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公开(公告)号：EP0944645A1
公开(公告)日：1999-09-29
申请号：EP97954531.0
申请日：1997-12-05
发明人： GOLEC, Julian, M., C. , LAUFFER, David, J. , LIVINGSTON, David, J. , MULLICAN, Michael, D. , MURCKO, Mark, A. , NYCE, Philip, L. , ROBIDOUX, Andrea, L., C. , WANNAMAKER, Marion, W.
IPC分类号： A61K38 , A61P1 , A61P7 , A61P9 , A61P17 , A61P19 , A61P25 , A61P29 , A61P31 , A61P35 , A61P37 , A61P43 , C07K5
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1beta converting enzyme ("ICE"). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-("IL-1"), apoptosis-, interferon-gamma inducing factor-(IGIF), interferon-gamma-("IFN-gamma") mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-gamma production and methods for treating interleukin-1, apoptosis- and interferon-gamma-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
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公开(公告)号：EP1474147B1
公开(公告)日：2010-05-05
申请号：EP02799913.5
申请日：2002-12-09
IPC分类号： A61K31/506 , C07D239/94 , A61P35/00 , C07D401/12 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D413/12 , C07D409/12 , C07D401/04 , C07D409/04 , C07D495/04 , C07D471/04 , C07D475/00
CPC分类号： C07D401/12 , C07D239/94 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D475/10 , C07D487/04 , C07D495/04
摘要： The present invention provides a compound of formula (I): (I), or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3 mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders, such as diabetes, cancer, stroke and Alzheimer’s disease.
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公开(公告)号：EP1532145A1
公开(公告)日：2005-05-25
申请号：EP03767010.6
申请日：2003-07-31
IPC分类号： C07D471/04 , C07D403/12 , A61K31/4427 , A61K31/4155 , A61P9/00 , A61P25/00 , A61P29/00
CPC分类号： C07D403/12 , C07D471/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
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公开(公告)号：EP1064298B1
公开(公告)日：2008-10-08
申请号：EP99912662.6
申请日：1999-03-19
发明人： WANNAMAKER, Marion, W. , BEMIS, Guy, W. , CHARIFSON, Paul, S. , LAUFFER, David, J. , MULLICAN, Michael, D. , MURCKO, Mark, A. , WILSON, Keith, P. , JANETKA, James, W. , DAVIES, Robert, J. , GRILLOT, Anne-Laure , SHI, Zhan , FORSTER, Cornelia, J.
CPC分类号： C07K5/0202 , A61K38/00 , C07D401/12 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1² converting enzyme ("ICE") inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1- ("IL-1"), apoptosis-, interferon-³ inducing factor-(IGIF), or interferon-³-("IFN-³") mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-³ production and methods for treating interleukin-1, apoptosis-, and interferon-³ mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
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公开(公告)号：EP1474147A1
公开(公告)日：2004-11-10
申请号：EP02799913.5
申请日：2002-12-09
IPC分类号： A61K31/506 , C07D239/94 , A61P35/00 , C07D401/12 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D413/12 , C07D409/12 , C07D401/04 , C07D409/04 , C07D495/04 , C07D471/04 , C07D475/00
CPC分类号： C07D401/12 , C07D239/94 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D475/10 , C07D487/04 , C07D495/04
摘要： The present invention provides a compound of formula (I): (I), or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3 mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders, such as diabetes, cancer, stroke and Alzheimer’s disease.
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6.发明公开1,2-DIAZEPANE DERIVATIVES AS INTERLEUKIN-1BETA CONVERTING ENZYME INHIBITORS 有权1,2- DIAZEPANDERIVATE白介素1β的转化酶抑制剂的
公开(公告)号：EP1062210A1
公开(公告)日：2000-12-27
申请号：EP99909935.1
申请日：1999-03-09
IPC分类号： C07D243/02 , A61K31/55 , C07D401/14 , C07D405/12 , C07D401/12
CPC分类号： C07D401/12 , C07D243/02 , C07D401/14 , C07D405/12
摘要： The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme ('ICE') inhibitors represented by formula (I), wherein Y is (a) or (b). This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-η production and methods for treating interleukin-1, apoptosis-, and interferon-η-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
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7.发明授权
公开(公告)号：EP1278737B1
公开(公告)日：2010-06-30
申请号：EP01927217.8
申请日：2001-04-19
IPC分类号： C07D307/32 , C07D307/66 , C07F9/535
CPC分类号： C07D307/33 , C07D307/66 , C07F9/65515
摘要： Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula (I), wherein R1 is an optionally substituted group selected from an aliphatic group, aralkyl group, heterocyclylalkyl group or aryl group, and R2 is preferably a P¿2?-P4 moiety of a caspase inhibitor. Key intermediates include the azidolactones (III) and (VIII).
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公开(公告)号：EP1532145B1
公开(公告)日：2006-09-13
申请号：EP03767010.6
申请日：2003-07-31
IPC分类号： C07D471/04 , C07D403/12 , A61K31/4427 , A61K31/4155 , A61P9/00 , A61P25/00 , A61P29/00
CPC分类号： C07D403/12 , C07D471/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
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公开(公告)号：EP0944645B1
公开(公告)日：2005-03-09
申请号：EP97954531.6
申请日：1997-12-05
发明人： GOLEC, Julian, M., C. , LAUFFER, David, J. , LIVINGSTON, David, J. , MULLICAN, Michael, D. , MURCKO, Mark, A. , NYCE, Philip, L. , ROBIDOUX, Andrea, L., C. , WANNAMAKER, Marion, W.
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1beta converting enzyme ("ICE"). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-("IL-1"), apoptosis-, interferon-gamma inducing factor-(IGIF), interferon-gamma-("IFN-gamma") mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-gamma production and methods for treating interleukin-1, apoptosis- and interferon-gamma-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
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公开(公告)号：EP0942925B1
公开(公告)日：2006-11-22
申请号：EP97949771.6
申请日：1997-12-05
发明人： GOLEC, Julian, M., C. , LAUFFER, David, J. , LIVINGSTON, David, J. , MULLICAN, Michael, D. , NYCE, Philip, L. , ROBIDOUX, Andrea, L., C. , WANNAMAKER, Marion, W.
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1beta converting enzyme ("ICE"). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-("IL-1"), apoptosis-, interferon-gamma inducing factor-(IGIF), or interferon-gamma-("IFN-gamma") mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-gamma production and methods for treating interleukin-1, apoptosis- and interferon-gamma-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
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