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公开(公告)号：US06972290B2
公开(公告)日：2005-12-06
申请号：US10347529
申请日：2003-01-17
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31/4965 , A61K31/497 , A61P29/00 , A61P43/00 , C07D241/04 , C07D261/14 , C07D295/185 , C07D307/52 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , A61K31/495
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
摘要翻译： 本发明涉及可用作抗炎剂的酰基哌嗪衍生物。 本发明还涉及含有本发明化合物的药物组合物，以及使用该化合物治疗人类炎性疾病的方法。
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公开(公告)号：US06541476B1
公开(公告)日：2003-04-01
申请号：US09713606
申请日：2000-11-14
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31496
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives, for example, of the following formula (Ia): wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives are useful anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.
摘要翻译： 本发明涉及例如下式（Ia）的酰基哌嗪衍生物：其中R1a，R2，R3，R4，R5和R6如本文所述。 这些衍生物是有用的抗炎剂。 本发明还涉及含有衍生物的药物组合物，以及使用该衍生物治疗人类炎性疾病的方法。
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公开(公告)号：US06573266B1
公开(公告)日：2003-06-03
申请号：US09714937
申请日：2000-11-16
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31496
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives of the following formula (Id): wherein R1b, R3, R4, R5, R6 and R10 are described herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.
摘要翻译： 本发明涉及下式（Id）的酰基哌嗪衍生物：其中R1b，R3，R4，R5，R6和R10如本文所述。 这些衍生物可用作抗炎剂。 本发明还涉及含有衍生物的药物组合物，以及使用该衍生物治疗人类炎性疾病的方法。
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公开(公告)号：US07268140B2
公开(公告)日：2007-09-11
申请号：US11248618
申请日：2005-10-13
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31/4965 , C07D241/04
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
摘要翻译： 本发明涉及可用作抗炎剂的酰基哌嗪衍生物。 本发明还涉及含有本发明化合物的药物组合物，以及使用该化合物治疗人类炎性疾病的方法。
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公开(公告)号：US06977258B2
公开(公告)日：2005-12-20
申请号：US10347530
申请日：2003-01-17
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31/4965 , A61K31/497 , A61P29/00 , A61P43/00 , C07D241/04 , C07D261/14 , C07D295/185 , C07D307/52 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , A61K31/495
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives of formula (Ia): wherein R1a, R2, R3, R4, R5 and R6 are defined herein, which are useful as anti-inflammatory agents. This invention is also directed to other acyl piperazine derivatives, pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
摘要翻译： 本发明涉及式（Ia）的酰基哌嗪衍生物：其中R 1a，R 2，R 3，R 4， 本文定义的R 5和R 6是有用的抗炎剂。 本发明还涉及其它酰基哌嗪衍生物，含有本发明化合物的药物组合物，以及使用该化合物治疗人类炎性疾病的方法。
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公开(公告)号：US06555537B2
公开(公告)日：2003-04-29
申请号：US09726808
申请日：2000-11-29
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31495
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives, for example, of the following formula (Ia): wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.
摘要翻译： 本发明涉及例如下式（Ia）的酰基哌嗪衍生物：其中R1a，R2，R3，R4，R5和R6如本文所述。 这些衍生物可用作抗炎剂。 本发明还涉及含有衍生物的药物组合物，以及使用该衍生物治疗人类炎性疾病的方法。
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公开(公告)号：US06534509B1
公开(公告)日：2003-03-18
申请号：US09713881
申请日：2000-11-15
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31495
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives, for example, of the following formula (1a): wherein R1a, R2, R3, R4, R5, and R6are descried herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmacetutical compostions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.
摘要翻译： 本发明涉及例如下式（1a）的酰基哌嗪衍生物：其中R1a，R2，R3，R4，R5和R6如本文所述。 这些衍生物可用作抗炎剂。 本发明还涉及含有衍生物的药物组合物，以及使用衍生物治疗人类炎症性疾病的方法。
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公开(公告)号：US06207665B1
公开(公告)日：2001-03-27
申请号：US09094397
申请日：1998-06-09
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Guo Ping Wei , Wei Xu , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Guo Ping Wei , Wei Xu , Wei Zheng
IPC分类号： A61K315377
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives of formula (Ia): wherein R1a, R2, R3, R4, R5 and R6 are defined herein, which are useful as anti-inflammatory agents. This invention is also directed to other acyl piperazine derivatives, pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
摘要翻译： 本发明涉及式（Ia）的酰基哌嗪衍生物：其中R1a，R2，R3，R4，R5和R6如本文所定义，其可用作抗炎剂。 本发明还涉及其它酰基哌嗪衍生物，含有本发明化合物的药物组合物，以及使用该化合物治疗人类炎性疾病的方法。
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公开(公告)号：US20060135487A1
公开(公告)日：2006-06-22
申请号：US11248618
申请日：2005-10-13
申请人： John Bauman , Brad Buckman , Ameen Ghannam , Joseph Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen May , Sean Monahan , Michael Morrissey , Howard Ng , Kenneth Shaw , Guo Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John Bauman , Brad Buckman , Ameen Ghannam , Joseph Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen May , Sean Monahan , Michael Morrissey , Howard Ng , Kenneth Shaw , Guo Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31/655 , A61K31/496 , A61K31/495
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
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10.发明授权Methods and compositions for modulating the interaction between the APJ receptor and the HIV virus 失效用于调节APJ受体和HIV病毒之间的相互作用的方法和组合物公开(公告)号：US06475718B2
公开(公告)日：2002-11-05
申请号：US09149045
申请日：1998-09-08
申请人： Robert W. Doms , Daryl Faulds , Joseph E. Hesselgesser , Richard Horuk , Branislava Mitrovic , Yiqing Zhou
发明人： Robert W. Doms , Daryl Faulds , Joseph E. Hesselgesser , Richard Horuk , Branislava Mitrovic , Yiqing Zhou
IPC分类号： C12Q170
CPC分类号： C07K14/7158 , A01K2217/05 , A61K38/00
摘要： The orphan seven transmembrane domain receptor, APJ, can function as a coreceptor for cellular infection by the HIV virus. The establishment of cell lines that coexpress CD4 and APJ provide valuable tools for continuing research on HIV infection and the development of anti-HIV therapeutics.
摘要翻译： 孤儿七跨膜结构域受体APJ可以作为HIV病毒细胞感染的共同受体。 共同表达CD4和APJ的细胞系的建立为持续研究艾滋病毒感染和抗艾滋病治疗的发展提供了有价值的工具。
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