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公开(公告)号：US10072025B2
公开(公告)日：2018-09-11
申请号：US15519740
申请日：2015-10-21
发明人： Mark E. Scott , David Guerin , Danielle Molinari , Sam Kattar , Peter Fuller , Christopher Dinsmore , Norman Kong , Yunfeng Bai , Jianmin Fu , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D519/00 , C07D471/04 , A61K31/4545 , A61K31/5377 , A61K31/538 , A61K31/55 , A61K31/553 , A61K31/554 , A61K31/541
CPC分类号： C07D519/00 , A61K31/00 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/5377 , A61K31/538 , A61K31/541 , A61K31/55 , A61K31/553 , A61K31/554 , A61P11/06 , A61P19/02 , A61P35/00 , C07D471/04
摘要： 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. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds.
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公开(公告)号：US09957265B2
公开(公告)日：2018-05-01
申请号：US14778052
申请日：2014-03-19
发明人： Christopher Dinsmore , Peter Fuller , David Guerin , Christopher F. Thompson , Qinglin Pu , Mark E. Scott , Jason David Katz , Ravi Kurukulasuriya , Joshua T. Close , Danielle Falcone , Jason Brubaker , Hongbo Zeng , Yunfeng Bai , Jianmin Fu , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： 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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公开(公告)号：US20180179190A1
公开(公告)日：2018-06-28
申请号：US15737334
申请日：2016-06-24
发明人： Frank Bennett , Jinlong Jiang , Alexander Pasternak , Shuzhi Dong , Xin Gu , Jack D. Scott , Haiqun Tang , Zhiqiang Zhao , Yuhua Huang , David Hunter , Dexi Yang , Katherine Young , Li Xiao , Zhibo Zhang , Jianmin Fu , Yunfeng Bai , Zhixiang Zheng , Xu Zhang
IPC分类号： C07D403/14 , A61K45/06 , A61K31/4184 , C07D401/14 , A61K31/454 , C07D471/04 , A61K31/437 , A61K31/4545 , C07D487/04 , A61K31/5025 , C07D403/10 , A61K31/416 , A61K31/4439 , C07D417/14 , A61K31/428 , A61K31/4375 , C07D413/14 , A61K31/423 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/506 , A61K31/498 , A61K31/5377 , A61P31/04
CPC分类号： C07D403/10 , A61K31/198 , A61K31/407 , A61K31/41 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/428 , A61K31/431 , A61K31/437 , A61K31/4375 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K31/546 , A61K45/06 , A61P31/04 , C07D401/10 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08
摘要： The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and RB are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
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公开(公告)号：US09957264B2
公开(公告)日：2018-05-01
申请号：US14778046
申请日：2014-03-19
发明人： Matthew Lloyd Childers , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Michelle Martinez , Danielle Falcone , Luis Torres , Yongqi Deng , Ravi Kurukulasuriya , Hongbo Zeng , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： 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：US09725445B2
公开(公告)日：2017-08-08
申请号：US14778019
申请日：2014-03-19
发明人： Matthew Lloyd Childers , Christopher Dinsmore , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Hongjun Zhang , Danielle Falcone , Luis Torres , Jason Brubaker , Hongbo Zeng , Jiaqiang Cai , Xiaoxing Du , Chonggang Wang , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： 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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6.发明申请CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS 有权甘氨酸激酶抑制剂CYCLOALKYL NITRILE PYRAZOLO PYRIDONES公开(公告)号：US20160280704A1
公开(公告)日：2016-09-29
申请号：US14778019
申请日：2014-03-19
申请人： Matthew Lloyd Childers , Christopher Dinsmore , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Hongjun Zhang , Danielle Falcone , Luis Torres , Jason Brubaker , Hongbo Zeng , Jiaqiang Cai , Xiaoxing Du , Chonggang Wang , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng , Merck Sharp & Dohme Corp.
发明人： Matthew Lloyd Childers , Christopher Dinsmore , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Hongjun Zhang , Danielle Falcone , Luis Torres , Jason Brubaker , Hongbo Zeng , Jiaqiang Cai , Xiaoxing Du , Chonggang Wang , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： 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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7.发明申请N-(2-CYANO HETEROCYCLYL) PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS 有权N-（2-氰基杂环基）吡唑并吡喃酮作为甘薯激酶抑制剂公开(公告)号：US20160272633A1
公开(公告)日：2016-09-22
申请号：US14778052
申请日：2014-03-19
申请人： Christopher DINSMORE , Peter FULLER , David GUERIN , Christopher F. THOMPSON , Qinglin PU , Mark E. SCOTT , Jason David KATZ , Ravi KURUKLASURIYA , Joshua T. CLOSE , Danielle FALCONE , Jason BRUDAKER , Hongbo ZENG , Yunfeng BAI , Jianmin FU , Norman KONG , Yumei LIU , Zhixiang ZHENG , MERCK SHARP & DOHME CORP.
发明人： Christopher Dinsmore , Peter Fuller , David Guerin , Christopher F. Thompson , Qinglin Pu , Mark E. Scott , Jason David Katz , Ravi Kuruklasuriya , Joshua T. Close , Danielle Falcone , Jason Brubaker , Hongbo Zeng , Yunfeng Bai , Jianmin Fu , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： 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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8.发明申请GEMINALLY SUBSTITUTED CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS 有权作为JANUS KINASE抑制剂的GEMYALLY取代的氰基乙基吡唑啉吡啶公开(公告)号：US20160272632A1
公开(公告)日：2016-09-22
申请号：US14778046
申请日：2014-03-19
申请人： Matthew Lloyd CHILDERS , Peter FULLER , David GUERIN , Jason David KATZ , Qinglin PU , Mark E. SCOTT , Christopher E. THOMPSON , Michelle MARTINEZ , Danielle FALCONE , Luis TORRES , Yongqi DENG , Ravi KURUKULASURIYA , Hongbo ZENG , Yunfeng BAI , Norman KONG , Yumei LIU , MERCK SHARP & DOHME CORP.
发明人： Matthew Lloyd Childers , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Michelle Martinez , Danielle Falcone , Luis Torres , Yongqi Deng , Ravi Kurukulasuriya , Hongbo Zeng , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： 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.
摘要翻译： 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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公开(公告)号：US10227331B2
公开(公告)日：2019-03-12
申请号：US15737334
申请日：2016-06-24
发明人： Frank Bennett , Jinlong Jiang , Alexander Pasternak , Shuzhi Dong , Xin Gu , Jack D. Scott , Haiqun Tang , Zhiqiang Zhao , Yuhua Huang , David Hunter , Dexi Yang , Katherine Young , Li Xiao , Zhibo Zhang , Jianmin Fu , Yunfeng Bai , Zhixiang Zheng , Xu Zhang
IPC分类号： C07D403/10 , C07D403/12 , C07D413/14 , C07D401/10 , C07D403/14 , C07D407/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , A61P31/04 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D487/04 , A61K31/198 , A61K31/407 , A61K31/41 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/431 , A61K31/439 , A61K31/496 , A61K31/541 , A61K31/546 , C07D405/14 , C07D453/02 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08
摘要： The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and RB are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
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公开(公告)号：US10059705B2
公开(公告)日：2018-08-28
申请号：US14778055
申请日：2014-03-19
发明人： Christopher Dinsmore , Peter Fuller , David Guerin , Jason David Katz , Christopher F. Thompson , Danielle Falcone , Wei Deng , Luis Torres , Hongbo Zeng , Yunfeng Bai , Jianmin Fu , Norman Kong , Yumei Liu , Zhixiang Zheng , Mark E. Scott
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： 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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