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公开(公告)号:EP2863914A4
公开(公告)日:2015-12-16
申请号:EP13807800
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 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04
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,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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2.SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS 有权
标题翻译: 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: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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4.2-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS 有权
标题翻译: 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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5.DIARYL ETHER DERIVATIVES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 审中-公开
标题翻译: 二芳基醚衍生物作为抗缺损型的GAMMETETETER抑制剂公开(公告)号:EP2488031A4
公开(公告)日:2014-07-23
申请号:EP10823842
申请日:2010-10-05
申请人: MERCK SHARP & DOHME
发明人: BROWN WILLIAM COLBY , HEIDEBRECHT RICHARD W , BRUBAKER JASON , FISCHER CHRISTIAN , HENDRIX JOHN T , KELLEY ELIZABETH H , MACCOSS RACHEL N , METHOT JOEY L , MILLER THOMAS , OTTE KARIN M , SILIPHAIVANH PHIENG , REGER THOMAS , WILLIAMS PETER D , WISCOUNT CATHERINE M
IPC分类号: C07D231/20 , A61K31/415 , A61P25/28 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/113
CPC分类号: C07D231/22 , C07D231/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/113
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公开(公告)号:EP2770987A4
公开(公告)日:2015-04-08
申请号:EP12844405
申请日:2012-10-25
申请人: MERCK SHARP & DOHME
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: 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).
摘要翻译: 公开了式(1)的ERK抑制剂及其药学上可接受的盐。 还公开了使用式(1)的化合物治疗癌症的方法。
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公开(公告)号:EP2117311A4
公开(公告)日:2011-05-11
申请号:EP08725176
申请日:2008-02-05
申请人: MERCK SHARP & DOHME
发明人: FISCHER CHRISTIAN , MUNOZ BENITO , RIVKIN ALEXEY A
IPC分类号: C07D403/10 , A61K31/415 , C07D413/10 , C07D413/14 , C07D417/10 , C07D487/04 , C07D491/04 , C07D495/04
CPC分类号: C07D487/04 , C07D403/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D491/04 , C07D495/04
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公开(公告)号:EP3226689A4
公开(公告)日:2018-06-13
申请号:EP15866163
申请日:2015-12-01
申请人: MERCK SHARP & DOHME
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: A61K31/551 , A61P35/00 , C07D471/04 , C07D471/14 , C07D519/00
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.
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公开(公告)号:EP2706853A4
公开(公告)日:2014-11-05
申请号:EP12782298
申请日:2012-05-04
申请人: MERCK SHARP & DOHME
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 , A61K31/506 , A61P11/06 , A61P35/00 , C07D417/12 , C07D417/14
CPC分类号: C07D417/12 , C07D417/14
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公开(公告)号:EP2563125A4
公开(公告)日:2013-10-02
申请号:EP11775457
申请日:2011-04-21
申请人: MERCK SHARP & DOHME
发明人: CASH BRANDON , FISCHER CHRISTIAN , GARCIA YUDITH , JUNG JOON , KATZ JASON , KIM JUNE , RIVKIN ALEXEY , SCHELL ADAM , SIU TONY , WITTER DAVID , ZHOU HUA
IPC分类号: C07D471/04 , A01N43/42 , A61K31/44 , C07D519/00
CPC分类号: C07D471/04 , C07D519/00
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