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公开(公告)号：US20100331335A1
公开(公告)日：2010-12-30
申请号：US12701474
申请日：2010-02-05
申请人： Hing L. Sham , Roy K. Hom , Andrei W. Konradi , Gary D. Probst , Simeon Bowers , Anh Truong , R. Jeffrey Neitz , Jennifer Sealy , Gergely Toth
发明人： Hing L. Sham , Roy K. Hom , Andrei W. Konradi , Gary D. Probst , Simeon Bowers , Anh Truong , R. Jeffrey Neitz , Jennifer Sealy , Gergely Toth
IPC分类号： A61K31/498 , C07D409/04 , C07D409/14 , C07D405/14 , C07D409/12 , C07D471/04 , C07D487/04 , C07D417/14 , A61K31/4196 , A61K31/4709 , A61K31/4725 , A61K31/454 , A61K31/4535 , A61K31/4375 , A61K31/437 , A61K31/422 , A61K31/4245 , A61K31/4155 , A61K31/41 , A61K31/4178 , A61K31/497 , C12Q1/48 , C12N5/071 , A61P25/28 , A61P25/16 , A61P25/00
CPC分类号： C07D409/04 , A61K31/381 , A61K31/401 , A61K31/4196 , A61K31/4245 , A61K31/433 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/4985 , A61K31/519 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
摘要翻译： 本公开提供了具有下式结构的c-Jun N-末端激酶（JNK）抑制剂：其盐或溶剂合物，其中环A，Ca，Cb，Z，R 5，W和Cy在本文中定义 。 本公开进一步提供药物组合物，包括本公开的化合物和制备和使用本公开的化合物和组合物的方法，例如治疗和预防各种疾病，例如阿尔茨海默病。
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公开(公告)号：US09073891B2
公开(公告)日：2015-07-07
申请号：US13617630
申请日：2012-09-14
申请人： Hing L. Sham , Roy K. Hom , Andrei W. Konradi , Gary D. Probst , Simeon Bowers , Anh Truong , R. Jeffrey Neitz , Jennifer Sealy , Gergely Toth
发明人： Hing L. Sham , Roy K. Hom , Andrei W. Konradi , Gary D. Probst , Simeon Bowers , Anh Truong , R. Jeffrey Neitz , Jennifer Sealy , Gergely Toth
IPC分类号： C07D409/04 , A61K31/381 , A61K31/433 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , A61K31/401 , A61K31/4196 , A61K31/4245 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/4985 , A61K31/519
CPC分类号： C07D409/04 , A61K31/381 , A61K31/401 , A61K31/4196 , A61K31/4245 , A61K31/433 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/4985 , A61K31/519 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
摘要翻译： 本公开提供了具有下式结构的c-Jun N-末端激酶（JNK）抑制剂：其盐或溶剂合物，其中环A，Ca，Cb，Z，R 5，W和Cy在本文中定义 。 本公开进一步提供药物组合物，包括本公开的化合物和制备和使用本公开的化合物和组合物的方法，例如治疗和预防各种疾病，例如阿尔茨海默病。
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公开(公告)号：US08450363B2
公开(公告)日：2013-05-28
申请号：US12701474
申请日：2010-02-05
申请人： Hing L. Sham , Roy K. Hom , Andrei W. Konradi , Gary D. Probst , Simeon Bowers , Anh Truong , R. Jeffrey Neitz , Jennifer Sealy , Gergely Toth
发明人： Hing L. Sham , Roy K. Hom , Andrei W. Konradi , Gary D. Probst , Simeon Bowers , Anh Truong , R. Jeffrey Neitz , Jennifer Sealy , Gergely Toth
IPC分类号： A61K31/38 , A01N43/06 , C07D333/36
CPC分类号： C07D409/04 , A61K31/381 , A61K31/401 , A61K31/4196 , A61K31/4245 , A61K31/433 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/4985 , A61K31/519 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
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公开(公告)号：US20130072494A1
公开(公告)日：2013-03-21
申请号：US13617630
申请日：2012-09-14
申请人： Hing L. SHAM , Roy K. Hom , Andrei W. Konradi , Gary D. Probst , Simeon Bowers , Anh Truong , R. Jeffrey Neitz , Jennifer Sealy , Gergely Toth
发明人： Hing L. SHAM , Roy K. Hom , Andrei W. Konradi , Gary D. Probst , Simeon Bowers , Anh Truong , R. Jeffrey Neitz , Jennifer Sealy , Gergely Toth
IPC分类号： A61K31/517 , C07D409/04 , A61K31/4725 , C07D413/04 , A61K31/519 , C07D487/04 , A61K31/4196 , A61K31/4245 , C07D471/04 , A61K31/4985 , A61K31/401 , A61K31/498 , C07D417/14 , C07D417/02 , A61K31/4709
CPC分类号： C07D409/04 , A61K31/381 , A61K31/401 , A61K31/4196 , A61K31/4245 , A61K31/433 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/4985 , A61K31/519 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
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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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公开(公告)号：US20110207716A1
公开(公告)日：2011-08-25
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： A61K31/519 , C07D475/00 , C07D475/12 , A61K31/5377 , A61K31/55 , A61K31/5383 , A61P25/28 , A61P25/16 , A61P35/00 , A61P35/04 , A61P35/02
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：US20110212942A1
公开(公告)日：2011-09-01
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： A61K31/55 , C07D475/00 , C07D471/14 , C07D487/14 , C07D498/14 , A61K31/4985 , A61K31/5383 , A61P35/00 , A61P25/28 , A61P25/16 , A61P35/02 , A61P35/04
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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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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公开(公告)号：US07754712B2
公开(公告)日：2010-07-13
申请号：US11951097
申请日：2007-12-05
申请人： Simeon Bowers , Albert W. Garofalo , Roy K. Hom , Andrei W. Konradi , Matthew N. Mattson , Martin L. Neitzel , Christopher M. Semko , Anh P. Truong , Jing Wu , Ying-zi Xu
发明人： Simeon Bowers , Albert W. Garofalo , Roy K. Hom , Andrei W. Konradi , Matthew N. Mattson , Martin L. Neitzel , Christopher M. Semko , Anh P. Truong , Jing Wu , Ying-zi Xu
IPC分类号： A61K31/5365 , A61K31/437 , A61K31/4985 , A61P25/28 , C07D497/04 , C07D497/14 , C07D471/14
CPC分类号： C07D451/14 , C07D471/08 , C07D471/18 , C07D471/22 , C07D498/08
摘要： The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.
摘要翻译： 本发明提供了N-环磺酰氨基化合物和式I的盐：其中A如说明书中所述，并且R 1和R 2结合形成[3.3.1]或[3.2.1]环体系，其中氮被连接 并且[3.3.1]或[3.2.1]环体系任选地与杂芳基或杂环烷基环稠合。 式I的化合物可用于治疗或预防认知障碍，例如阿尔茨海默病。 本发明还包括含有式I化合物的药物组合物，治疗认知障碍的方法，例如阿尔茨海默氏病，以及可用于制备式I化合物的中间体。
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