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公开(公告)号：US08067434B2
公开(公告)日：2011-11-29
申请号：US12082665
申请日：2008-04-11
申请人： Prabha Ibrahim , Dean Richard Artis , Ryan Bremer , Gaston Habets , Clarence R. Hurt , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Heike Krupka , Abhinav Kumar , Brian West
发明人： Prabha Ibrahim , Dean Richard Artis , Ryan Bremer , Gaston Habets , Clarence R. Hurt , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Heike Krupka , Abhinav Kumar , Brian West
CPC分类号： C07D471/04
摘要： Compounds active on Ret are described, as well as methods of using such compounds. Also described are crystal structures of Ret surrogates that were determined using X-ray crystallography. The use of such Ret surrogate crystals and structural information can, for example, be used for identifying molecular scaffolds and for developing ligands that bind to and modulate Ret and for identifying improved ligands based on known ligands.
摘要翻译： 描述了在Ret上活性的化合物，以及使用这些化合物的方法。 还描述了使用X射线晶体学测定的Ret替代物的晶体结构。 使用这种Ret替代晶体和结构信息可以例如用于鉴定分子支架和开发结合并调节Ret的配体，并用于基于已知配体鉴定改良的配体。
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公开(公告)号：US20120053177A1
公开(公告)日：2012-03-01
申请号：US13243748
申请日：2011-09-23
申请人： Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
发明人： Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
IPC分类号： A61K31/5377 , A61P35/00 , A61K31/496 , A61K31/506 , C12N9/99 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要： Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译： 描述了对蛋白激酶有活性的化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。
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公开(公告)号：US08415469B2
公开(公告)日：2013-04-09
申请号：US12616079
申请日：2009-11-10
申请人： Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , Jianming Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
发明人： Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , Jianming Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
IPC分类号： C07D413/14 , C07D401/14 , C07D471/04 , C07F7/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要： Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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公开(公告)号：US20100256365A1
公开(公告)日：2010-10-07
申请号：US12616079
申请日：2009-11-10
申请人： Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
发明人： Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
IPC分类号： C07D413/14 , C07D401/14 , C07F7/02 , C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要： Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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公开(公告)号：US20140038948A1
公开(公告)日：2014-02-06
申请号：US13926959
申请日：2013-06-25
申请人： Guoxian Wu , Jiazhong Zhang , Yong-Liang Zhu , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , Dean R. Artis , James Tsai
发明人： Guoxian Wu , Jiazhong Zhang , Yong-Liang Zhu , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , Dean R. Artis , James Tsai
IPC分类号： C07D285/16 , A61K31/5377 , A61K31/505 , A61K31/437 , A61K31/47 , C07D213/76 , A61K31/44 , C07D239/49 , C07D471/04 , C07D215/38 , C07D417/12 , A61K31/549 , A61K31/4439
CPC分类号： A61K31/44 , A61K31/415 , A61K31/42 , A61K31/433 , A61K31/437 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/549 , A61K45/06 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D231/40 , C07D239/48 , C07D239/49 , C07D261/14 , C07D263/48 , C07D285/135 , C07D285/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , A61K31/4427 , A61K2300/00
摘要： Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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公开(公告)号：US20100190777A1
公开(公告)日：2010-07-29
申请号：US12669450
申请日：2008-07-16
申请人： Guoxian Wu , Jiazhong Zhang , Yong-Liang Zhu , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , Dean R. Artis , James Tsai
发明人： Guoxian Wu , Jiazhong Zhang , Yong-Liang Zhu , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , Dean R. Artis , James Tsai
IPC分类号： C07D213/75 , A61K31/54 , A61K31/5377 , A61K31/505 , A61K31/47 , A61K31/437 , A61K31/44 , A61K31/41 , A61K31/42 , A61K31/415 , A61K31/165 , C07D471/02 , C07D413/02 , C07D403/00 , A61K31/444 , C07D215/38 , A61P35/00 , C07D417/02 , C07D213/02 , C07D285/12 , C07D261/14 , C07D231/02 , C07C233/64
CPC分类号： A61K31/44 , A61K31/415 , A61K31/42 , A61K31/433 , A61K31/437 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/549 , A61K45/06 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D231/40 , C07D239/48 , C07D239/49 , C07D261/14 , C07D263/48 , C07D285/135 , C07D285/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , A61K31/4427 , A61K2300/00
摘要： Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.
