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公开(公告)号：EP2706853B1
公开(公告)日：2017-06-14
申请号：EP12782298.9
申请日：2012-05-04
发明人： ALTMAN, Michael D. , CHILDERS, Kaleen Konrad , DI FRANCESCO, Maria Emilia , ELLIS, John Michael , FISCHER, Christian , GRIMM, Jonathan , HAIDLE, Andrew M. , KATTAR, Solomon D. , NORTHRUP, Alan B. , OTTE, Ryan D. , PETROCCHI, Alessia , SCHELL, Adam J. , ZHOU, Hua
IPC分类号： A01N43/54 , A61K31/505 , C07D417/12 , A61K31/506 , A61P11/06 , A61P35/00 , C07D417/14
CPC分类号： C07D417/12 , C07D417/14
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公开(公告)号：EP2513098B1
公开(公告)日：2016-11-09
申请号：EP10801736.9
申请日：2010-12-15
发明人： ALTMANN, Michael D. , ANDRESEN, Brian M. , ARRINGTON, Kenneth L. , CHILDERS, Kaleen Konrad , DI FRANCESCO, Maria Emilia , DONOFRIO, Anthony , ELLIS, John Michael , FISCHER, Christian , GUERIN, David Joseph , HAIDLE, Andrew M. , KATTAR, Solomon , KNOWLES, Sandra Lee , LI, Chaomin , LIM, Jongwon , MACHACEK, Michelle , NORTHRUP, Alan B. , O'BOYLE, Brendan M. , OTTE, Ryan D. , PETROCCHI, Alessia , REUTERSHAN, Michael H. , ROMEO, Eric , SIU, Tony , TAOKA, Brandon M. , TROTTER, B. Wesley , ZHOU, Hua , BURCH, Jason , COTE, Bernard , DUPONT-GAUDET, Kristina , FOURNIER, Jean-Francois , GAUTHIER, Jacques Yves , GUAY, Daniel , ROBICHAUD, Joel S. , GRIMM, Jonathan , MADDESS, Matthew L. , SCHELL, Adam J. , SPENCER, Kerrie B. , WOO, Hyun Chong , BHAT, Sathesh
IPC分类号： C07D417/12 , C07D417/14 , A61K31/497 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00
CPC分类号： C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D495/04 , C07F9/65583
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公开(公告)号：EP2706852A1
公开(公告)日：2014-03-19
申请号：EP12782391.2
申请日：2012-05-04
发明人： DESCHENES, Denis , ALTMAN, Michael D. , ELLIS, John Michael , FISCHER, Christian , HAIDLE, Andrew M. , KATTAR, Solomon D. , NORTHRUP, Alan B. , SCHELL, Adam J. , SMITH, Graham F. , TAOKA, Brandon M. , BIENSTOCK, Corey , DI FRANCESCO, Maria Emilia , DONOFRIO, Anthony , PETERSON, Scott , SPENCER, Kerrie B. , JEWELL, James Patrick , ALI, Amjad , BENNETT, David Jonathan , DANG, Qun , WAL, John
IPC分类号： A01N43/40 , A61K31/44 , C07D213/04
CPC分类号： C07D401/14 , C07D401/12 , C07D409/14 , C07D417/14 , C07D471/04
摘要： The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.
摘要翻译： 本发明提供了式I的新型嘧啶胺，它们是脾酪氨酸激酶的有效抑制剂，或者是其前药，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD和类风湿性关节炎和癌症。
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公开(公告)号：EP2379075A1
公开(公告)日：2011-10-26
申请号：EP09836673.5
申请日：2009-12-07
IPC分类号： A61K31/4196 , C07D249/14
CPC分类号： C07D403/10 , C07D401/10
摘要： According to the invention there is provided a compound of formula (I): (I) or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aß42 and hence are useful in treatment of Alzheimer's disease and related conditions.
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公开(公告)号：EP2378879A1
公开(公告)日：2011-10-26
申请号：EP09833803.1
申请日：2009-12-07
发明人： FISCHER, Christian , METHOT, Joey , ZHOU, Hua , SCHELL, Adam, J. , MUNOZ, Benito , RIVKIN, Alexey, A. , AHEARN, Sean, P. , CHICHETTI, Stephanie , MACCOSS, Rachel, N. , KATTAR, Sam, D. , CHRISTOPHER, Matthew , LI, Chaomin , ROSENAU, Andrew , BROWN, William Colby
CPC分类号： A61K31/41 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aß42 and hence are useful in treatment of Alzheimer's disease and related conditions.
