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公开(公告)号：EP2731932A1
公开(公告)日：2014-05-21
申请号：EP12734923.1
申请日：2012-07-09
发明人： BILOTTA, Joseph Anthony , CHEUNG, Adrian Wai-Hing , FIROOZNIA, Fariborz , GUERTIN, Kevin Richard , HAYDEN, Stuart , HAYNES, Nancy-Ellen , LUKACS-LESBURG, Christine M. , MARCOPULOS, Nicholas , MERTZ, Eric , QI, Lida , QIAN, Yimin , SO, Sung-Sau , TAN, Jenny , THAKKAR, Kshitij Chhabilbhai
IPC分类号： C07D215/48 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D215/233 , A61K31/4709 , A61P3/10 , A61P19/00 , A61P35/00 , A61P25/00
CPC分类号： C07D215/48 , C07D215/233 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula (I): wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
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公开(公告)号：EP2731932B1
公开(公告)日：2015-12-30
申请号：EP12734923.1
申请日：2012-07-09
发明人： BILOTTA, Joseph Anthony , CHEUNG, Adrian Wai-Hing , FIROOZNIA, Fariborz , GUERTIN, Kevin Richard , HAYDEN, Stuart , HAYNES, Nancy-Ellen , LUKACS-LESBURG, Christine M. , MARCOPULOS, Nicholas , MERTZ, Eric , QI, Lida , QIAN, Yimin , SO, Sung-Sau , TAN, Jenny , THAKKAR, Kshitij Chhabilbhai
IPC分类号： C07D215/48 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D215/233 , A61K31/4709 , A61P3/10 , A61P19/00 , A61P35/00 , A61P25/00
CPC分类号： C07D215/48 , C07D215/233 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
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3.发明授权THIAZOLO-PYRAMIDINE / PYRIDINE UREA DERIVATIVES AS ADENOSINE A2B RECEPTOR ANTAGONISTS 有权噻唑并吡啶/吡啶尿素衍生物作为腺苷A2B受体拮抗剂
公开(公告)号：EP2027132B1
公开(公告)日：2010-09-15
申请号：EP07728869.4
申请日：2007-05-08
发明人： BRINKMAN, John A. , CHEUNG, Adrian Wai-Hing , FIROOZNIA, Fariborz , GUERTIN, Kevin Richard , MARCOPULOS, Nicholas , QI, Lida , RACHA, Jagdish Kumar , SARABU, Ramakanth , TAN, Jenny , TILLEY, Jefferson Wright
IPC分类号： C07D513/04 , C07D521/00 , A61K31/519 , A61K31/437 , A61P3/10
CPC分类号： C07D513/04 , C07D521/00
摘要： There are presented compounds of the formula (I) wherein R1, R2, R3 and R4 are as defined in the description and claims, or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.
摘要翻译： 提供了式（I）化合物，其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，或其药学上可接受的盐，它们是活性的腺苷A 2B受体拮抗剂并可用于治疗糖尿病，糖尿病 视网膜病，哮喘和腹泻。
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4.发明公开THIAZOLO-PYRAMIDINE / PYRIDINE UREA DERIVATIVES AS ADENOSINE A2B RECEPTOR ANTAGONISTS 有权THIAZOLOPYRAMIDIN / PYRIDINHARNSTOFFDERIVATE拮抗剂腺苷2B受体
公开(公告)号：EP2027132A1
公开(公告)日：2009-02-25
申请号：EP07728869.4
申请日：2007-05-08
发明人： BRINKMAN, John A. , CHEUNG, Adrian Wai-Hing , FIROOZNIA, Fariborz , GUERTIN, Kevin Richard , MARCOPULOS, Nicholas , QI, Lida , RACHA, Jagdish Kumar , SARABU, Ramakanth , TAN, Jenny , TILLEY, Jefferson Wright
IPC分类号： C07D513/04 , C07D521/00 , A61K31/519 , A61K31/437 , A61P3/10
CPC分类号： C07D513/04 , C07D521/00
摘要： There are presented compounds of the formula (I) wherein R1, R2, R3 and R4 are as defined in the description and claims, or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.
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公开(公告)号：EP2603500B1
公开(公告)日：2014-11-19
申请号：EP11746518.7
申请日：2011-08-09
发明人： BERTHEL, Steven, Joseph , BILLEDEAU, Roland, J. , BROTHERTON-PLEISS, Christine, E. , FIROOZNIA, Fariborz , GABRIEL, Stephen, Deems , HAN, Xiaochun , HILGENKAMP, Ramona , JAIME-FIGUEROA, Saul , KOCER, Buelent , LOPEZ-TAPIA, Francisco, Javier , LOU, Yan , ORZECHOWSKI, Lucja , OWENS, Timothy, D. , TAN, Jenny , WOVKULICH, Peter, Michael
IPC分类号： C07D405/14 , C07D413/14 , C07D417/14 , C07D487/10
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107
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公开(公告)号：EP2603500A1
公开(公告)日：2013-06-19
申请号：EP11746518.7
申请日：2011-08-09
发明人： BERTHEL, Steven, Joseph , BILLEDEAU, Roland, J. , BROTHERTON-PLEISS, Christine, E. , FIROOZNIA, Fariborz , GABRIEL, Stephen, Deems , HAN, Xiaochun , HILGENKAMP, Ramona , JAIME-FIGUEROA, Saul , KOCER, Buelent , LOPEZ-TAPIA, Francisco, Javier , LOU, Yan , ORZECHOWSKI, Lucja , OWENS, Timothy, D. , TAN, Jenny , WOVKULICH, Peter, Michael
IPC分类号： C07D401/14 , C07D403/14 , C07D487/04 , C07D487/08 , C07D491/107 , A61K31/517
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107
摘要： This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula (I): wherein, variables X, R, and Y
4 , 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.
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