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1.发明授权SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYL PYRAZINONES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 有权取代的多环芳基和HETEROARYLPYRAZINONE用于凝血级联的选择性抑制
公开(公告)号：EP1202975B1
公开(公告)日：2005-04-06
申请号：EP00931916.1
申请日：2000-05-18
发明人： SOUTH, Michael, S. , PARLOW, John, J. , JONES, Darin, E. , CASE, Brenda , DICE, Tom , LINDMARK, Richard , HAYES, Michael, J. , RUEPPEL, Melvin, L. , FENTON, Rick , FRANKLIN, Gary, W. , HUANG, Horng-Chih , HUANG, Wei , KUSTURIN, Carrie , LONG, Scott, A. , NEUMANN, William, L. , REITZ, David B. , TRUJILLO, John, I. , WANG, Ching-Cheng , WOOD, Rhonda , MAHONEY, Matthew, W. , Zeng, Qingping
IPC分类号： C07D241/20 , C07D417/12 , C07D401/12 , C07D403/12 , C07D413/12 , C07D409/12 , A61K31/495 , A61K31/497 , A61P7/02
CPC分类号： C07D401/12 , C07D241/20 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
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2.发明公开SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYL PYRIDINES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开取代的多环芳基和HETEROARYLPYRIDINE FOR选择性抑制凝血级联
公开(公告)号：EP1351686A2
公开(公告)日：2003-10-15
申请号：EP01995851.1
申请日：2001-11-20
发明人： SOUTH, Michael, S. , CASE, Brenda , GARLAND, Danny, J. , HAYES, Michael, J. , HUANG, Horng-Chih , HUANG, Wei , JONES, Darin, E. , NEUMANN, William, L. , PARLOW, John, J. , REITZ, David, B. , RUEPPEL, Melvin, L. , WEBBER, Ronald, K.
IPC分类号： A61K31/4418
CPC分类号： C07D213/74 , C07D213/89
摘要： The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
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公开(公告)号：EP1525003A1
公开(公告)日：2005-04-27
申请号：EP03762236.2
申请日：2003-06-27
发明人： JONES, Claude, R. , BASHKIN, James, K. , RADER, Randall, K. , KOTYK, John, J. , NEUMANN, William, L. , MISKO, Thomas, P. , KORNMEIER, Christine, M.
IPC分类号： A61K49/06
CPC分类号： A61K49/101 , A61K49/10 , A61K49/106
摘要： A contrast agent for nuclear magnetic resonance spectroscopy adapted for use in a living tissue comprising at least one reporter nucleus, together with a pharmaceutically acceptable carrier is disclosed. The contrast agent exhibits a first spectral property when not bound by nitric oxide, and a second spectral property when bound by nitric oxide. Methods of using the contrast agents for the detection of nitric oxide are also disclosed.
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4.发明公开POLYCYCLIC ARYL AND HETEROARYL SUBSTITUTED 4-PYRIDONES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开多环芳基和杂芳基取代-4-吡啶酮衍生物的常用FOR凝血级联的选择性抑制
公开(公告)号：EP1268428A2
公开(公告)日：2003-01-02
申请号：EP01924684.2
申请日：2001-04-04
发明人： SOUTH, Michael, S. , MA, Chun, C. , KOELLER, Kevin, J. , RAHMAN, Hayat, K. , NEUMANN, William, L.
IPC分类号： C07D213/74 , A61K31/4412 , A61P7/00 , A61P9/00
CPC分类号： C07D213/74
摘要： The invention relates to polycyclic aryl and heteroaryl substituted 4-pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
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5.发明授权POLYCYCLIC ARYL AND HETEROARYL SUBSTITUTED 4-PYRONES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 有权POLYZYCLISCH芳基和用作凝结的选择性抑制的杂芳基取代的4-吡喃酮
公开(公告)号：EP1268463B1
公开(公告)日：2005-02-16
申请号：EP01923149.7
申请日：2001-04-04
发明人： SOUTH, Michael, S. , MA, Chun, C. , KOELLER, Kevin, J. , RAHMAN, Hayat, K. , NEUMANN, William, L.
