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公开(公告)号:EP3233859A4
公开(公告)日:2018-06-13
申请号:EP15870726
申请日:2015-12-10
发明人: SLOMAN DAVID L , WITTER DAVID , MANSOOR UMAR FARUK
IPC分类号: C07D471/04
CPC分类号: C07D498/18 , A61K31/437 , A61K31/444 , C07D471/18 , C07D471/22
摘要: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).
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公开(公告)号:EP3226690A4
公开(公告)日:2018-06-20
申请号:EP15866280
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 , KIM ALEXANDER J , LAMPE JOHN W , MACHACEK MICHELLE R , MCMASTERS DANIEL R , PARKER DANN L JR , SUN WANYING , SCIAMMETTA NUNZIO , SHAO PENGCHENG P , SLOMAN DAVID L , UJJAINWALLA FEROZE , HUANG CHUNHUI
IPC分类号: C07D471/04 , A01N43/00 , A61K31/551 , A61K31/5513 , A61P35/00 , C07D471/14 , C07D519/00
CPC分类号: A61K31/5513 , A01N43/00 , A61K31/551 , A61K45/06 , A61P35/00 , C07D471/04 , C07D471/14 , C07D519/00 , A61K2300/00
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), (II-ii), (II-iii), and (II-iv). 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:EP3082810A4
公开(公告)日:2017-05-10
申请号:EP14871205
申请日:2014-12-12
申请人: MERCK SHARP & DOHME
IPC分类号: C07D471/04 , A61K31/437 , A61P35/00
CPC分类号: C07D471/04 , A61K31/437 , A61K31/444 , A61K45/06 , A61K2300/00
摘要: Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.
摘要翻译: 公开了式(1.0)的ERK抑制剂及其药学上可接受的盐。 还公开了使用式(1.0)化合物治疗癌症的方法。 本发明提供了ERK抑制剂(即ERK2抑制剂)的化合物。 本发明还提供了包含有效量的至少一种(例如1种)式(1.0)化合物和药学上可接受的载体的药物组合物。
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公开(公告)号:EP2523552A4
公开(公告)日:2013-06-19
申请号:EP11733241
申请日:2011-01-11
申请人: MERCK SHARP & DOHME
发明人: LIM JONGWON , TAOKA BRANDON M , LEE SANDRA , NORTHRUP ALAN , ALTMAN MICHAEL D , SLOMAN DAVID L , STANTON MATTHEW G , NOUCTI NJAMKOU
IPC分类号: C07D487/04 , A61K31/519 , A61P25/28
CPC分类号: C07D487/04
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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:EP1945028A4
公开(公告)日:2011-01-19
申请号:EP06826996
申请日:2006-10-30
申请人: MERCK SHARP & DOHME
发明人: HAMBLETT CHRISTOPHER , MAMPREIAN DAWN M , METHOT JOEY L , MILLER THOMAS , SLOMAN DAVID L , STANTON MATTHEW G , WILSON KEVIN
CPC分类号: C07D213/56 , C07D239/28 , C07D401/12 , C07D487/08
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公开(公告)号:EP3233858A4
公开(公告)日:2018-06-13
申请号:EP15870725
申请日:2015-12-10
申请人: MERCK SHARP & DOHME
发明人: SILIPHAIVANH PHIENG , METHOT JOEY , LIPFORD KATHRYN ANN , MOLINARI DANIELLE , SLOMAN DAVID L , WITTER DAVID , ZHOU HUA , BOYCE CHRISTOPHER , HUANG XIANHAI , LIM JONGWON , GUERIN DAVID , KARUNAKARAN GANESH BABU , BAKSHI RAMAN KUMAR , LIU ZIPING , FU JIANMIN , WAN ZHILONG , LIU WEI
IPC分类号: C07D471/04
CPC分类号: A61K31/437 , A61K31/444 , A61K31/4545 , C07D471/04 , C07D519/00
摘要: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.
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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:EP1976511A4
公开(公告)日:2010-09-08
申请号:EP07762514
申请日:2007-01-09
申请人: MERCK SHARP & DOHME
IPC分类号: A61K31/38 , C07D231/40 , C07D333/70 , C07D409/12
CPC分类号: C07D231/40 , C07D333/20 , C07D333/70 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14
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