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公开(公告)号：US20110269713A1
公开(公告)日：2011-11-03
申请号：US12937793
申请日：2010-10-14
申请人： Gary E. Keck , Matthew B. Kraft , Anh P. Truong , Carina C. Sanchez , Wei Li , Jonathan A. Covel , Dennie Welch , Yam Poudel
发明人： Gary E. Keck , Matthew B. Kraft , Anh P. Truong , Carina C. Sanchez , Wei Li , Jonathan A. Covel , Dennie Welch , Yam Poudel
IPC分类号： A61K31/695 , C07D309/22 , A61P37/00 , A61K31/351 , A61P35/00 , A61P25/28 , C07F7/08 , C07D323/00
CPC分类号： C07D259/00 , A61K31/351 , A61K31/695 , C07D309/22 , C07D323/00 , C07D471/04 , C07D493/18 , C07D493/22 , C07F7/08 , C07F7/1876 , C07F7/1892
摘要： Described herein are tricyclic macrolactones. The macrolactones have a high binding affinity for PKC. The compounds described herein can be used in a number of therapeutic applications including cancer and Alzheimer's prevention and treatment. The compounds described herein can also treat memory loss. Also described herein are methods for producing macrolactones. The methods permit the high-yield synthesis of macrolactones in fewer steps and with a higher degree of substitution and specificity.
摘要翻译： 本文描述的是三环大环内酯。 该大环内酯对PKC具有高的结合亲和力。 本文所述的化合物可用于许多治疗应用，包括癌症和阿尔茨海默病的预防和治疗。 本文所述的化合物还可以治疗记忆丧失。 本文还描述了生产羟基己内酯的方法。 该方法允许以较少的步骤和更高的取代度和特异性高产率地合成大分子内酯。
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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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公开(公告)号：US20150284337A1
公开(公告)日：2015-10-08
申请号：US14122199
申请日：2012-05-21
申请人： Danielle L. Aubele , Albert W. Garofalo , Simeon Bowers , Anh P. Truong , Xiaocong Michael Ye , Maurizio Franzini , Marc Adler , R. Jeffrey Nietz , Gary Probst
发明人： Danielle L. Aubele , Albert W. Garofalo , Simeon Bowers , Anh P. Truong , Xiaocong Michael Ye , Maurizio Franzini , Marc Adler , R. Jeffrey Nietz , Gary Probst
IPC分类号： C07D237/28 , C07D405/12 , C07D401/14 , C07D403/04 , C07D413/10 , C07D417/04 , C07D401/12 , C07D401/04
CPC分类号： C07D237/28 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D413/10 , C07D417/04
摘要： The present invention provides compounds having a structure according to Formula I: (I) or a salt or solvate thereof, wherein 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：（I）或其盐或溶剂合物，其中R1，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：US20100081680A1
公开(公告)日：2010-04-01
申请号：US12554134
申请日：2009-09-04
申请人： Andrei W. Konradi , Xiaocong Michael Ye , Simeon Bowers , Albert W. Garofalo , Danielle L. Aubele , Darren Dressen , Raymond Ng , Gary Probst , Christopher M. Semko , Minghua Sun , Anh P. Truong , Michael S. Dappen
发明人： Andrei W. Konradi , Xiaocong Michael Ye , Simeon Bowers , Albert W. Garofalo , Danielle L. Aubele , Darren Dressen , Raymond Ng , Gary Probst , Christopher M. Semko , Minghua Sun , Anh P. Truong , Michael S. Dappen
IPC分类号： A61K31/439 , C07D221/04 , C07D471/08 , A61K31/438 , A61P25/28
CPC分类号： C07D451/14 , C07D451/00
摘要： The current invention provides compounds having a structure according to Formulae 1, 2, 3, and 4: wherein the A-ring, B-ring, C-ring, m, n, R25, R50, and R51 are as described in the specification. The invention also provides pharmaceutical compositions comprising compounds of Formulae 1, 2, 3, and 4, as well as methods of treating cognitive disorders, such as Alzheimer's disease. The invention further provides intermediates useful in preparing the compounds of Formulae 1, 2, 3, and 4.