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公开(公告)号：EP2584903B1
公开(公告)日：2018-10-24
申请号：EP11798821.2
申请日：2011-06-22
发明人： DENG, Yongqi , ZHU, Liang , SHIPPS, Gerald, W., Jr. , LO, Sie-Mun , SUN, Binyuan , HUANG, Xiaohua , BEINSTOCK, Corey , COOPER, Alan, B. , GAO, Xiaolei , YAO, Xin , ZHU, Hugh, Y. , KELLY, Joseph, M. , BOGA, Sobhana Babu , ALHASSAN, Abdul-Basit , TAGAT, Jayaram, R. , MANSOOR, Umar Faruk , WILSON, Kevin , O'BOYLE, Brendan, M. , DANIELS, Matthew , SCHELL, Adam , SILIPHAIVANH, Phieng , FISCHER, Christian
IPC分类号： A01N43/56 , C07D231/56 , C07D209/48 , C07D235/04
CPC分类号： C07D401/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/1804
摘要： The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
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公开(公告)号：EP2770987B1
公开(公告)日：2018-04-04
申请号：EP12844405.6
申请日：2012-10-25
发明人： LIM, Jongwon , KELLEY, Elizabeth Helen , METHOT, Joey, L. , ZHOU, Hua , PETROCCHI, Alessia , MANSOOR, Umar Faruk , O'BOYLE, Brendan, M. , GUERIN, David Joseph , BIENSTOCK, Corey, E. , BOYCE, Christopher, W. , DANIELS, Matthew, H. , FALCONE, Danielle , FERGUSON, Ronald, D., II , FEVRIER, Salem , HUANG, Xiandai , LIPFORD, Kathryn Ann , SLOMAN, David, L. , WILSON, Kevin , ZHOU, Wei , WITTER, David , MALETIC, Milana, M. , SILIPHAIVANH, Phieng , FISCHER, Christian
IPC分类号： C07D471/04 , A61K9/66
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D519/00
摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
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28.发明授权SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS 有权取代的双嗪和三磷酸肌醇酪氨酸激酶（Syk）抑制剂
公开(公告)号：EP2863915B1
公开(公告)日：2017-12-06
申请号：EP13806343.3
申请日：2013-06-17
发明人： HAIDLE, Andrew, M. , ALTMAN, Michael, D. , KATTAR, Solomon, D. , CHRISTOPHER, Matthew. , ELLIS, John, Michael , FISCHER, Christian , NORTHRUP, Alan, B. , CHILDERS, Kaleen Konrad
IPC分类号： C07D239/42 , C07D239/47 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/506 , A61P11/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D239/42 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61K45/06 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
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公开(公告)号：EP3226690A1
公开(公告)日：2017-10-11
申请号：EP15866280.9
申请日：2015-12-01
发明人： FISCHER, Christian , BOGEN, Stephane, L. , CHILDERS, Matthew, L. , LLINAS, Francesc Xavier Fradera , KIM, Alexander, J. , LAMPE, John, W. , MACHACEK, Michelle, R. , MCMASTERS, Daniel, R. , PARKER, Dann, L., Jr. , SUN, Wanying , SCIAMMETTA, Nunzio , SHAO, Pengcheng, P. , SLOMAN, David, L. , UJJAINWALLA, Feroze , HUANG, Chunhui
IPC分类号： A01N43/00
CPC分类号： A61K31/5513 , A01N43/00 , A61K31/551 , A61K45/06 , A61P35/00 , C07D471/04 , C07D471/14 , C07D519/00 , A61K2300/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), (II-ii), (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
摘要翻译： 本发明涉及式（I）的三环化合物，其为一种或多种突变IDH酶的抑制剂：（I）; 其中A是-C（R 1）=或-N =; 并且X选自：（II-i），（II-ii），（II-iii）和（II-iv）。 本发明还涉及本文所述的三环化合物在潜在治疗或预防其中涉及一种或多种突变IDH酶的癌症中的用途。 本发明还涉及包含这些化合物的组合物。 本发明还涉及这些组合物在潜在的预防或治疗这些癌症中的用途。
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公开(公告)号：EP3226689A1
公开(公告)日：2017-10-11
申请号：EP15866163.7
申请日：2015-12-01
发明人： FISCHER, Christian , BOGEN, Stephane, L. , CHILDERS, Matthew, L. , LLINAS, Francesc Xavier Fradera , ELLIS, J. Michael , ESPOSITE, Sara , HOFFMAN, Dawn, M. , HUANG, Chunhui , KATTAR, Solomon , KIM, Alexander, J. , LAMPE, John, W. , MACHACEK, Michelle, R. , MCMASTERS, Daniel, R. , PARKER, Dann, L., Jr. , REUTERSHAN, Michael , SCIAMMETTA, Nunzio , SHAO, Pengcheng, P. , SLOMAN, David, L. , SUN, Wanying , UJJAINWALLA, Feroze , WU, Zhicai
IPC分类号： A01N43/00
CPC分类号： C07D471/04 , C07D471/14 , C07D519/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
摘要翻译： 本发明涉及式（I）的三环化合物，其为一种或多种突变IDH酶（I）的抑制剂; 其中A是-C（R 1）=或-N = X选自：（II-i）和（II-ii）。 本发明还涉及本文所述的三环化合物在潜在治疗或预防其中涉及一种或多种突变IDH酶的癌症中的用途。 本发明还涉及包含这些化合物的组合物。 本发明还涉及这些组合物在潜在的预防或治疗这些癌症中的用途。
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