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公开(公告)号：EP2863913A4
公开(公告)日：2015-12-16
申请号：EP13807108
申请日：2013-06-18
发明人： LIM JONGWON , REUTERSHAN MICHAEL H , ELLIS JOHN MICHAEL , CHILDERS KALEEN KONRAD , DONOFRIO ANTHONY , ALTMAN MICHAEL D , HAIDLE ANDREW M , ZABIEREK ANNA , CHRISTOPHER MATTHEW , GRIMM JONATHAN , BURCH JASON , FRANCESCO MARIA EMILIA DI , PETROCCHI ALESSIA , BEAULIEU CHRISTIAN , TRUONG VOUY LINH , NORTHRUP ALAN B , BLOUIN MARC
IPC分类号： A61K31/50 , A61K31/501 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14
摘要： The present invention provides novel imidazole analogs 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的新型咪唑类似物，其是脾脏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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公开(公告)号：EP2706852A4
公开(公告)日：2014-11-05
申请号：EP12782391
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，其是脾脏酪氨酸激酶的有效抑制剂，或其前药，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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3.发明公开THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS 审中-公开噻唑取代的氨基水杨酸作为米氮芥诱导酶抑制剂
公开(公告)号：EP2988744A4
公开(公告)日：2016-11-02
申请号：EP14788026
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 , A61K31/426 , A61K31/53 , A61P11/00 , A61P19/00 , C07D417/12 , C07D417/14
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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4.发明公开SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS 有权SUBSTITUIERTE PYRIDIN-MILZ-TYROSINKINASEINHIBITOREN
公开(公告)号：EP2863916A4
公开(公告)日：2015-12-16
申请号：EP13807050
申请日：2013-06-17
发明人： HAIDLE ANDREW M , KNOWLES SANDRA LEE , KATTAR SOLOMON D , DESCHENES DENIS , BURCH JASON , ROBICHAUD JOEL , CHRISTOPHER MATTHEW , ALTMAN MICHAEL D , JEWELL JAMES P , NORTHHRUP ALAN B , BLOUIN MARC , ELLIS JOHN MICHAEL , ZHOU HUA , FISCHER CHRISTIAN , SCHELL ADAM J , REUTERSHAN MICHAEL H , TAOKA BRANDON M , DONOFRIO ANTHONY
IPC分类号： C07D401/12 , A61K31/506 , A61P11/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/08 , C07D491/107 , C07D491/113 , C07D498/04
CPC分类号： C07D401/12 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/08 , C07D491/107 , C07D491/113 , C07D498/04 , A61K2300/00
摘要： The invention provides certain substituted pyridines of the Formula (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.
摘要翻译： 本发明提供了式（I）的某些取代的吡啶或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy，Cy和t如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。
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公开(公告)号：EP2900665A4
公开(公告)日：2016-03-23
申请号：EP13841430
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 , A61K31/506 , A61P11/06 , A61P29/00 , A61P35/00 , C07D239/50 , C07D417/14
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： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物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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公开(公告)号：EP3200789A4
公开(公告)日：2018-04-11
申请号：EP15847222
申请日：2015-09-25
申请人： MERCK SHARP & DOHME
发明人： ALTMAN MICHAEL D , BRUBAKER JASON D , CHILDERS MATTHEW L , DONOFRIO ANTHONY , FISCHMANN THIERRY , GIBEAU CRAIG R , KATTAR SOLOMON D , LESBURG CHARLES A , LIM JONGWON , MACLEAN JOHN K F , MANSOOR UMAR F , NORTHRUP ALAN B , SANDERS JOHN M , SMITH GRAHAM F
IPC分类号： A61K31/444 , A61K31/506 , A61K45/06 , A61P29/00 , A61P35/00 , C07D239/88 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12
CPC分类号： C07D491/08 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/5386 , A61K31/55 , A61K45/06 , A61P29/00 , A61P35/00 , C07D239/88 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D491/048 , C07D491/052 , C07D498/08 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibutors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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7.发明公开2-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS 有权2-吡啶基甲酰胺CONTAINING MILZTYROSINKINASE抑制剂
公开(公告)号：EP2763976A4
公开(公告)日：2015-03-04
申请号：EP12838717
申请日：2012-10-01
申请人： MERCK SHARP & DOHME
发明人： ALTMAN MICHAEL D , BIENSTOCK CORE E , BUTCHER JOHN W , DI FRANCESCO MARIA EMILIA , DONOFRIO ANTHONY , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , HAIDLE ANDREW M , HAIDLE ANDREW M , JEWELL JAMES P , KNOWLES SANDRA LEE , NORTHRUP ALAN B , OTTE RYAN D , PETERSON SCOTT L , SMITH GRAHAM FRANK
IPC分类号： C07D401/00 , A61P37/00
CPC分类号： A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K31/5377 , C07D213/81 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D495/04
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公开(公告)号：EP3200787A4
公开(公告)日：2018-03-28
申请号：EP15846218
申请日：2015-09-25
申请人： MERCK SHARP & DOHME
发明人： ALTMAN MICHAEL D , ANDRESEN BRIAN M , BRUBAKER JASON D , CHILDERS MATTHEW L , DONOFRIO ANTHONY , FISCHMANN THIERRY , GIBEAU CRAIG R , KATTAR SOLOMON D , LESBURG CHARLES A , LIM JONGWON , MACLEAN JOHN K F , MANSOOR UMAR F , NORTHRUP ALAN B , SANDERS JOHN M , SMITH GRAHAM F , TORRES LUIS
IPC分类号： A61K31/444 , A61K31/506 , A61K45/06 , A61P37/00 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/14
CPC分类号： C07D498/04 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K45/06 , A61P37/00 , C07D239/94 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/048 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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公开(公告)号：EP3200790A4
公开(公告)日：2018-05-16
申请号：EP15847644
申请日：2015-09-25
申请人： MERCK SHARP & DOHME
发明人： ALTMAN MICHAEL D , ANDRESEN BRIAN M , BRUBAKER JASON D , DONOFRIO ANTHONY , FISCHMANN THIERRY , GIBEAU CRAIG R , LESBURG CHARLES A , LIM JONGWON , MACLEAN JOHN K F , MANSOOR UMAR F , NORTHRUP ALAN B , SANDERS JOHN M , SMITH GRAHAM F , TORRES LUIS
IPC分类号： A61K31/444 , A61K31/506 , A61K45/06 , A61P29/00 , A61P35/00 , C07D239/94 , C07D405/04
CPC分类号： A61K31/517 , A61K45/06 , A61P29/00 , A61P35/00 , C07D239/94 , C07D405/04 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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公开(公告)号：EP3200788A4
公开(公告)日：2018-02-28
申请号：EP15846420
申请日：2015-09-25
申请人： MERCK SHARP & DOHME
发明人： ALTMAN MICHAEL D , BRUBAKER JASON D , CHILDERS MATTHEW L , DONOFRIO ANTHONY , FISCHMANN THIERRY , GIBEAU CRAIG R , KATTAR SOLOMON D , LESBURG CHARLES A , LIM JONGWON , MACLEAN JOHN K F , MANSOOR UMAR F , NORTHRUP ALAN B , SANDERS JOHN M , SMITH GRAHAM F
IPC分类号： C07D239/88 , A61K31/444 , A61K31/506 , A61K45/06 , A61P19/00 , A61P29/00 , A61P35/00 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D491/107
CPC分类号： C07D491/107 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , A61P19/00 , A61P29/00 , A61P35/00 , C07D239/88 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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