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公开(公告)号：EP2744804A1
公开(公告)日：2014-06-25
申请号：EP12748200.8
申请日：2012-08-14
发明人： BROTHERTON-PLEISS, Christine , JAIME-FIGUEROA, Saul , LOPEZ-TAPIA, Francisco Javier , LOU, Yan , OWENS, Timothy D.
IPC分类号： C07D401/14 , C07D487/04 , A61K31/4725 , A61P19/02
CPC分类号： C07D401/14 , C07D487/04
摘要： This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据通式I的化合物：其中变量如本文所述定义并且抑制Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了含有式I化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：EP2709997A1
公开(公告)日：2014-03-26
申请号：EP12721812.1
申请日：2012-05-14
发明人： BILLEDEAU, Roland J. , KONDRU, Rama K. , LOPEZ-TAPIA, Francisco Javier , LOU, Yan , OWENS, Timothy D. , QIAN, Yimin , SO, Sung-Sau , THAKKAR, Kshitij Chhabilbhai , WANNER, Jutta , MORALES, Omar Jose
IPC分类号： C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D413/10 , C07D417/10 , C07D471/04 , A61K31/502 , A61P29/00 , A61P37/00
CPC分类号： C07D405/10 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/10 , C07D417/10 , C07D471/04
摘要： This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
摘要翻译： 该申请公开了根据通式（I）的化合物，其中所有变量如本文所述定义，其抑制Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过度Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎性和自身免疫疾病，如类风湿性关节炎。 还公开了含有式（I）化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：EP2571881A1
公开(公告)日：2013-03-27
申请号：EP11721743.0
申请日：2011-05-17
发明人： HENDRICKS, Robert Than , HERMANN, Johannes Cornelius , KONDRU, Rama K. , LOU, Yan , LYNCH, Stephen M. , OWENS, Timothy D. , SOTH, Michael , YEE, Calvin Wesley
IPC分类号： C07D487/04 , A61K31/4965 , A61K31/497 , A61P29/00 , A61P37/00 , A61P35/00 , A61P25/00 , A61P9/00 , A61P3/00 , A61P11/00 , A61P19/00
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables Q and R
1 and R
2 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.摘要翻译： 本发明涉及式（I）的新型吡咯并吡嗪衍生物的用途，其中变量Q和R 1和R 2如本文所述定义，其抑制JAK和SYK并可用于治疗自身免疫和炎症 疾病。
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公开(公告)号：EP2709997B1
公开(公告)日：2016-06-29
申请号：EP12721812.1
申请日：2012-05-14
发明人： BILLEDEAU, Roland J. , KONDRU, Rama K. , LOPEZ-TAPIA, Francisco Javier , LOU, Yan , OWENS, Timothy D. , QIAN, Yimin , SO, Sung-Sau , THAKKAR, Kshitij Chhabilbhai , WANNER, Jutta , MORALES, Omar Jose
IPC分类号： C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D413/10 , C07D417/10 , C07D471/04 , A61K31/502 , A61P29/00 , A61P37/00
CPC分类号： C07D405/10 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/10 , C07D417/10 , C07D471/04
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公开(公告)号：EP2550273A2
公开(公告)日：2013-01-30
申请号：EP11711061.9
申请日：2011-03-18
发明人： HENDRICKS, Robert Than , HERMANN, Johannes Cornelius , KONDRU, Rama K. , LOU, Yan , LYNCH, Stephen M. , OWENS, Timothy D. , SOTH, Michael
IPC分类号： C07D487/04 , C07D519/00 , A61K31/4985 , A61P29/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables n, p, q, Q, X, X' and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
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