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公开(公告)号：US20050130954A1
公开(公告)日：2005-06-16
申请号：US10993173
申请日：2004-11-19
申请人： Ian Mitchell , Keith Spencer , Peter Stengel , Yongxin Han , Nicholas Kallan , Mark Munson , Guy Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Riu Xu , Chang Rao , Bin Wang , April Bernacki
发明人： Ian Mitchell , Keith Spencer , Peter Stengel , Yongxin Han , Nicholas Kallan , Mark Munson , Guy Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Riu Xu , Chang Rao , Bin Wang , April Bernacki
IPC分类号： A61K20060101 , A61K31/496 , A61K31/519 , A61K31/53
CPC分类号： C07D239/94 , B41M3/008 , B44F1/10 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , G09F13/16 , Y10T428/24802 , Y10T428/24851 , Y10T428/25 , Y10T428/31507 , Y10T428/31551 , Y10T428/31786 , Y10T428/31855
摘要： The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供包括拆分的对映异构体，非对映异构体，溶剂合物和药学上可接受的盐的化合物，其包含式：<？在线公式描述=“在线公式”end =“lead”→> AL-CR < in-line-formula description =“In-line Formulas”end =“tail”？>其中CR是循环核心组，L是连接组，A如本文所定义。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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公开(公告)号：US08680114B2
公开(公告)日：2014-03-25
申请号：US12567258
申请日：2009-09-25
申请人： Ian S. Mitchell , Keith L. Spencer , Peter Stengel , Yongxin Han , Nicholas C. Kallan , Mark Munson , Guy P. A. Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Rui Xu , Chang Rao , Bing Wang , April L. Bernacki
发明人： Ian S. Mitchell , Keith L. Spencer , Peter Stengel , Yongxin Han , Nicholas C. Kallan , Mark Munson , Guy P. A. Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Rui Xu , Chang Rao , Bing Wang , April L. Bernacki
IPC分类号： A61K31/47 , A01N43/42 , C07D215/00
CPC分类号： C07D239/94 , B41M3/008 , B44F1/10 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , G09F13/16 , Y10T428/24802 , Y10T428/24851 , Y10T428/25 , Y10T428/31507 , Y10T428/31551 , Y10T428/31786 , Y10T428/31855
摘要： The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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公开(公告)号：US20100168123A1
公开(公告)日：2010-07-01
申请号：US12567258
申请日：2009-09-25
申请人： Ian S. Mitchell , Keith L. Spencer , Peter Stengel , Yongxin Han , Nicholas C. Kallan , Mark Munson , Guy P.A. Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Rui Xu , Chang Rao , Bing Wang , April L. Bernacki
发明人： Ian S. Mitchell , Keith L. Spencer , Peter Stengel , Yongxin Han , Nicholas C. Kallan , Mark Munson , Guy P.A. Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Rui Xu , Chang Rao , Bing Wang , April L. Bernacki
IPC分类号： A61K31/497 , C07D401/04 , C07D471/04 , C07D403/04 , C07D487/04 , A61K31/437 , A61P35/00
CPC分类号： C07D239/94 , B41M3/008 , B44F1/10 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , G09F13/16 , Y10T428/24802 , Y10T428/24851 , Y10T428/25 , Y10T428/31507 , Y10T428/31551 , Y10T428/31786 , Y10T428/31855
摘要： The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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公开(公告)号：US20070142413A1
公开(公告)日：2007-06-21
申请号：US10595807
申请日：2004-11-15
申请人： Michael Block , John Lee , David Scott , Haixia Wang , Tao Wang , Dingwei Yu , Yongxin Han , John Josey , Bin Wang
发明人： Michael Block , John Lee , David Scott , Haixia Wang , Tao Wang , Dingwei Yu , Yongxin Han , John Josey , Bin Wang
IPC分类号： A61K31/506 , C07D403/14 , C07D413/14
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Compounds of formula (I): and their use in the inhibition of Trk activity are described.