IPC分类号： C07D309/38 , C07D309/40 , C07D405/12 , A61K31/351 , A61P7/02
CPC分类号： C07D405/12 , C07D309/38 , C07D309/40
摘要： The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
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6.发明公开PRODRUGS OF SUBSTITUTED POLYCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开PRODRUGS VON SUBSTITUIERTEN POLYZYCLISCHEN VEBINDUNGENFÜRDIE SELEKTIVE HEMMUNG DER KOAGULATIONSKASKADE
公开(公告)号：EP1482940A2
公开(公告)日：2004-12-08
申请号：EP02773700.6
申请日：2002-10-03
发明人： SOUTH, Michael, S. , WEBBER, Ronald, K. , HUANG, Horng-Chih , TOTH, Mihaly, V. , MOORMANN, Alan, E. , SNYDER, Jeffrey, S. , SCHOLTEN, Jeffrey, A. , GARLAND, Danny, J. , RUEPPEL, Melvin, L. , NEUMANN, William, L. , LONG, Scott , WEI, Huang , TRUJILLO, John , PARLOW, John, J. , JONES, Darin, E. , CASE, Brenda , HAYES, Michael, J. , ZENG, Qingping
IPC分类号： A61K31/4965 , C07D241/20 , C07D413/12 , A61K31/497 , C07D407/12 , C07D471/04 , C07D401/12
CPC分类号： C07D213/74 , C07C257/18 , C07C2601/04 , C07C2601/10 , C07D207/32 , C07D211/56 , C07D211/98 , C07D231/38 , C07D231/48 , C07D237/04 , C07D239/10 , C07D239/22 , C07D241/04 , C07D241/20 , C07D249/14 , C07D253/06 , C07D253/075 , C07D263/48 , C07D265/02 , C07D277/42 , C07D307/22 , C07D333/36 , C07D401/12 , C07D403/10 , C07D409/12 , C07D413/12 , C07D471/04
摘要： The present invention relates to prodrug compounds, comprising a 5- or 6- membered heterocyclic or aromatic ring substituted with a derivatized amidine, as well as compositions and methods useful for preventing and treating thrombotic conditions in mammals. The prodrug compounds of the present invention selectively inhibit certain proteases of the coagulation cascade.
摘要翻译： 本发明涉及包含被衍生的脒取代的5-或6-元杂环或芳环的前药化合物，以及可用于预防和治疗哺乳动物血栓形成状况的组合物和方法。 本发明的前药化合物选择性地抑制凝血级联的某些蛋白酶。
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7.发明公开6-MEMBERED UNSATURATED HETEROCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OFTHE COAGULATION CASCADE 审中-公开6-GLIEDRIGEUNGESÄTTIGTEHETEROCYCLEN VERWENDBARFÜRSELEKTIVE HEMMUNG DER COAGULATIONSKASKADE
公开(公告)号：EP1448534A1
公开(公告)日：2004-08-25
申请号：EP02800488.5
申请日：2002-10-03
发明人： SOUTH, Michael, S. , WEBBER, Ronald, K. , HUANG, Horng-Chih , TOTH, Mihaly, V. , MOORMANN, Alan, E. , SNYDER, Jeffrey, S. , SCHOLTEN, Jeffrey, A. , GARLAND, Danny, J. , RUEPPEL, Melvin, L. , NEUMANN, William, L. , LONG, Scott , WEI, Huang , TRUJILLO, John , PARLOW, John, J. , JONES, Darin, E. , CASE, Brenda , HAYES, Michael, J. , ZENG, Qingping , ABBAS, Zaheer , FENTON, Ricky L. , KUSTURIN, Carrie L. , HAYAT, Rahman K. , SAMPLE, Kirby R. , SCHWEITZER, Barbara A. , WOOD, Rhonda S. , SZALONY, Jim , SULEYMANOV, Osman D. , SALYERS, Anita , NICHOLSON, Nancy S.
IPC分类号： C07D239/47 , C07D241/20 , C07D403/12 , C07D409/12 , C07D401/12 , C07D403/10 , C07D403/04 , C07D471/04 , A61K31/4965 , A61K31/513 , A61P7/02
CPC分类号： C07D231/38 , C07C257/18 , C07C2601/04 , C07C2601/10 , C07D207/32 , C07D211/56 , C07D211/98 , C07D213/74 , C07D231/48 , C07D237/04 , C07D239/10 , C07D239/22 , C07D241/04 , C07D241/20 , C07D249/14 , C07D253/06 , C07D253/075 , C07D263/48 , C07D265/02 , C07D277/42 , C07D307/22 , C07D333/36 , C07D401/12 , C07D403/10 , C07D409/12 , C07D413/12 , C07D471/04
摘要： The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
摘要翻译： 本发明涉及化合物及其前药，可用于预防和治疗哺乳动物血栓形成状况的组合物和方法。 本发明的化合物及其前药选择性地抑制凝血级联的某些蛋白酶。
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8.发明公开6-MEMBERED HETEROCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开6-元杂环的化合物其中用于选择性抑制凝血级联SUITABLE
公开(公告)号：EP1438292A1
公开(公告)日：2004-07-21
申请号：EP02800484.4
申请日：2002-10-03
发明人： SOUTH, Michael, S. , WEBBER, Ronald, K. , HUANG, Horng-Chih , TOTH, Mihaly, V. , MOORMANN, Alan, E. , SNYDER, Jeffery, S. , SCHOLTEN, Jeffrey, A. , GARLAND, Danny, J. , RUEPPEL, Melvin, L. , NEUMANN, William, L. , LONG, Scott , WEI, Huang , TRUJILLO, John , PARLOW, John, J. , JONES, Darin, E. , CASE, Brenda , HAYES, Michael, J.
