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公开(公告)号：US08637509B2
公开(公告)日：2014-01-28
申请号：US13696601
申请日：2011-05-05
申请人： Joelle Lorraine Burgess , Neil Johnson , Steven D. Knight , Louis LaFrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma , Dominic Suarez
发明人： Joelle Lorraine Burgess , Neil Johnson , Steven D. Knight , Louis LaFrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma , Dominic Suarez
IPC分类号： A61K31/444 , A61P35/00 , A61K31/506 , A61K31/5377 , A61K31/513 , C07D471/04 , A61K31/4545
CPC分类号： C07D471/04 , C07D519/00
摘要： Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
摘要翻译： 本文公开了式（I）的氮杂吲唑，其中各种基团在本文中定义，并且其可用于治疗癌症。
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公开(公告)号：US20130059849A1
公开(公告)日：2013-03-07
申请号：US13696601
申请日：2011-05-05
申请人： Joelle Lorraine Burgess , Neil Johnson , Steven D. Knight , Louis Lafrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma , Dominic Suarez
发明人： Joelle Lorraine Burgess , Neil Johnson , Steven D. Knight , Louis Lafrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma , Dominic Suarez
IPC分类号： A61K31/444 , A61P35/00 , A61K31/506 , A61K31/5377 , A61K31/496 , A61K31/513 , C07D471/04 , A61K31/4545
CPC分类号： C07D471/04 , C07D519/00
摘要： Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
摘要翻译： 本文公开了式（I）的氮杂吲唑，其中各种基团在本文中定义，并且其可用于治疗癌症。
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公开(公告)号：US20130053397A1
公开(公告)日：2013-02-28
申请号：US13696362
申请日：2011-05-05
申请人： James Brackley, III , Joelle Lorraine Burgess , Seth Grant , Neil Johnson , Steven D. Knight , Louis Lafrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma
发明人： James Brackley, III , Joelle Lorraine Burgess , Seth Grant , Neil Johnson , Steven D. Knight , Louis Lafrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma
IPC分类号： C07D401/14 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/00 , A61P31/10 , A61P19/02 , A61K31/496 , A61P1/00
CPC分类号： A61K31/496 , A61K31/405 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/541 , A61K31/551 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D498/04
摘要： Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful in treating cancer.
摘要翻译： 本文公开了式（I）的吲哚，其中各种基团在本文中定义，并且其可用于治疗癌症。
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公开(公告)号：US08846935B2
公开(公告)日：2014-09-30
申请号：US13696436
申请日：2011-05-05
申请人： Celine Duquenne , Neil Johnson , Steven D. Knight , Louis Lafrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma
发明人： Celine Duquenne , Neil Johnson , Steven D. Knight , Louis Lafrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma
IPC分类号： C07D401/00 , C07D405/00 , C07D231/56
CPC分类号： C07D409/14 , C07D401/12 , C07D401/14 , C07D471/04
摘要： Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
摘要翻译： 本文公开了式（I）的吲唑，其中各种基团在本文中定义，并且其可用于治疗癌症。
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公开(公告)号：US20130053383A1
公开(公告)日：2013-02-28
申请号：US13696436
申请日：2011-05-05
申请人： Celine Duquenne , Neil Johnson , Steven D. Knight , Louis Lafrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma
发明人： Celine Duquenne , Neil Johnson , Steven D. Knight , Louis Lafrance , William H. Miller , Kenneth Newlander , Stuart Romeril , Meagan B. Rouse , Xinrong Tian , Sharad Kumar Verma
IPC分类号： A61K31/4439 , A61P35/00 , A61P35/02 , C07D401/14 , A61K31/4545 , A61K31/496 , A61K31/506 , C07D413/14 , A61K31/5377 , C07D409/14 , C07D401/12 , A61K31/444
CPC分类号： C07D409/14 , C07D401/12 , C07D401/14 , C07D471/04
摘要： Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
摘要翻译： 本文公开了式（I）的吲唑，其中各种基团在本文中定义，并且其可用于治疗癌症。
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公开(公告)号：US09073924B2
公开(公告)日：2015-07-07
申请号：US14344110
申请日：2012-09-12
申请人： Joelle Lorraine Burgess , Neil W. Johnson , Steven David Knight , Louis Vincent LaFrance, III , William Henry Miller , Kenneth Allen Newlander , Stuart Paul Romeril , Meagan B. Rouse , Dominic Suarez , Xinrong Tian , Sharad Kumar Verma
发明人： Joelle Lorraine Burgess , Neil W. Johnson , Steven David Knight , Louis Vincent LaFrance, III , William Henry Miller , Kenneth Allen Newlander , Stuart Paul Romeril , Meagan B. Rouse , Dominic Suarez , Xinrong Tian , Sharad Kumar Verma
IPC分类号： C07D471/02 , C07D471/04
CPC分类号： C07D471/04
摘要： Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
摘要翻译： 本文公开了式（I）的氮杂吲唑，其中各种基团在本文中定义，并且其可用于治疗癌症。
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公开(公告)号：US08536179B2
公开(公告)日：2013-09-17
申请号：US13696362
申请日：2011-05-05
IPC分类号： A61K31/497
CPC分类号： A61K31/496 , A61K31/405 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/541 , A61K31/551 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D498/04
摘要： Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful in treating cancer.