摘要翻译： 描述式（I）化合物及其在抑制Trk活性中的用途。
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公开(公告)号：US20100152219A1
公开(公告)日：2010-06-17
申请号：US12712659
申请日：2010-02-25
申请人： Michael Howard Block , John W. Lee , David Scott , Haixia Wang , Tao Wang , Dingwei Yu , Yongxin Han , John Anthony Josey , Bin Wang
发明人： Michael Howard Block , John W. Lee , David Scott , Haixia Wang , Tao Wang , Dingwei Yu , Yongxin Han , John Anthony Josey , Bin Wang
IPC分类号： A61K31/506 , C07D403/12
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Compounds of formula (I): and their use in the inhibition of Trk activity are described.
摘要翻译： 描述式（I）化合物及其在抑制Trk活性中的用途。
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公开(公告)号：US07622482B2
公开(公告)日：2009-11-24
申请号：US11816376
申请日：2006-02-15
申请人： Yongxin Han , Michelle Lamb , Peter Mohr , Bin Wang , Tao Wang , Dingwei Yu
发明人： Yongxin Han , Michelle Lamb , Peter Mohr , Bin Wang , Tao Wang , Dingwei Yu
IPC分类号： A01N43/42 , A61K31/44 , C07D471/00 , C07D487/00 , C07D471/02 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04 , C07D401/12 , C07D403/12 , C07D473/32
摘要： This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
摘要翻译： 本发明涉及具有式（I）的新化合物及其药物组合物及其使用方法。 这些新型化合物为癌症提供治疗。
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公开(公告)号：US20090137624A1
公开(公告)日：2009-05-28
申请号：US11816376
申请日：2006-02-15
申请人： Michelle Lamb , Tao Wang , Dingwel Yu , Yongxin Han , Peter Mohr , Bin Wang
发明人： Michelle Lamb , Tao Wang , Dingwel Yu , Yongxin Han , Peter Mohr , Bin Wang
IPC分类号： A61K31/52 , C07D471/02 , A61K31/4745 , C07D473/02
CPC分类号： C07D471/04 , C07D401/12 , C07D403/12 , C07D473/32
摘要： This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
摘要翻译： 本发明涉及具有式（I）的新化合物及其药物组合物及其使用方法。 这些新型化合物为癌症提供治疗。
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8.发明授权公开(公告)号：US11655216B2
公开(公告)日：2023-05-23
申请号：US16341595
申请日：2017-10-09
申请人： Merck Sharp & Dohme Corp. , Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
IPC分类号： C07D221/20 , C07D401/12 , C07D417/12 , C07D405/12 , C07D211/22 , C07D401/14 , C07D417/14
CPC分类号： C07D221/20 , C07D211/22 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12 , C07D417/14
摘要： In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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公开(公告)号：US10894775B2
公开(公告)日：2021-01-19
申请号：US16341591
申请日：2017-10-09
申请人： Merck Sharp & Dohme Corp. , Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu , Chuanman Huang
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu , Chuanman Huang
IPC分类号： C07D221/20 , C07D211/16 , C07D211/96
摘要： In its many embodiments, the present invention provides certain piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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10.发明申请公开(公告)号：US20200277252A1
公开(公告)日：2020-09-03
申请号：US16753035
申请日：2018-10-04
申请人： Meredeth Ann McGowan , Abdelghani Achab , Xavier Fradera , Yongxin Han , Derun Li , Jongwon Lim , Kun Liu , Nunzio Sciammetta , Catherine M. White , Wensheng Yu , Hongjun Zhang , Hua Zhou , MERCK SHARP & DOHME CORP.
发明人： Meredeth Ann McGowan , Abdelghani Achab , Xavier Fradera , Yongxin Han , Derun Li , Jongwon Lim , Kun Liu , Nunzio Sciammetta , Catherine M. White , Wensheng Yu , Hongjun Zhang , Hua Zhou
IPC分类号： C07C237/42 , C07D241/24 , C07D213/82 , C07D233/90 , C07D263/34 , C07D231/14 , C07D277/56 , C07D239/28 , C07D213/75 , C07D309/14 , C07D237/20 , C07D307/14 , C07D205/04 , C07D285/06 , C07D487/04
摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
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