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公开(公告)号：EP2900665A1
公开(公告)日：2015-08-05
申请号：EP13841430.5
申请日：2013-09-24
发明人： MACHACEK, Michelle R. , ROMEO, Eric T. , KATTAR, Solomon D. , CHRISTOPHER, Matthew , ALTMAN, Michael D. , NORTHRUP, Alan B. , ELLIS, John Michael , BOYLE, Brendan O' , DONOFRIO, Anthony , GRIMM, Jonathan , REUTERSHAN, Michael H. , CHILDERS, Kaleen Konrad , OTTE, Ryan D. , CASH, Brandon , DUCHARME, Yves , HAIDLE, Andrew M. , SPENCER, Kerrie , VITHARANA, Dilrukshi , WU, Lingyun , ZHANG, Li , ZHANG, Peng , BEAULIEU, Christian , GUAY, Daniel
IPC分类号： C07D417/12 , C07D417/14 , C07D239/50 , A61K31/506 , A61P11/06 , A61P29/00 , A61P35/00
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 提供了式I的三唑衍生物，它们是有效的脾酪氨酸激酶抑制剂和药物组合物。 三唑衍生物可用于治疗和预防由所述酶介导的疾病，如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：EP2513098A1
公开(公告)日：2012-10-24
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
摘要： The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
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，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。
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公开(公告)号：EP2988744A1
公开(公告)日：2016-03-02
申请号：EP14788026.4
申请日：2014-04-22
发明人： ANTHONY, Neville, J. , ANDRESEN, Brian, M. , NORTHRUP, Alan, B. , CHILDERS, Kaleen, K. , DONOFRIO, Anthony , MILLER, Thomas, A. , LIU, Yuan , MACHACEK, Michelle, R. , WOO, Hyun Chong , SPENCER, Kerrie, B. , ELLIS, John Michael , ALTMAN, Michael, D. , ROMEO, Eric, T. , GUAY, Daniel , GRIMM, Jonathan , LEBRUN, Marie-Eve , ROBICHAUD, Joel, S. , WANG, Liping , DUBOIS, Byron , DENG, Qiaolin
IPC分类号： A61K31/44 , A61K31/53 , A61K31/426
CPC分类号： C07D417/14 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 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).
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公开(公告)号：EP2900665B1
公开(公告)日：2018-01-03
申请号：EP13841430.5
申请日：2013-09-24
发明人： MACHACEK, Michelle R. , ROMEO, Eric T. , KATTAR, Solomon D. , CHRISTOPHER, Matthew , ALTMAN, Michael D. , NORTHRUP, Alan B. , ELLIS, John Michael , BOYLE, Brendan O' , DONOFRIO, Anthony , GRIMM, Jonathan , REUTERSHAN, Michael H. , CHILDERS, Kaleen Konrad , OTTE, Ryan D. , CASH, Brandon , DUCHARME, Yves , HAIDLE, Andrew M. , SPENCER, Kerrie , VITHARANA, Dilrukshi , WU, Lingyun , ZHANG, Li , ZHANG, Peng , BEAULIEU, Christian , GUAY, Daniel
IPC分类号： C07D417/12 , C07D417/14 , C07D239/50 , A61K31/506 , A61P11/06 , A61P29/00 , A61P35/00
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
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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：EP2884982A2
公开(公告)日：2015-06-24
申请号：EP13831537.9
申请日：2013-08-15
发明人： HAIDLE, Andrew, M. , BURCH, Jason , GUAY, Daniel , GAUTHIER, Jacques Yves , ROBICHAUD, Joel , FOURNIER, Jean Francois , ELLIS, John Michael , CHRISTOPHER, Matthew , KATTAR, Solomon, D. , SMITH, Graham , NORTHRUP, Alan, B.
IPC分类号： A61K31/54 , A61K31/505 , A61K31/506
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
摘要： The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R
1 , R
2 , R
3 , R
4 , R
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).-
公开(公告)号：EP2863914B1
公开(公告)日：2018-10-03
申请号：EP13807800.1
申请日：2013-06-18
发明人： MACHACEK, Michele, R. , ALTMAN, Michael, D. , ROMEO, Eric, T. , WITHARANA, Dilrukshi , CASH, Brandon , SIU, Tony , ZHOU, Hua , CHRISTOPHER, Matthew , KATTAR, Solomon, D. , HAIDLE, Andrew, M. , CHILDERS, Kaleen Konrad , MADDESS, Matthew, H. , REUTERSHAN, Michael, H. , DUCHARME, Yves , GUERIN, David, J. , SPENCER, Kerrie , BEAULIEU, Christian , TRUONG, Vouy Linh , GUAY, Daniel , NORTHRUP, Alan, B. , TAOKA, Brandon, M. , LIM, Jongwon , FISCHER, Christian , BUTCHER, John, W. , OTTE, Ryan, D. , SUN, Binyuan , ELLIS, John, Michael
IPC分类号： A61K31/50 , A61K31/501 , C07D401/14 , C07D405/14 , C07D413/14 , C07D403/14 , C07D409/14 , C07D471/04 , C07D403/12
CPC分类号： C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
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公开(公告)号：EP2884982B1
公开(公告)日：2017-09-20
申请号：EP13831537.9
申请日：2013-08-15
发明人： HAIDLE, Andrew, M. , BURCH, Jason , GUAY, Daniel , GAUTHIER, Jacques Yves , ROBICHAUD, Joel , FOURNIER, Jean Francois , ELLIS, John Michael , CHRISTOPHER, Matthew , KATTAR, Solomon, D. , SMITH, Graham , NORTHRUP, Alan, B.
IPC分类号： A61K31/54 , A61K31/505 , A61K31/506
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
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公开(公告)号：EP2863914A1
公开(公告)日：2015-04-29
申请号：EP13807800.1
申请日：2013-06-18
发明人： MACHACEK, Michele, R. , ALTMAN, Michael, D. , ROMEO, Eric, T. , WITHARANA, Dilrukshi , CASH, Brandon , SIU, Tony , ZHOU, Hua , CHRISTOPHER, Matthew , KATTAR, Solomon, D. , HAIDLE, Andrew, M. , CHILDERS, Kaleen Konrad , MADDESS, Matthew, H. , REUTERSHAN, Michael, H. , DUCHARME, Yves , GUERIN, David, J. , SPENCER, Kerrie , BEAULIEU, Christian , TRUONG, Vouy Linh , GUAY, Daniel , NORTHRUP, Alan, B. , TAOKA, Brandon, M. , LIM, Jongwon , FISCHER, Christian , BUTCHER, John, W. , OTTE, Ryan, D. , SUN, Binyuan , ELLIS, John, Michael
IPC分类号： A61K31/50 , A61K31/501
CPC分类号： C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 本发明提供了式I的新型吡唑衍生物，它们是脾酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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10.发明授权ALKYNE-ARYL-NAPHTHYRIDIN-4(1H)-0NE DERIVATIVES AS TYPE IV PHOSPHODIESTERASE INHIBITOR 有权炔芳基萘啶-4（1H）-0NE衍生物作为IV型磷酸的抑制剂
公开(公告)号：EP1436290B8
公开(公告)日：2013-12-04
申请号：EP02754079.8
申请日：2002-08-27
申请人： Merck Canada Inc.
IPC分类号： C07D471/04 , C07D519/00 , A61K31/435
CPC分类号： A61K45/06 , A61K31/435 , A61K31/4375 , C07D471/04 , A61K2300/00
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