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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
Applicant: MERCK SHARP & DOHME , MERCK CANADA INC
Inventor： 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: A61K31/50 , A61K31/501 , C07D401/14 , C07D403/12 , C07D403/14
CPC classification number: C07D403/12 , C07D401/14 , C07D403/14
Abstract: 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.
Abstract translation: 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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2.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
Applicant: MERCK SHARP & DOHME , MERCK CANADA INC
Inventor： 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: 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 classification number: 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
Abstract: 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.
Abstract translation: 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
Applicant: MERCK SHARP & DOHME , MERCK CANADA INC
Inventor： 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: C07D417/12 , A61K31/506 , A61P11/06 , A61P29/00 , A61P35/00 , C07D239/50 , C07D417/14
CPC classification number: 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
Abstract: 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.
Abstract translation: 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：EP2863914A4
公开(公告)日：2015-12-16
申请号：EP13807800
申请日：2013-06-18
Applicant: MERCK SHARP & DOHME , MERCK CANADA INC
Inventor： 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: A61K31/50 , A61K31/501 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04
CPC classification number: C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
Abstract: 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.
Abstract translation: 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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5.发明公开SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS 有权SUBSTITUIERTE PHENYL-MILZ-TYROSINKINASEINHIBITOREN
公开(公告)号：EP2884982A4
公开(公告)日：2016-03-30
申请号：EP13831537
申请日：2013-08-15
Applicant: MERCK SHARP & DOHME , MERCK CANADA INC
Inventor： 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: A61K31/54 , A61K31/505 , A61K31/506
CPC classification number: 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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Patent Agency Ranking
公开(公告)号：EP2788000A4
公开(公告)日：2015-11-18
申请号：EP12855868
申请日：2012-11-30
Applicant: MERCK SHARP & DOHME
Inventor： AHEARN SEAN P , CHRISTOPHER MATTHEW , JUNG JOON , PU QINGLIN , RIVKIN ALEXEY , SCOTT MARK E , WITTER DAVID J , WOO HYUN CHONG , CASH BRANDON , DINSMORE CHRISTOPHER , GUERIN DAVID
IPC: A61K31/519 , C07D471/04 , C07D487/04 , C07D519/00
CPC classification number: C07D487/04 , C07D471/04 , C07D519/00
Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.
Abstract translation: 本发明提供了作为JAK3抑制剂的式I化合物。 具体地，式I化合物是吡咯并[2,3-d]嘧啶衍生物化合物。 本发明还提供了通过给予式I的吡咯并[2,3-d]嘧啶衍生物化合物来治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症的方法。
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7.发明公开
公开(公告)号：EP2863915A4
公开(公告)日：2015-12-23
申请号：EP13806343
申请日：2013-06-17
Applicant: MERCK SHARP & DOHME
Inventor： HAIDLE ANDREW M , ALTMAN MICHAEL D , KATTAR SOLOMON D , CHRISTOPHER MATTHEW , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , NORTHRUP ALAN B , CHILDERS KALEEN KONRAD
IPC: C07D239/42 , A61K31/506 , A61P11/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , C07D239/47 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC classification number: 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
Abstract: 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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8.发明公开
公开(公告)号：EP2758051A4
公开(公告)日：2015-03-18
申请号：EP12834379
申请日：2012-09-21
Applicant: MERCK SHARP & DOHME
Inventor： BRUBAKER JASON , CHILDERS MATTHEW LLOYD , CHRISTOPHER MATTHEW , CLOSE JOSHUA T , KATZ JASON DAVID , JUNG JOON , PETERSON SCOTT , SILIPHAIVANH PHIENG , SIU TONY , SMITH GRAHAM FRANK , TORRES LUIS E , WOO HYUN CHONG , YOUNG JONATHAN R , ZHANG HONGJUN
IPC: C07D401/14 , A61K31/415 , A61P11/06 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
CPC classification number: C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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公开(公告)号：EP2378879A4
公开(公告)日：2012-06-06
申请号：EP09833803
申请日：2009-12-07
Applicant: MERCK SHARP & DOHME
Inventor： 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 classification number: A61K31/41 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
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公开(公告)号：EP2166846A4
公开(公告)日：2011-03-23
申请号：EP08768504
申请日：2008-06-16
Applicant: MERCK SHARP & DOHME
Inventor： ALTMAN MICHAEL , CHRISTOPHER MATTHEW , GRIMM JONATHAN B , HAIDLE ANDREW , KONRAD KALEEN , LIM JONGWON , MACCOSS RACHEL N , MACHACEK MICHELLE , OSIMBONI EKUNDAYO , OTTE RYAN D , SIU TONY , SPENCER KERRIE , TAOKA BRANDON , TEMPEST PAUL , WILSON KEVIN , WOO HYUN CHONG , YOUNG JONATHAN , ZABIEREK ANNA
IPC: C07D409/12 , A61K31/381 , A61K31/44 , A61P35/00 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/10 , C07F9/6558
CPC classification number: C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/10 , C07F9/65586 , C07F9/65685
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