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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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2.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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3.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：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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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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公开(公告)号：EP2512246A4
公开(公告)日：2014-07-09
申请号：EP10838241
申请日：2010-12-16
发明人： ALTMAN MICHAEL D , ARRINGTON KENNETH L , BURCH JASON , COTE BERNARD , FOURNIER JEAN-FRANCOIS , GAUTHIER JACQUES YVES , KATTAR SOLOMON , KNOWLES SANDRA LEE , LIM JONGWON , MACHACEK MICHELLE R , NORTHRUP ALAN B , REUTERSHAN MICHAEL H , ROBICHAUD JOEL S , SCHELL ADAM J , SPENCER KERRIE B
IPC分类号： C07D417/14 , A61K31/505 , A61P11/06 , C07D417/12 , C07D471/10 , C07D487/04 , C07D491/10
CPC分类号： C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10
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8.发明公开THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS 有权THIAZOLSUBSTITUIERTE AMINOHETEROARYLE ALS MILZTYROSINKINASEHEMMER
公开(公告)号：EP3082807A4
公开(公告)日：2017-05-10
申请号：EP14872398
申请日：2014-12-15
申请人： MERCK SHARP & DOHME
IPC分类号： C07D417/12 , A61K31/427 , A61P11/00
CPC分类号： C07D417/12 , A61K31/427 , A61K31/433 , A61K31/5377 , A61K45/06
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R3, R5, R6, A, Cy and the subscripts r, s, 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).
摘要翻译： 本发明提供了式（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中R 1，R 3，R 5，R 6，A，Cy和下标r，s和t如本文所定义。 本发明还提供了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）介导的疾病或病症的方法。
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9.发明公开SUBSTITUTED AMIDOPYRAZOLE INHIBITORS OF INTERLEUKIN RECEPTOR-ASSOCIATED KINASES (IRAK-4) 审中-公开替代亚胺基二苯并噻唑酮（IRAK-4）
公开(公告)号：EP3019171A4
公开(公告)日：2017-01-25
申请号：EP14823386
申请日：2014-07-07
申请人： MERCK SHARP & DOHME
发明人： LIM JONGWON , ALTMAN MICHAEL D
IPC分类号： A61K31/519 , A61K31/497 , A61K45/06 , A61P29/00 , C07D487/04
CPC分类号： A61K31/519 , A61K45/06 , C07D487/04 , A61K2300/00
摘要： This invention relates to amidopyrazole compounds that are inhibitors of Interieukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment of cellular proliferative diseases. Speifically (5-methylpyridin-2-yl)-1 H-pyrazol-5-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamide derivatives are disclosed for use in the method of treating inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease and cancer.
摘要翻译： 本发明涉及作为白介素受体相关激酶抑制剂，特别是IRAK-4的氨基吡唑化合物，可用于治疗细胞增殖性疾病。 公开了用于治疗炎症性疾病如类风湿性关节炎的方法中使用的（5-甲基吡啶-2-基）-1H-吡唑-5-基]吡唑并[1,5-a]嘧啶-3-甲酰胺衍生物， 炎性肠病和癌症。
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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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