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公开(公告)号：US20170240567A1
公开(公告)日：2017-08-24
申请号：US15519740
申请日：2015-10-21
申请人： Mark E. Scott , David Guerin , Danielle Molinari , Sam Kattar , Peter Fuller , Christopher Dinsmore , Normon Kong , Yunfeng Bai , Jianmin FU , Yumei Liu , Zhixiang Zheng
发明人： Mark E. Scott , David Guerin , Danielle Molinari , Sam Kattar , Peter Fuller , Christopher Dinsmore , Normon Kong , Yunfeng Bai , Jianmin FU , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D519/00 , A61K31/4545 , A61K31/55 , A61K31/538 , A61K31/541 , A61K31/554 , A61K31/553 , C07D471/04 , A61K31/5377
CPC分类号： C07D519/00 , 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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12.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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公开(公告)号：US20070078154A1
公开(公告)日：2007-04-05
申请号：US10572167
申请日：2004-09-17
IPC分类号： A61K31/4741 , A61K31/4709 , A61K31/4704 , C07D413/02 , C07D401/02
CPC分类号： C07D215/227 , C07D215/38 , C07D215/54 , C07D401/06 , C07D413/06 , C07D413/14
摘要： The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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公开(公告)号：US20160272634A1
公开(公告)日：2016-09-22
申请号：US14778055
申请日：2014-03-19
申请人： 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 , MERCK SHARP & DOHME CORP.
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.
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：US20080008708A1
公开(公告)日：2008-01-10
申请号：US11890755
申请日：2007-08-07
IPC分类号： A61K31/404 , A61K31/4196 , A61K31/4535 , A61K39/395 , A61P35/00 , C07D209/04 , C07D249/08
CPC分类号： C07D403/12 , C07D209/42 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises an indole-sulfonamide moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
摘要翻译： 本发明涉及能够抑制，调节和/或调节受体型和非受体型酪氨酸激酶的信号转导的化合物。 本发明的化合物具有包含吲哚磺酰胺部分的核心结构。 本发明还涉及这些化合物的药学上可接受的盐，水合物和立体异构体。
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公开(公告)号：US20060276450A1
公开(公告)日：2006-12-07
申请号：US10572342
申请日：2004-09-17
申请人： B. Trotter , Kausik Nanda , Nathan Kett , Christopher Dinsmore , Gerald Ponticello , David Claremon
发明人： B. Trotter , Kausik Nanda , Nathan Kett , Christopher Dinsmore , Gerald Ponticello , David Claremon
IPC分类号： A61K31/4709 , C07D491/04 , C07D405/02 , C07D403/02 , C07D401/02
CPC分类号： C07D217/14 , C07D217/16 , C07D401/04
摘要： The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译： 本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构（I）的化合物等。
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公开(公告)号：US20060270704A1
公开(公告)日：2006-11-30
申请号：US10572343
申请日：2004-09-22
IPC分类号： C07D217/22 , A61K31/4704
CPC分类号： C07D217/26 , C07D217/24 , C07D401/04 , C07D401/06 , C07D417/04
摘要： The present invention relates to compounds having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译： 本发明涉及具有结构式（I）的化合物，其可用作治疗心律失常的钾通道抑制剂等。
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公开(公告)号：US20050261496A1
公开(公告)日：2005-11-24
申请号：US10523285
申请日：2003-08-05
IPC分类号： C07D487/10 , A61K31/138 , A61K31/337 , A61K31/40 , A61K31/404 , A61K31/407 , A61K31/438 , A61K31/44 , A61K31/4465 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/547 , A61K31/55 , A61K31/551 , A61K31/553 , A61K39/395 , A61K45/00 , A61P1/04 , A61P3/10 , A61P27/02 , A61P35/00 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/02 , C07D209/42 , C07D209/96 , C07D211/02 , C07D215/02 , C07D267/02 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/02 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D451/02 , C07D491/04 , C07D491/048 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/12 , C07D498/04 , C07D513/04 , C07D513/08
CPC分类号： C07D487/10 , C07D209/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D491/04 , C07D491/10 , C07D513/04 , C07D513/08
摘要： The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
摘要翻译： 本发明涉及能够抑制，调节和/或调节受体型和非受体型酪氨酸激酶的信号转导的化合物。 本发明的化合物具有包含磺酰基吲哚部分的核心结构。 本发明还涉及这些化合物的药学上可接受的盐，水合物和立体异构体。
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公开(公告)号：US06248756B1
公开(公告)日：2001-06-19
申请号：US09248883
申请日：1999-02-11
申请人： Neville J. Anthony , Christopher Dinsmore , Robert P. Gomez , John H. Hutchinson , John S. Wai , Theresa M. Williams , Ian M. Bell , Mark W. Embrey , Thorsten E. Fisher
发明人： Neville J. Anthony , Christopher Dinsmore , Robert P. Gomez , John H. Hutchinson , John S. Wai , Theresa M. Williams , Ian M. Bell , Mark W. Embrey , Thorsten E. Fisher
IPC分类号： A61K314468
CPC分类号： C07D401/06 , C07D211/62 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferas (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
摘要翻译： 本发明涉及抑制法尼基蛋白转移（Fatease-protein transferas，FTase）和致癌基因蛋白Ras的法呢基化的化合物。 本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶的方法和癌基因蛋白Ras的法呢基化。
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20.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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