摘要翻译： 描述了对蛋白激酶有活性的式I化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。 式（I）其中Ar是任选取代的杂芳基; R2是氢，低级烷基或卤素; U选自-S（O）2 - ， - C（X） - ， - C（X）-N（R 10） - 和-S（O）2 -N（R 10） - ; R 3是任选取代的低级烷基，任选取代的C 3-6环烷基，任选取代的杂环烷基，任选取代的芳基或任选取代的杂芳基; 并且其中R 1，R 3，R 4，m，L 1，X R 10如本文所述。
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公开(公告)号：US20120115848A1
公开(公告)日：2012-05-10
申请号：US13267834
申请日：2011-10-06
申请人： Robert A. Galemmo, JR. , Dean Richard Artis, I , Xiaocong Michael Ye , Danielle L. Aubele , Anh P. Truong , Simeon Bowers , Roy K. Hom , Yong-Liang Zhu , R. Jeffrey Neitz , Jennifer Sealy , Marc Adler , Paul Beroza , John P. Anderson
发明人： Robert A. Galemmo, JR. , Dean Richard Artis, I , Xiaocong Michael Ye , Danielle L. Aubele , Anh P. Truong , Simeon Bowers , Roy K. Hom , Yong-Liang Zhu , R. Jeffrey Neitz , Jennifer Sealy , Marc Adler , Paul Beroza , John P. Anderson
IPC分类号： A61K31/55 , C07D471/22 , C07D487/22 , C07D498/22 , A61K31/519 , A61P35/02 , A61K31/5377 , A61P25/00 , A61P25/16 , A61P25/28 , A61P35/00 , A61P35/04 , C07D487/14 , A61K31/5383
CPC分类号： C07D487/14 , C07D487/22 , C07D498/22
摘要： The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, U1, U2, U3, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
摘要翻译： 本发明提供具有式（I）结构的化合物或其盐或溶剂化物，其中环A，U1，U2，U3，R2，R3和R4如本文所定义。 本发明进一步提供包含本发明化合物的药物组合物以及制备和使用本发明化合物和组合物的方法，例如治疗和预防各种疾病如帕金森病。
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8.发明授权Benzenesulfonamide derivatives of quinoxaline, pharmaceutical compositions thereof, and their use in methods for treating cancer 有权喹喔啉的苯磺酰胺衍生物及其药物组合物及其在治疗癌症的方法中的用途公开(公告)号：US09295671B2
公开(公告)日：2016-03-29
申请号：US13594634
申请日：2012-08-24
申请人： Yong-Liang Zhu , Xiangping Qian
发明人： Yong-Liang Zhu , Xiangping Qian
IPC分类号： A61K31/498 , A61K31/5377 , C07D401/04 , C07D403/04 , C07D413/04 , C07D241/42 , C07D241/44 , A61K31/18 , A61P35/00 , A61P35/02 , G01N33/574 , C12Q1/68
CPC分类号： A61K31/498 , A61K31/18 , A61K31/5377 , A61K45/06 , C07D241/42 , C07D241/44 , C07D401/04 , C07D403/04 , C07D413/04 , C12Q1/6886 , C12Q2600/106 , C12Q2600/118 , C12Q2600/156 , G01N33/5748 , G01N2333/47
摘要： Chemical entities that are benzenesulfonamide derivatives of quinoxaline, pharmaceutical compositions and methods of treatment of cancer are described.
摘要翻译： 描述了喹喔啉的苯磺酰胺衍生物，药物组合物和癌症治疗方法的化学实体。
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公开(公告)号：US08541418B2
公开(公告)日：2013-09-24
申请号：US12974622
申请日：2010-12-21
申请人： Robert A. Galemmo , Dean R. Artis , Xiaocong Michael Ye , Danielle Aubele , Anh Truong , Simeon Bowers , Roy K. Hom , Yong-Liang Zhu , R. Jeffrey Neitz , Jennifer Sealy , Marc Adler , Paul Beroza , John P. Anderson
发明人： Robert A. Galemmo , Dean R. Artis , Xiaocong Michael Ye , Danielle Aubele , Anh Truong , Simeon Bowers , Roy K. Hom , Yong-Liang Zhu , R. Jeffrey Neitz , Jennifer Sealy , Marc Adler , Paul Beroza , John P. Anderson
IPC分类号： A61K31/4965 , C07D475/00
CPC分类号： C07D475/00 , A61K31/519 , A61K31/5377 , A61K31/5383 , C07D475/04 , C07D475/12 , C07D487/14 , C07D498/14 , C07D519/00
摘要： The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
摘要翻译： 本发明提供具有式（I）结构的化合物或其盐或溶剂化物，其中环A，E1，E2，R 1，R 2，R 3和R 4在本文中定义。 本发明进一步提供包含本发明化合物的药物组合物以及制备和使用本发明化合物和组合物的方法，例如治疗和预防各种疾病如帕金森病。
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公开(公告)号：US08445503B2
公开(公告)日：2013-05-21
申请号：US12974401
申请日：2010-12-21
申请人： Robert A. Galemmo , Dean R. Artis , Xiaocong Michael Ye , Danielle Aubele , Anh Truong , Simeon Bowers , Roy K. Hom , Yong-Liang Zhu , R. Jeffrey Neitz , Jennifer Sealy , Marc Adler , Paul Beroza , John P. Anderson
发明人： Robert A. Galemmo , Dean R. Artis , Xiaocong Michael Ye , Danielle Aubele , Anh Truong , Simeon Bowers , Roy K. Hom , Yong-Liang Zhu , R. Jeffrey Neitz , Jennifer Sealy , Marc Adler , Paul Beroza , John P. Anderson
IPC分类号： A01N43/54 , A61K31/505 , C07D491/00
CPC分类号： C07D475/00 , A61K31/519 , A61K31/5377 , A61K31/5383 , C07D475/04 , C07D475/12 , C07D487/14 , C07D498/14 , C07D519/00
摘要： The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
摘要翻译： 本发明提供具有式（I）结构的化合物或其盐或溶剂化物，其中环A，X，R 1，R 2，R 3，R 4，R 5和R 6在本文中定义。 本发明进一步提供包含本发明化合物的药物组合物以及制备和使用本发明化合物和组合物的方法，例如治疗和预防各种疾病如帕金森病。
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