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1.6-MEMBERED UNSATURATED HETEROCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
Title translation: 6成员不饱和杂环化合物可用于选择性抑制凝聚剂CASCADE公开(公告)号:WO2003029224A1
公开(公告)日:2003-04-10
申请号:PCT/US2002/031784
申请日:2002-10-03
Applicant: PHARMACIA CORPORATION , 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.
Inventor: 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: C07D239/47
CPC classification number: 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
Abstract: 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.
Abstract translation: 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病症的组合物和方法。 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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2.POLYCYCLIC ARYL AND HETEROARYL SUBSTITUTED 1,4-QUINONES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
Title translation: 用于选择性抑制凝聚剂CASCADE的多环芳烃和杂环取代的1,4-Quonones公开(公告)号:WO0179155A3
公开(公告)日:2002-05-16
申请号:PCT/US0111798
申请日:2001-04-10
Applicant: PHARMACIA CORP , SOUTH MICHAEL S , PARLOW JOHN J
Inventor: SOUTH MICHAEL S , PARLOW JOHN J
IPC: A61P7/02 , A61K31/165 , A61P9/00 , A61P9/10 , A61P11/00 , A61P35/00 , C07C257/18 , C07D295/13 , C07C237/18
CPC classification number: C07D295/13 , C07C257/18 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42
Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone 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.
Abstract translation: 本发明涉及可用作凝血级联丝氨酸蛋白酶抑制剂的多环芳基和杂芳基取代的1,4-醌化合物,以及用于抗凝治疗的组合物和方法,用于治疗和预防多种血栓形成状况,包括冠状动脉和脑血管 疾病。
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3.
公开(公告)号:WO2003093242A3
公开(公告)日:2003-11-13
申请号:PCT/US2002/031770
申请日:2002-10-03
Applicant: PHARMACIA CORPORATION , 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.
Inventor: 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: C07D231/48
Abstract: 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.
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4.
公开(公告)号:WO2002042272A3
公开(公告)日:2002-05-30
申请号:PCT/US2001/043280
申请日:2001-11-20
Applicant: PHARMACIA CORPORATION , 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.
Inventor: 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: A61K31/4418
Abstract: 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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5.SUBSTITUTED 5-MEMBERED POLYCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
Title translation: 取代的5组分多环化合物可用于选择性抑制凝聚剂CASCADE公开(公告)号:WO2003093242A2
公开(公告)日:2003-11-13
申请号:PCT/US2002/031770
申请日:2002-10-03
Applicant: PHARMACIA CORPORATION , 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.
Inventor: 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: C07D231/00
CPC classification number: 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
Abstract: 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.
Abstract translation: 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病症的组合物和方法。 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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6.6-MEMBERED HETEROCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
Title translation: 用于选择性抑制凝聚剂CASCADE的6组分杂环化合物公开(公告)号:WO2003029216A1
公开(公告)日:2003-04-10
申请号:PCT/US2002/031769
申请日:2002-10-03
Applicant: PHARMACIA CORPORATION , 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.
Inventor: 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: C07D211/98
CPC classification number: 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
Abstract: 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.
Abstract translation: 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病症的组合物和方法。 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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7.SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYL PYRIDINES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
Title translation: 用于选择性抑制凝聚剂CASCADE的取代的多环芳烃和异丁基吡啶公开(公告)号:WO0242272A8
公开(公告)日:2003-10-23
申请号:PCT/US0143280
申请日:2001-11-20
Applicant: PHARMACIA CORP , 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
Inventor: 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: A61K31/44 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61K45/00 , A61P7/02 , A61P9/10 , A61P11/00 , A61P35/00 , A61P43/00 , C07D213/74 , C07D213/89 , C07D401/10 , C07D409/04 , C07D213/77 , C07D213/90 , C07D237/20 , C07D239/36 , C07D239/42 , C07D241/20 , C07D253/04 , C07D253/06 , C07D265/02 , C07D417/12
CPC classification number: C07D213/74 , C07D213/89
Abstract: 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.
Abstract translation: 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病症的组合物和方法。 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.
公开(公告)号:WO2003028729A3
公开(公告)日:2003-04-10
申请号:PCT/US2002/031468
申请日:2002-10-03
Applicant: PHARMACIA CORPORATION , 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
Inventor: 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: A61K31/4965
Abstract: 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.
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9.PRODRUGS OF SUBSTITUTED POLYCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
Title translation: 用于选择性抑制凝聚剂CASCADE的取代多环化合物的制剂公开(公告)号:WO2003028729A2
公开(公告)日:2003-04-10
申请号:PCT/US2002/031468
申请日:2002-10-03
Applicant: PHARMACIA CORPORATION , 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
Inventor: 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: A61K31/4965
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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10.SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYL PYRIDINES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
Title translation: 用于选择性抑制凝聚剂CASCADE的取代的多环芳烃和异丁基吡啶公开(公告)号:WO0242272A2
公开(公告)日:2002-05-30
申请号:PCT/US0143280
申请日:2001-11-20
Applicant: PHARMACIA CORP , 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
Inventor: 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: A61K31/44 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61K45/00 , A61P7/02 , A61P9/10 , A61P11/00 , A61P35/00 , A61P43/00 , C07D213/74 , C07D213/89 , C07D401/10 , C07D409/04 , C07D213/00
CPC classification number: C07D213/74 , C07D213/89
Abstract: 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.
Abstract translation: 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病症的组合物和方法。 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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