摘要翻译： 本发明提供具有式1,2,3和4结构的化合物：其中A环，B-环，C环，m，n，R25，R50和R51如说明书中所述 。 本发明还提供包含式1,2,3和4的化合物的药物组合物，以及治疗认知障碍如阿尔茨海默氏病的方法。 本发明还提供了可用于制备式1,2,3和4的化合物的中间体。
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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：US07345056B2
公开(公告)日：2008-03-18
申请号：US11465726
申请日：2006-08-18
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： A01N43/42 , A61K31/44 , C07D487/00 , C07D491/00 , C07D451/02
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N-环磺酰氨基化合物和式I的盐：其中A如说明书中所述，R 1和R 2 2结合形成[3.3.1 ]或[3.2.1]环体系，其中氮连接到两个桥头堡碳上，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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公开(公告)号：US09884828B2
公开(公告)日：2018-02-06
申请号：US14122199
申请日：2012-05-21
申请人： Danielle L. Aubele , Albert W. Garofalo , Simeon Bowers , Anh P. Truong , Xiaocong Michael Ye , Maurizio Franzini , Marc Adler , R. Jeffrey Neitz , Gary Probst
发明人： Danielle L. Aubele , Albert W. Garofalo , Simeon Bowers , Anh P. Truong , Xiaocong Michael Ye , Maurizio Franzini , Marc Adler , R. Jeffrey Neitz , Gary Probst
IPC分类号： A61K31/502 , C07D237/28 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D417/04 , C07D413/10
CPC分类号： C07D237/28 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D413/10 , C07D417/04
摘要： The present invention provides compounds having a structure according to Formula I: (I) or a salt or solvate thereof, wherein 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.
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公开(公告)号：US08283358B2
公开(公告)日：2012-10-09
申请号：US12554134
申请日：2009-09-04
申请人： Andrei W. Konradi , Xiaocong Michael Ye , Simeon Bowers , Albert W. Garofalo , Danielle L. Aubele , Darren Dressen , Raymond Ng , Gary Probst , Christopher M. Semko , Minghua Sun , Anh P. Truong , Michael S. Dappen
发明人： Andrei W. Konradi , Xiaocong Michael Ye , Simeon Bowers , Albert W. Garofalo , Danielle L. Aubele , Darren Dressen , Raymond Ng , Gary Probst , Christopher M. Semko , Minghua Sun , Anh P. Truong , Michael S. Dappen
IPC分类号： A61K31/439 , C07D471/18
CPC分类号： C07D451/14 , C07D451/00
摘要： The current invention provides compounds having a structure according to Formulae 1, 2, 3, and 4: wherein the A-ring, B-ring, C-ring, m, n, R25, R50, and R51 are as described in the specification. The invention also provides pharmaceutical compositions comprising compounds of Formulae 1, 2, 3, and 4, as well as methods of treating cognitive disorders, such as Alzheimer's disease. The invention further provides intermediates useful in preparing the compounds of Formulae 1, 2, 3, and 4.
摘要翻译： 本发明提供具有式1,2,3和4结构的化合物：其中A环，B-环，C环，m，n，R25，R50和R51如说明书中所述 。 本发明还提供包含式1,2,3和4的化合物的药物组合物，以及治疗认知障碍如阿尔茨海默氏病的方法。 本发明还提供了可用于制备式1,2,3和4的化合物的中间体。
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公开(公告)号：US20110003802A1
公开(公告)日：2011-01-06
申请号：US12830914
申请日：2010-07-06
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： A61K31/5383 , C07D498/06 , C07D498/16 , C07D453/02 , C07D471/16 , C07D487/06 , C07D487/16 , A61K31/439 , A61K31/4995 , A61P25/28
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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