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公开(公告)号：EP1317429B1
公开(公告)日：2006-08-30
申请号：EP01968579.1
申请日：2001-09-05
申请人： Genentech Inc.
IPC分类号： C07D207/16 , C07D401/06 , C07D403/12 , C07D207/48 , C07D401/12 , A61K31/40 , A61K31/401 , A61K31/4025 , A61P7/02
CPC分类号： C07D401/06 , C07D207/16 , C07D207/48 , C07D401/12 , C07D403/12
摘要： Inhibitors of serine proteases are provided having formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.
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公开(公告)号：EP1144373A2
公开(公告)日：2001-10-17
申请号：EP00911572.6
申请日：2000-01-11
申请人： Genentech, Inc.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C317/00
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having structure (A) are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
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公开(公告)号：EP1144373A3
公开(公告)日：2002-01-02
申请号：EP00911572.6
申请日：2000-01-11
申请人： Genentech, Inc.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C311/51
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
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公开(公告)号：EP1144373B1
公开(公告)日：2005-10-19
申请号：EP00911572.6
申请日：2000-01-11
申请人： GENENTECH, INC.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C311/51
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having structure (A) are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
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公开(公告)号：EP1330430A2
公开(公告)日：2003-07-30
申请号：EP01965996.0
申请日：2001-08-16
申请人： GENENTECH, INC.
发明人： ARTIS, Dean, R. , JACKSON, David, Y. , RAWSON, Thomas, E. , REYNOLDS, Mark, E. , SUTHERLIN, Daniel, P. , STANLEY, Mark, S.
IPC分类号： C07C237/22 , C07C237/20 , C07C233/81 , C07C233/75 , C07C237/04 , A61K31/40 , A61K31/216 , A61K31/196 , C07D207/16 , C07D207/48 , A61P19/02
CPC分类号： C07D403/12 , C07C233/25 , C07C233/60 , C07C233/81 , C07C237/04 , C07C237/20 , C07C237/22 , C07C2601/08 , C07C2603/18 , C07C2603/32 , C07D207/16 , C07D207/48 , C07D209/88 , C07D405/12
摘要： Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhibit binding of ligands for α4 integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with α4 integrins or their ligands.
摘要翻译： 提供式（I）的化合物，其中A，Q，W，X，Y，Z，R 1至R 4，m和n如本文所定义。 本发明的化合物结合α4H整联蛋白受体，从而抑制α4A整联蛋白的配体结合，其可用于预防和/或治疗与 α4整联蛋白或其配体。
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公开(公告)号：EP1317429A1
公开(公告)日：2003-06-11
申请号：EP01968579.1
申请日：2001-09-05
申请人： Genentech Inc.
IPC分类号： C07D207/16 , C07D401/06 , C07D403/12 , C07D207/48 , C07D401/12 , A61K31/40 , A61K31/401 , A61K31/4025 , A61P7/02
CPC分类号： C07D401/06 , C07D207/16 , C07D207/48 , C07D401/12 , C07D403/12
摘要： Inhibitors of serine proteases are provided having formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.
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