IPC分类号： C07D211/98 , A61K31/45 , C07D239/22 , C07D239/10 , C07D253/06 , C07D211/56 , C07D241/04 , C07D213/73 , C07D237/02 , A61K31/535 , A61K31/495 , A61P7/02
CPC分类号： C07D213/74 , C07C257/18 , C07C2601/04 , C07C2601/10 , C07D207/32 , C07D211/56 , C07D211/98 , C07D231/38 , C07D231/48 , C07D237/04 , C07D239/10 , C07D239/22 , C07D241/04 , C07D241/20 , C07D249/14 , C07D253/06 , C07D253/075 , C07D263/48 , C07D265/02 , C07D277/42 , C07D307/22 , C07D333/36 , C07D401/12 , C07D403/10 , C07D413/12 , C07D471/04
摘要： The present invention relates to compounds, and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
摘要翻译： 本发明涉及化合物及其前药，组合物以及预防和治疗哺乳动物的血栓形成病症的方法。 本发明的前药的化合物，以及它们的，选择性地抑制凝血级联的蛋白酶的某些。
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9.发明公开SUBSTITUTED 5-MEMBERED POLYCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开替代品FÜNFGLIEDRIGEPOLYZYCLISCHEN VEBINDUNGENFÜRDIE SELEKTIVE HEMMUNG DER KOAGULATIONSKASKADE
公开(公告)号：EP1432687A2
公开(公告)日：2004-06-30
申请号：EP02807360.9
申请日：2002-10-03
发明人： SOUTH, Michael, S. , WEBBER, Ronald, K. , HUANG, Horng-Chih , TOTH, Mihaly, V. , MOORMANN, Alan, E. , SNYDER, Jeffrey, S. , SCHOLTEN, Jeffrey, A. , GARLAND, Danny, J. , RUEPPEL, Melvin, L. , NEUMANN, William, L. , LONG, Scott , WEI, Huang , TRUJILLO, John , PARLOW, John, J. , JONES, Darin, E. , CASE, Brenda , HAYES, Michael, J.
IPC分类号： C07D231/00
CPC分类号： C07D213/74 , C07C257/18 , C07C2601/04 , C07C2601/10 , C07D207/32 , C07D207/46 , C07D211/56 , C07D211/98 , C07D231/38 , C07D231/48 , C07D237/04 , C07D239/10 , C07D239/22 , C07D241/04 , C07D241/20 , C07D249/14 , C07D253/06 , C07D253/075 , C07D263/48 , C07D265/02 , C07D277/42 , C07D307/22 , C07D333/36 , C07D401/12 , C07D403/10 , C07D413/12 , C07D471/04
摘要： The present invention relates to substituted 5-membered polycyclic compounds and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
摘要翻译： 本发明涉及化合物及其前药，可用于预防和治疗哺乳动物血栓形成状况的组合物和方法。 本发明的化合物及其前药选择性地抑制凝血级联的某些蛋白酶。
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10.发明公开POLYCYCLIC ARYL AND HETEROARYL SUBSTITUTED 4-PYRONES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 有权POLYZYCLISCH芳基和用作凝结的选择性抑制的杂芳基取代的4-吡喃酮
公开(公告)号：EP1268463A2
公开(公告)日：2003-01-02
申请号：EP01923149.7
申请日：2001-04-04
发明人： SOUTH, Michael, S. , MA, Chun, C. , KOELLER, Kevin, J. , RAHMAN, Hayat, K. , NEUMANN, William, L.
IPC分类号： C07D309/38 , C07D309/40 , C07D405/12 , A61K31/351 , A61P7/02
CPC分类号： C07D405/12 , C07D309/38 , C07D309/40
摘要： The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
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