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公开(公告)号：EP3713930A1
公开(公告)日：2020-09-30
申请号：EP18836556.3
申请日：2018-11-19
发明人： LIU, Chunjian , YANG, Michael G. , XIAO, Zili , CHEN, Ling , MOSLIN, Ryan M. , TOKARSKI, John S. , WEINSTEIN, David S. , WROBLESKI, Stephen, T.
IPC分类号： C07D401/14 , A61K31/501 , C07D401/12 , C07D487/04 , A61P29/00 , A61P37/00
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2.发明授权METHODS OF TREATING P38 KINASE-ASSOCIATED CONDITIONS AND PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS 有权治疗与p38激酶和吡咯并三嗪化合物作为激酶抑制剂相关的病症的方法。
公开(公告)号：EP1363910B1
公开(公告)日：2006-03-01
申请号：EP01992298.8
申请日：2001-11-07
IPC分类号： C07D487/04 , C07D519/00 , A61K31/53 , A61P29/00 , C07D253/00 , C07D209/00 , C07D487/00 , C07D471/00
CPC分类号： C07D487/04
摘要： Methods of treating one or more conditions associated with p38 kinase activity are disclosed comprising administering to a patient in need thereof at least one compound having the formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, or NH2, preferably methyl, and X, R1 through R6, and Z are as described in the specification. Advantageously the groups ZR4R5 taken together comprise an NH-subsituted aryl.
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公开(公告)号：EP1620108A2
公开(公告)日：2006-02-01
申请号：EP04760705.6
申请日：2004-05-03
发明人： DYCKMAN, Alaric , DAS, Jagabandhu , LEFTHERIS, Katerina , LIU, Chunjian , MOQUIN, Robert, V. , WROBLESKI, Stephen, T.
IPC分类号： A61K31/535
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
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公开(公告)号：EP1409463A1
公开(公告)日：2004-04-21
申请号：EP02739978.1
申请日：2002-06-25
发明人： MORIARTY, Kevin, J. , SHIMSHOCK, Yvonne , AHMED, Gulzar , WU, Junjun , WEN, James , LI, Wei , ERICKSON, Shawn, D. , LETOURNEAU, Jeffrey, J. , MCDONALD, Edward , LEFTHERIS, Katerina , WROBLESKI, Stephen, T. , HUSSAIN, Zahid , HENDERSON, Ian , METZGER, Axel , BALDWIN, John, J. , DYCKMAN, Alaric
IPC分类号： C07D239/32 , C07D239/46 , C07D239/48 , C07D239/50 , C07D251/46 , C07D251/52 , C07D251/54 , A61K31/166 , A61P29/00 , A61P37/08 , A61P7/02
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I). Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-a expression utilizing compounds of the present invention are also disclosed.
摘要翻译： 公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。 在一个实施方案中，本发明的化合物由式（I）表示。 也公开了使用本发明化合物治疗与不适当的p38激酶活性或TNF-α表达有关的病症的方法，药物组合物和方法。
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公开(公告)号：EP1928879B1
公开(公告)日：2013-02-13
申请号：EP06825074.5
申请日：2006-09-22
发明人： VACCARO, Wayne , CHEN, Zhong , DODD, Dharmpal, S. , HUYNH, Tram, N. , LIN, James , LIU, Chunjian , MUSSARI, Christopher, P. , TOKARSKI, John, S. , TORTOLANI, David, R. , WROBLESKI, Stephen, T.
IPC分类号： C07D487/04 , A61K31/437 , A61P29/00
CPC分类号： C07D487/04
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公开(公告)号：EP1617840A2
公开(公告)日：2006-01-25
申请号：EP04760683.5
申请日：2004-05-03
发明人： DYCKMAN, Alaric , DAS, Jagabandhu , LEFTHERIS, Katerina , LIU, Chunjian , MOQUIN, Robert, V. , WROBLESKI, Stephen, T.
IPC分类号： A61K31/415 , C07D231/04
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
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7.发明公开METHODS FOR THE PREPARATION OF PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS 有权用于生产PYRROLOTRIAZINVERBINDUNGEN引致的，激酶抑制剂适合...
公开(公告)号：EP1562949A2
公开(公告)日：2005-08-17
申请号：EP03781756.6
申请日：2003-11-03
发明人： GODFREY, Jollie, Duaine, Jr. , HYNES, John, Jr. , DYCKMAN, Alaric, J. , LEFTHERIS, Katerina , SHI, Zhongping , WROBLESKI, Stephen, T. , DOUBLEDAY, Wendel, William , GROSSO, John, A.
IPC分类号： C07D487/04 , A61K31/53
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.
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公开(公告)号：EP1406875A1
公开(公告)日：2004-04-14
申请号：EP02746724.0
申请日：2002-06-26
发明人： AHMED, Gulzar , METZGER, Axel , WROBLESKI, Stephen, T. , HENDERSON, Ian , WEN, James , DILLER, David, J. , LEFTHERIS, Katerina
IPC分类号： C07D239/42 , C07D239/48 , A61K31/505
CPC分类号： C07D239/48 , C07D213/85 , C07D239/47 , C07D239/50 , C07D401/12 , C07D403/12
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I). Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
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公开(公告)号：EP1620108B1
公开(公告)日：2012-06-06
申请号：EP04760705.6
申请日：2004-05-03
发明人： DYCKMAN, Alaric , DAS, Jagabandhu , LEFTHERIS, Katerina , LIU, Chunjian , MOQUIN, Robert, V. , WROBLESKI, Stephen, T.
IPC分类号： C07D231/14 , A61K31/535 , A61P29/00 , C07D231/40 , C07D231/38
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.
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10.发明授权ARYL-SUBSTITUTED PYRAZOLE-AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS 有权作为激酶抑制剂的合适的芳PYRAZOLAMIDVERBINDUNGEN
公开(公告)号：EP1618092B1
公开(公告)日：2010-09-22
申请号：EP04751133.2
申请日：2004-05-03
发明人： DYCKMAN, Alaric , DAS, Jagabandhu , LEFTHERIS, Katerina , LIU, Chunjian , ZHAO, Rulin , CHEN, Bang-Chi , WROBLESKI, Stephen, T.
IPC分类号： C07D231/18 , A61K31/4155 , A61P37/00
CPC分类号： C07D231/14 , C07D231/12 , C07D231/40 , C07D401/12 , C07D413/12
摘要： The present invention relates to compounds having the formula (I), and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, or pyrazinyl ring; R2 is alkyl or an amino group as defined herein; and Z is optionally-substituted oxadiazolyl or -C(=O)NR6, wherein R6 is lower alkyl or cyclopropyl. The compounds are surprisingly advantageous in preparing medicaments for treating p38 kinase related conditions and/or in preparing medicaments for use in treating inflammatory disorders or conditions in a patient.
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