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公开(公告)号：EP2192838A4
公开(公告)日：2011-07-27
申请号：EP08795375
申请日：2008-08-15
发明人： CUNY GREGORY D , TENG XIN , YUAN JUNYING , DEGTEREV ALEXEI , PORCO JOHN A JR
CPC分类号： C07D417/12 , C07D207/34 , C07D231/14 , C07D241/24 , C07D263/34 , C07D277/56 , C07D285/06 , C07D307/68 , C07D307/84 , C07D333/38
摘要： The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-±) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-± induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
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公开(公告)号：EP2968276A4
公开(公告)日：2017-02-15
申请号：EP14763816
申请日：2014-03-14
发明人： YUAN JUNYING , DEGTEREV ALEXEI , CUNY GREGORY D
IPC分类号： C07D401/14 , A61K31/4025 , A61K31/4166 , A61P9/00 , A61P11/00 , C07D471/04 , C07D487/04
CPC分类号： C07D487/04 , C07D401/14 , C07D471/04
摘要： The present invention relates to heterocyclic compounds (e.g., compounds described by Formula (I)) and pharmaceutically acceptable salts thereof. The invention also features pharmaceutical compositions that include these compounds and their use in therapy for treating conditions in which necroptosis is likely to play a substantial role. The heterocyclic compounds described herein can also achieve improved activity and selectivity towards RIP1 and/or RIP3.
摘要翻译： 本发明涉及杂环化合物（例如式（I）所述的化合物）及其药学上可接受的盐。 本发明的特征还在于包含这些化合物的药物组合物及其在治疗中用于治疗可能发生重要作用的坏死的病症的用途。 本文所述的杂环化合物也可以实现改善的对RIP1和/或RIP3的活性和选择性。
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公开(公告)号：EP2381775A4
公开(公告)日：2012-08-15
申请号：EP09835866
申请日：2009-12-23
申请人： HARVARD COLLEGE
发明人： YUAN JUNYING , HSU EMILY S
IPC分类号： A61K31/519 , A61K31/045 , A61K31/415 , A61K31/4178 , A61K31/429 , A61K31/496 , A61K31/517 , A61P35/00 , C07D231/06 , C07D231/12 , C07D231/56 , C07D277/46 , C07D403/12 , C07D417/12 , C07D495/04 , C07D498/08
CPC分类号： C07C35/37 , C07C33/38 , C07D209/08 , C07D211/78 , C07D211/90 , C07D215/08 , C07D231/06 , C07D231/12 , C07D231/56 , C07D233/02 , C07D277/18 , C07D277/46 , C07D307/52 , C07D333/20 , C07D403/06 , C07D403/12 , C07D405/06 , C07D417/12 , C07D495/04 , C07D498/08
摘要： The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-±) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-± induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
摘要翻译： 本发明的特征是一系列抑制肿瘤坏死因子α（TNF-α）诱导的坏死病的杂环衍生物。 （I） - （VIII）和化合物（1） - （7），（13） - （26），（27） - （33），（48） - （57） ）和（58） - （70）。 已显示这些坏死杆菌素抑制人Jurkat T细胞的FADD缺陷型变体中TNF-α诱导的坏死。 本发明的特征还在于以坏死菌素为特征的药物组合物。 本发明的化合物和组合物也可用于治疗坏死病可能发挥重大作用的病症。
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公开(公告)号：EP1968583A4
公开(公告)日：2010-09-15
申请号：EP06847822
申请日：2006-12-20
IPC分类号： C07D225/04 , A61K31/4178 , A61K31/513 , A61P25/28
CPC分类号： C07D231/54 , A61K31/4178 , C07D403/06 , C07D491/052 , C07D495/04
摘要： The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described.
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