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公开(公告)号：US08044213B2
公开(公告)日：2011-10-25
申请号：US12634771
申请日：2009-12-10
申请人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, Jr. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, Jr. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
IPC分类号： A61K31/427 , C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.
摘要翻译： 本发明涉及式（1）的化合物及其药学上可接受的盐，其制备方法及其使用方法。
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公开(公告)号：US20100160308A1
公开(公告)日：2010-06-24
申请号：US12634771
申请日：2009-12-10
申请人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, JR. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, JR. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
IPC分类号： A61K31/5377 , A61K31/496 , C07D413/14 , C07D417/14 , A61P35/00
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.
摘要翻译： 本发明涉及式（1）的化合物及其药学上可接受的盐，其制备方法及其用途。
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公开(公告)号：US20090318408A1
公开(公告)日：2009-12-24
申请号：US12485108
申请日：2009-06-16
申请人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
IPC分类号： A61K31/551 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
摘要翻译： 本发明提供式I的PLK1抑制剂化合物：可用于治疗或控制细胞增殖性疾病，特别是肿瘤疾病。 含有这些化合物的这些化合物和制剂可用于治疗或控制实体瘤，例如乳腺癌，结肠癌，肺癌和前列腺肿瘤以及其它肿瘤疾病如非霍奇金淋巴瘤。 还提供了可用于合成式I化合物的中间体化合物。
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公开(公告)号：US08003785B2
公开(公告)日：2011-08-23
申请号：US12485108
申请日：2009-06-16
申请人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
摘要翻译： 本发明提供式I的PLK1抑制剂化合物：可用于治疗或控制细胞增殖性疾病，特别是肿瘤疾病。 含有这些化合物的这些化合物和制剂可用于治疗或控制实体瘤，例如乳腺癌，结肠癌，肺癌和前列腺肿瘤以及其它肿瘤疾病如非霍奇金淋巴瘤。 还提供了可用于合成式I化合物的中间体化合物。
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公开(公告)号：US07612212B2
公开(公告)日：2009-11-03
申请号：US11657800
申请日：2007-01-25
申请人： Shaoqing Chen , Nicholas J. S. Huby , Norman Kong , Steven Gregory Mischke , John Anthony Moliterni , Hong Wang , Zhuming Zhang
发明人： Shaoqing Chen , Nicholas J. S. Huby , Norman Kong , Steven Gregory Mischke , John Anthony Moliterni , Hong Wang , Zhuming Zhang
IPC分类号： C07D233/02 , A61K31/4166
CPC分类号： C07D233/76 , C07D233/78 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/06 , C07D417/06
摘要： The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
摘要翻译： 本发明涉及其制备方法的化合物及其使用方法。 该化合物可用于治疗以MEK多动症为特征的疾病。 因此，该化合物可用于治疗诸如癌症，认知和CNS疾病以及炎性/自身免疫性疾病的疾病。
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公开(公告)号：US20070197617A1
公开(公告)日：2007-08-23
申请号：US11657800
申请日：2007-01-25
申请人： Shaoqing Chen , Nicholas J. S. Huby , Norman Kong , Steven Gregory Mischke , John Anthony Moliterni , Hong Wang , Zhuming Zhang
发明人： Shaoqing Chen , Nicholas J. S. Huby , Norman Kong , Steven Gregory Mischke , John Anthony Moliterni , Hong Wang , Zhuming Zhang
IPC分类号： A61K31/4178 , A61K31/4166 , C07D403/02
CPC分类号： C07D233/76 , C07D233/78 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/06 , C07D417/06
摘要： The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
摘要翻译： 本发明涉及其制备方法的化合物及其使用方法。 该化合物可用于治疗以MEK多动症为特征的疾病。 因此，该化合物可用于治疗诸如癌症，认知和CNS疾病以及炎性/自身免疫性疾病的疾病。
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7.发明授权公开(公告)号：US07037924B2
公开(公告)日：2006-05-02
申请号：US10961906
申请日：2004-10-08
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D217/26 , C07D401/04
摘要： Compounds of formula (I) are provided, wherein R1 and R2 are as designated in the specification. The compounds have utility for the treatment of type 2 diabetes mellitus.
