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1.发明授权
公开(公告)号：EP2758050B1
公开(公告)日：2016-08-31
申请号：EP12834358.9
申请日：2012-09-21
Applicant: Merck Sharp & Dohme Corp.
Inventor： BRUBAKER, Jason , CLOSE, Joshua, T. , JUNG, Joon , MARTINEZ, Michelle , WHITE, Catherine , WILSON, Kevin , YOUNG, Jonathan, R. , ZHANG, Hongjun
IPC: C07D403/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D231/38 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/14 , A61K31/415 , A61P35/00
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
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公开(公告)号：EP2758389A1
公开(公告)日：2014-07-30
申请号：EP12834277.1
申请日：2012-09-21
Applicant: Merck Sharp & Dohme Corp.
Inventor： BRUBAKER, Jason , CLOSE, Joshua , SIU, Tony , SMITH, Graham Frank , TORRES, Luis E. , WOO, Hyun Chong , YOUNG, Jonathan R. , WEI, Zhongyong , SHI, Feng
IPC: C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/4155 , A61K31/4439 , A61K31/541 , A61P11/00 , A61P29/00 , A61P35/00
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.
Abstract translation: 本发明提供了式（I）化合物，它们是JAK抑制剂，因此可用于治疗JAK介导的疾病，例如类风湿性关节炎，哮喘，COPD和癌症。
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3.发明公开CYCLOBUTYL SULFONES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 有权CYCLOBUTYL SULFONES作为NOTCH SPARING GAMMA SECRETASE抑制剂
公开(公告)号：EP2273877A1
公开(公告)日：2011-01-19
申请号：EP09734395.8
申请日：2009-04-17
Applicant: Merck Sharp & Dohme Corp.
Inventor： HEIDEBRECHT, Richard, W. , LI, Chaomin , MUNOZ, Benito , ROSENAU, Andrew , SURDI, Laura, M. , TEMPEST, Paul , SILIPHAIVANH, Phieng , BRUBAKER, Jason
CPC classification number: C07C317/30 , C07C2601/04 , C07D309/12
Abstract: The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
Abstract translation: 本发明包括一类新的环丁基砜衍生物，其抑制由推定的γ-分泌酶加工APP而同时保留Notch信号传导途径，因此可用于治疗或预防阿尔茨海默氏病而不发展Notch抑制介导的胃肠问题。 药物组合物和使用方法也包括在内。
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公开(公告)号：EP2976340B1
公开(公告)日：2018-06-13
申请号：EP14767371.9
申请日：2014-03-19
Applicant: Merck Sharp & Dohme Corp.
Inventor： CHILDERS, Matthew Lloyd , DINSMORE, Christopher , FULLER, Peter , GUERIN, David , KATZ, Jason David , PU, Qinglin , SCOTT, Mark E. , THOMPSON, Christopher F. , ZHANG, Hongjun , FALCONE, Danielle , TORRES, Luis , BRUBAKER, Jason , ZENG, Hongbo , CAI, Jiaqiang , DU, Xiaoxing , WANG, Chonggang , BAI, Yunfeng , KONG, Norman , LIU, Yumei , ZHENG, Zhixiang
IPC: C07D487/04 , C07D487/08 , C07D487/14 , A61K31/437 , A61K31/4375 , A61P25/00 , A61P35/00 , A61P37/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: Compounds of formula I are provided, which are JAK inhibitors and 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：EP2976340A1
公开(公告)日：2016-01-27
申请号：EP14767371.9
申请日：2014-03-19
Applicant: Merck Sharp & Dohme Corp.