摘要翻译： 本文公开了式（I）的吲哚，其中各种基团在本文中定义，并且其可用于治疗癌症。
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公开(公告)号：US08415345B2
公开(公告)日：2013-04-09
申请号：US12991004
申请日：2009-05-04
申请人： George Adjabeng , Jerry Leroy Adams , Scott Howard Dickerson , Keith Hornberger , Neil W. Johnson , Kevin Kuntz , Kimberly Petrov , Jeffrey M. Ralph , Tara Renae Rheault , Gregory Schaaf , John Stellwagen , Xinrong Tian , David E. Uehling , Alex G. Waterson , Brian Wilson
发明人： George Adjabeng , Jerry Leroy Adams , Scott Howard Dickerson , Keith Hornberger , Neil W. Johnson , Kevin Kuntz , Kimberly Petrov , Jeffrey M. Ralph , Tara Renae Rheault , Gregory Schaaf , John Stellwagen , Xinrong Tian , David E. Uehling , Alex G. Waterson , Brian Wilson
IPC分类号： C07D403/14 , A61K31/505
CPC分类号： C07D417/14 , A61K31/427 , C07D413/04 , C07D413/14 , C07D417/04
摘要： The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
摘要翻译： 本发明提供噻唑磺酰胺和恶唑磺酰胺化合物，含有它们的组合物，以及其制备方法和用作药剂的方法。
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公开(公告)号：US08383635B2
公开(公告)日：2013-02-26
申请号：US13058251
申请日：2009-08-12
申请人： Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
发明人： Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00
CPC分类号： C07D471/04
摘要： The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译： 本发明涉及吡啶并[4,3-d]嘧啶-5（6H） - 酮衍生物。 具体地，本发明涉及式I化合物：其中R1，R2，R3和R4定义如下。 本发明的化合物是PDK1的抑制剂，可用于治疗特征在于组成型激活的ACG激酶（例如癌症，更特别是乳腺癌，结肠癌和肺癌）的病症。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制PDK1活性的方法和使用本发明化合物或与本发明化合物组合的药物组合物治疗与之相关的病症的方法。
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公开(公告)号：US06911447B2
公开(公告)日：2005-06-28
申请号：US10121874
申请日：2002-04-12
IPC分类号： C07D241/04 , A61K31/40 , A61K31/4453 , A61K31/495 , A61K31/496 , A61P3/06 , A61P3/10 , A61P5/00 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P15/00 , A61P15/08 , A61P15/10 , A61P21/04 , A61P29/00 , A61P31/04 , A61P35/00 , C07D207/12 , C07D211/46 , C07D241/06 , C07D241/08 , C07D401/12 , C07D403/06 , A01N25/00 , A61K9/14 , A61K47/00 , A61K47/30 , A61K47/34
CPC分类号： C07D241/08 , C07D207/12 , C07D211/46 , C07D241/06 , C07D401/12 , C07D403/06 , C07K5/06078 , C07K5/06191 , C07K5/0812 , C07K5/0821 , C07K5/0827
摘要： Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula: wherein A is a conformationally restricted ring system selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprises from 5 to 8 atoms; and W is a unit which preferable comprises D-1-fluorophenyalanine, Y comprises a heteroatom, and Z comprises an aromatic carbocyclic ring. Also disclosed are pharmaceutical compositions comprising the ligands of the invention as well as methods of treating diseases mediated through MC-3/MC-4 receptors.
摘要翻译： 公开了MC-3 / MC-4受体配体，所述配体具有下式：其中A是选自以下的构象限制性环系：a）非芳族碳环; b）芳族碳环; c）非芳族杂环; d）芳族杂环; 其中所述环包含5至8个原子; W是优选包含D-1-氟苯丙氨酸的单元，Y包含杂原子，Z包括芳族碳环。 还公开了包含本发明配体的药物组合物以及治疗通过MC-3 / MC-4受体介导的疾病的方法。
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