22
Applicant: John C. McKew , Steven Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James D. Clark
Inventor： John C. McKew , Steven Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James D. Clark
IPC: C07D40106
CPC classification number: C07D209/14 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/10
Abstract: 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.
Abstract translation: 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：US20100022536A1
公开(公告)日：2010-01-28
申请号：US12488182
申请日：2009-06-19
Applicant: John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
Inventor： John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
IPC: A61K31/5377 , A61K31/405 , A61K31/497 , A61P29/00 , A61P11/06 , A61P19/02 , A61P25/16 , A61P25/00 , A61P7/02
CPC classification number: C07D209/14 , C07D209/18
Abstract: 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.
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公开(公告)号：US07557135B2
公开(公告)日：2009-07-07
申请号：US11442199
申请日：2006-05-26
Applicant: John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
Inventor： John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
IPC: A61K31/404 , C07D209/14
CPC classification number: C07D209/14 , C07D209/18
Abstract: 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.
Abstract translation: 本发明提供了各种磷脂酶，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：US07713964B2
公开(公告)日：2010-05-11
申请号：US10302171
申请日：2002-11-22
Applicant: John C. McKew , Steven Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James D. Clark
Inventor： John C. McKew , Steven Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James D. Clark
IPC: A61K31/54 , A61K31/535 , A61K31/497 , A61K31/44 , A61K31/425 , A61K31/41 , A61K31/415 , A61K31/40
CPC classification number: C07D401/12 , C07D209/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/10 , Y10S514/826
Abstract: This invention provides methods for treating in mammals asthma and asthmatic conditions using 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.
Abstract translation: 本发明提供使用以下通式的取代吲哚化合物及其药学上可接受的盐形式来治疗哺乳动物哮喘和哮喘病症的方法，以及使用该化合物作为各种磷脂酶，特别是磷脂酶A2酶的活性的抑制剂的方法，以及 用于治疗，预防和抑制疼痛和炎症。
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Patent Agency Ranking
公开(公告)号：US20100029645A1
公开(公告)日：2010-02-04
申请号：US12488020
申请日：2009-06-19
Applicant: John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
Inventor： John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
IPC: A61K31/5377 , C07D209/04 , C07D403/02 , C07D413/02 , A61K31/405 , A61K31/497 , A61P29/00 , A61P19/02 , A61P25/00 , A61P7/02
CPC classification number: C07D209/14 , C07D209/18
Abstract: 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.
Abstract translation: 本发明提供了各种磷脂酶，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：US06635771B2
公开(公告)日：2003-10-21
申请号：US10302634
申请日：2002-11-22
Applicant: John C. McKew , Steven Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James D. Clark
Inventor： John C. McKew , Steven Y. Tam , Katherine L. Lee , Lihren Chen , Paresh Thakker , Fuk-Wah Sum , Mark Behnke , Baihua Hu , James D. Clark
IPC: C07D20916
CPC classification number: C07D401/12 , C07D209/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/10
Abstract: Compounds of the formula in which R, R′, R7-R11, X, n1 and n3 are as defined herein. These compounds are useful as intermediates for preparing pharmaceutical compounds having pharmacological activity as chemical inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes.
Abstract translation: R，R'，R 7 -R 11，X，n 1和n 3如本文所定义的化合物。 这些化合物可用作制备具有作为各种磷脂酶，特别是磷脂酶A2酶的活性的化学抑制剂的具有药理活性的药物化合物的中间体。
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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
Applicant: John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
Inventor： John C. McKew , Katherine L. Lee , Lihren Chen , Richard Vargas , James D. Clark , Cara Williams , Valerie Clerin , Suzana Marusic , Kevin Pong
IPC: A61K31/404
CPC classification number: C07D209/14 , C07D209/18
Abstract: 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.
Abstract translation: 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
Applicant: 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
Inventor： 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: A61K31/54
CPC classification number: 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
Abstract: 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.
Abstract translation: 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：US4806171A
公开(公告)日：1989-02-21
申请号：US116194
申请日：1987-11-03
Applicant: Walter H. Whitlock , William R. Weltmer, Jr. , James D. Clark
Inventor： Walter H. Whitlock , William R. Weltmer, Jr. , James D. Clark
CPC classification number: B24C1/003 , B01F3/06 , B01F5/0646 , B01F5/0652 , B08B3/02 , B24C3/322 , Y10S134/902
Abstract: Apparatus for removing small particles from a substrate comprising a source of fluid carbon dioxide, a first means for expanding a portion of the fluid carbon dioxide into a first mixture containing gaseous carbon dioxide and fine droplets of liquid carbon dioxide, coalescing means for converting the first mixture into a second mixture containing gaseous carbon dioxide and larger liquid droplets of carbon dioxide, second expansion means for converting said second mixture into a third mixture containing solid particles of carbon dioxide and gaseous carbon dioxide, and means for directing said third mixture toward the substrate. Also disclosed are methods for removing fine particles from substrates utilizing the subject apparatus.
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