Inventor： CHILDERS, Matthew Lloyd , DINSMORE, Christopher , FULLER, Peter , GUERIN, David , KATZ, Jason David , PU, Qinglin , SCOTT, Mark E. , THOMPSON, Christopher F. , ZHANG, Hongjun , FALCONE, Danielle , TORRES, Luis , BRUBAKER, Jason , ZENG, Hongbo , CAI, Jiaqiang , DU, Xiaoxing , WANG, Chonggang , BAI, Yunfeng , KONG, Norman , LIU, Yumei , ZHENG, Zhixiang
IPC: C07D487/04 , C07D487/08 , C07D487/14 , A61K31/437 , A61K31/4375 , A61P25/00 , A61P35/00 , A61P37/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Abstract translation: 提供了式I化合物，它们是JAK抑制剂并且可用于治疗JAK介导的疾病，例如类风湿性关节炎，哮喘，COPD和癌症。
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Patent Agency Ranking6.发明公开CYCLOALKYLNITRILE PYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS 有权环丙基鸟氨酸吡啶甲酰胺ALS JANUSKINASEINHIBITOREN
公开(公告)号：EP2758377A1
公开(公告)日：2014-07-30
申请号：EP12833410.9
申请日：2012-09-21
Applicant: Merck Sharp & Dohme Corp.
Inventor： BRUBAKER, Jason , DINSMORE, Christopher J. , HOFFMAN, Dawn Marie , JUNG, Joon , LIU, Duan , PETERSON, Scott , SIU, Tony , TORRES, Luis E. , ZHANG, Hongjun , WEI, Zhongyong , SHI, Feng
IPC: C07D231/10 , A61K31/415 , A61P37/00 , A61P35/00
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: Cycloalkylnitrile pyrazole carboxamides as JAK inhibitors useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer are provided.
Abstract translation: 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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7.发明授权CYCLOBUTYL SULFONES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 有权CYCLOBUTYL SULFONES作为NOTCH SPARING GAMMA SECRETASE抑制剂
公开(公告)号：EP2273877B1
公开(公告)日：2014-04-16
申请号：EP09734395.8
申请日：2009-04-17
Applicant: Merck Sharp & Dohme Corp.
Inventor： HEIDEBRECHT, Richard, W. , LI, Chaomin , MUNOZ, Benito , ROSENAU, Andrew , SURDI, Laura, M. , TEMPEST, Paul , SILIPHAIVANH, Phieng , BRUBAKER, Jason
CPC classification number: C07C317/30 , C07C2601/04 , C07D309/12
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8.发明授权CYANOMETHYLPYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS 有权CYANOMETHYLPYRAZOLE CARBOXIDES作为JANUS激酶抑制剂
公开(公告)号：EP2758051B1
公开(公告)日：2018-04-11
申请号：EP12834379.5
申请日：2012-09-21
Applicant: Merck Sharp & Dohme Corp.
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 , C07D405/14 , C07D413/14 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/14 , A61K31/415 , A61P11/06
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：EP2758389B1
公开(公告)日：2017-06-07
申请号：EP12834277.1
申请日：2012-09-21
Applicant: Merck Sharp & Dohme Corp.
Inventor： BRUBAKER, Jason , CLOSE, Joshua , SIU, Tony , SMITH, Graham Frank , TORRES, Luis E. , WOO, Hyun Chong , YOUNG, Jonathan R. , WEI, Zhongyong , SHI, Feng
IPC: C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/4155 , A61K31/4439 , A61K31/541 , A61P11/00 , A61P29/00 , A61P35/00
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
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10.发明公开N-(2-CYANO HETEROCYCLYL)PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS 有权N-（2-氰基 - 杂环基）吡唑并吡啶酮JANUSKINASEINHIBITOREN
公开(公告)号：EP2976338A1
公开(公告)日：2016-01-27
申请号：EP14767458.4
申请日：2014-03-19
Applicant: Merck Sharp & Dohme Corp.
Inventor： DINSMORE, Christopher , FULLER, Peter , GUERIN, David , THOMPSON, Christopher F. , PU, Qinglin , SCOTT, Mark E. , KATZ, Jason David , KURUKULASURIYA, Ravi , CLOSE, Joshua T. , FALCONE, Danielle , BRUBAKER, Jason , ZENG, Hongbo , BAI, Yunfeng , FU, Jianmin , KONG, Norman , LIU, Yumei , ZHENG, Zhixiang
IPC: C07D471/04 , A61K31/437 , A61P35/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
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