摘要翻译： 提供式（I）化合物，其中R 1和R 2如本说明书中所指出。 该化合物可用于治疗2型糖尿病。
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公开(公告)号：US07132425B2
公开(公告)日：2006-11-07
申请号：US10732838
申请日：2003-12-10
申请人： Shaoqing Chen , Wendy Lea Corbett , Kevin Richard Guertin , Nancy-Ellen Haynes , Robert Francis Kester , Francis A. Mennona , Steven Gregory Mischke , Yimin Qian , Ramakanth Sarabu , Nathan Robert Scott , Kshitij Chhabilbhai Thakkar
发明人： Shaoqing Chen , Wendy Lea Corbett , Kevin Richard Guertin , Nancy-Ellen Haynes , Robert Francis Kester , Francis A. Mennona , Steven Gregory Mischke , Yimin Qian , Ramakanth Sarabu , Nathan Robert Scott , Kshitij Chhabilbhai Thakkar
IPC分类号： A61K31/4965 , A61K31/44 , A01N43/40 , C07D401/00 , C07D241/02
CPC分类号： C07D213/75 , C07D213/76 , C07D213/78 , C07D241/20 , C07D241/26 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/04 , C07D413/04 , C07D417/06
摘要： The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are also provided.
摘要翻译： 本发明提供了在说明书中提供了取代基名称的根据式I的化合物。 还提供了包含式I化合物的药物组合物。
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公开(公告)号：US08658646B2
公开(公告)日：2014-02-25
申请号：US13600863
申请日：2012-08-31
申请人： Shaoqing Chen , Javier de Vicente Fidalgo , Matthew Michael Hamilton , Johannes Cornelius Hermann , Joshua Kennedy-Smith , Hongju Li , Allen John Lovey , Matthew C. Lucas , Kin-Chun Thomas Luk , Stephen M. Lynch , Counde O'yang , Fernando Padilla , Ryan Craig Schoenfeld , Achyutharao Sidduri , Michael Soth , Ce Wang , Peter Michael Wovkulich , Xiaohu Zhang
发明人： Shaoqing Chen , Javier de Vicente Fidalgo , Matthew Michael Hamilton , Johannes Cornelius Hermann , Joshua Kennedy-Smith , Hongju Li , Allen John Lovey , Matthew C. Lucas , Kin-Chun Thomas Luk , Stephen M. Lynch , Counde O'yang , Fernando Padilla , Ryan Craig Schoenfeld , Achyutharao Sidduri , Michael Soth , Ce Wang , Peter Michael Wovkulich , Xiaohu Zhang
IPC分类号： A61K31/495
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中所述变量如本文所述定义，其抑制JAK和SYK并且可用于治疗自身免疫和炎性疾病。
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公开(公告)号：US20130059834A1
公开(公告)日：2013-03-07
申请号：US13600863
申请日：2012-08-31
申请人： Shaoqing Chen , Javier de Vicente Fidalgo , Matthew Michael Hamilton , Johannes Cornelius Hermann , Joshua Kennedy-Smith , Hongju Li , Allen John Lovey , Matthew C. Lucas , Kin-Chun Thomas Luk , Stephen M. Lynch , Counde O'yang , Fernando Padilla , Ryan Craig Schoenfeld , Achyutharao Sidduri , Michael Soth , Ce Wang , Peter Michael Wovkulich , Xiaohu Zhang
发明人： Shaoqing Chen , Javier de Vicente Fidalgo , Matthew Michael Hamilton , Johannes Cornelius Hermann , Joshua Kennedy-Smith , Hongju Li , Allen John Lovey , Matthew C. Lucas , Kin-Chun Thomas Luk , Stephen M. Lynch , Counde O'yang , Fernando Padilla , Ryan Craig Schoenfeld , Achyutharao Sidduri , Michael Soth , Ce Wang , Peter Michael Wovkulich , Xiaohu Zhang
IPC分类号： A61K31/4985 , C07D491/107 , A61K31/5377 , C07D471/04 , C07D495/04 , A61P29/00 , A61P31/00 , A61P37/02 , A61P37/06 , A61P9/00 , A61P3/10 , A61P19/02 , A61P11/06 , A61P25/00 , A61P25/28 , A61P17/06 , A61P17/00 , A61P35/00 , A61P35/02 , A61P1/04 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中所述变量如本文所述定义，其抑制JAK和SYK并且可用于治疗自身免疫和炎性疾病。
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