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公开(公告)号：US20080070910A1
公开(公告)日：2008-03-20
申请号：US11880743
申请日：2007-07-24
IPC分类号： C07D493/04 , A61K31/341 , A61K31/352 , A61K31/357 , A61K31/427 , A61K31/536 , C12N9/99 , A61P31/18 , C07D277/22 , C07D307/02 , C07D307/77 , C07D413/00
CPC分类号： C07D493/04
摘要： The present invention provides compounds of Formula (I): wherein A, X, Q, R2-R6, m, and W have the values described herein, as well as compositions comprising such compounds. The compounds are protease inhibitors and are useful for inhibiting the development of drug resistance in animals.
摘要翻译： 本发明提供式（I）的化合物：其中A，X，Q，R 2，R 6，M和W也具有本文所述的值 作为包含这些化合物的组合物。 这些化合物是蛋白酶抑制剂，可用于抑制动物耐药性的发展。
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2.发明申请Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds 有权HIV蛋白酶抑制剂化合物的膦酸酯类似物的细胞积累公开(公告)号：US20050209197A1
公开(公告)日：2005-09-22
申请号：US10423496
申请日：2003-04-25
申请人： Murty Arimilli , Mark Becker , Clifford Bryant , James Chen , Xiaowu Chen , Azar Dastgah , Maria Fardis , Gong-Xin He , Haolun Jin , Choung Kim , William Lee , Christopher Lee , Kuei-Ying Lin , Hongtao Liu , Richard Mackman , Michael Mitchell , Peter Nelson , Hyung-Jung Pyun , Tanisha Rowe , Mark Sparacino , Sundaramoorthi Swaminathan , James Tario , Jianying Wang , Matthew Williams , Lianhong Xu , Zheng-Yu Yang , Richard Yu , Jiancun Zhang , Lijun Zhang
发明人： Murty Arimilli , Mark Becker , Clifford Bryant , James Chen , Xiaowu Chen , Azar Dastgah , Maria Fardis , Gong-Xin He , Haolun Jin , Choung Kim , William Lee , Christopher Lee , Kuei-Ying Lin , Hongtao Liu , Richard Mackman , Michael Mitchell , Peter Nelson , Hyung-Jung Pyun , Tanisha Rowe , Mark Sparacino , Sundaramoorthi Swaminathan , James Tario , Jianying Wang , Matthew Williams , Lianhong Xu , Zheng-Yu Yang , Richard Yu , Jiancun Zhang , Lijun Zhang
IPC分类号： C12N9/99 , A61K31/4155 , A61K31/66 , A61K31/665 , A61K31/675 , A61P31/18 , A61P43/00 , C07D213/75 , C07D213/85 , C07D231/12 , C07D231/20 , C07D233/42 , C07D239/48 , C07D239/80 , C07D243/04 , C07D265/18 , C07D307/68 , C07D401/06 , C07D403/06 , C07D471/14 , C07D491/04 , C07F20060101 , C07F9/02 , C07F9/38 , C07F9/40 , C07F9/44 , C07F9/58 , C07F9/62 , C07F9/645 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/653 , C07F9/6533 , C07F9/655 , C07F9/6558 , C07F9/6561 , C07F9/6584 , C12N9/16 , C12Q1/18 , C12Q1/37 , C12Q1/44 , C12Q1/70 , G01N33/04 , G01N33/50
CPC分类号： A61K31/66 , A61K31/675 , C07D213/75 , C07D213/85 , C07D231/12 , C07D231/20 , C07D233/42 , C07D239/49 , C07D239/80 , C07D243/04 , C07D265/18 , C07D307/68 , C07D401/06 , C07D403/06 , C07D471/14 , C07D491/04 , C07F9/4006 , C07F9/58 , C07F9/645 , C07F9/6506 , C07F9/650905 , C07F9/650947 , C07F9/6512 , C07F9/65128 , C07F9/65335 , C07F9/65515 , C07F9/65583 , C07F9/6561 , C12N9/16 , C12Q1/18 , C12Q1/37 , C12Q1/44 , C40B40/04 , G01N33/5038 , G01N2333/16 , G01N2500/04
摘要： Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.
摘要翻译： 公开了具有用作治疗剂和其它工业目的的具有HIV蛋白酶抑制性质的膦酸酯取代的化合物。 组合物抑制HIV蛋白酶活性和/或可用于治疗AIDS和其它抗病毒感染以及用于检测HIV蛋白酶的测定。
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3.发明申请Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds 审中-公开蜂窝状蛋白酶抑制剂化合物的膦酸酯类似物的细胞积累公开(公告)号：US20070010489A1
公开(公告)日：2007-01-11
申请号：US10511998
申请日：2003-04-25
申请人： Murty Arimilli , Mark Becker , Clifford Bryant , James Chen , Xiaowu Chen , Azar Dastgah , Maria Fardis , Gong-Xin He , Haolun Jin , Choung Kim , William Lee , Christopher Lee , Kuei-Ying Lin , Hongtao Liu , Richard Mackman , Michael Mitchell , Peter Nelson , Hyung-Jung Pyun , Tanisha Rowe , Mark Sparacino , Sundaramoorthi Swaminathan , James Tario , Jianying Wang , Matthew Wiliams , Lianhong Xu , Zheng-Yu Yang , Richard Yu , Jiancun Zhang , Lijun Zhang
发明人： Murty Arimilli , Mark Becker , Clifford Bryant , James Chen , Xiaowu Chen , Azar Dastgah , Maria Fardis , Gong-Xin He , Haolun Jin , Choung Kim , William Lee , Christopher Lee , Kuei-Ying Lin , Hongtao Liu , Richard Mackman , Michael Mitchell , Peter Nelson , Hyung-Jung Pyun , Tanisha Rowe , Mark Sparacino , Sundaramoorthi Swaminathan , James Tario , Jianying Wang , Matthew Wiliams , Lianhong Xu , Zheng-Yu Yang , Richard Yu , Jiancun Zhang , Lijun Zhang
IPC分类号： A61K31/663 , C07F9/6515 , C07F9/6512
CPC分类号： A61K31/66 , A61K31/675 , C07D213/75 , C07D213/85 , C07D231/12 , C07D231/20 , C07D233/42 , C07D239/49 , C07D239/80 , C07D243/04 , C07D265/18 , C07D307/68 , C07D401/06 , C07D403/06 , C07D471/14 , C07D491/04 , C07F9/4006 , C07F9/58 , C07F9/645 , C07F9/6506 , C07F9/650905 , C07F9/650947 , C07F9/6512 , C07F9/65128 , C07F9/65335 , C07F9/65515 , C07F9/65583 , C07F9/6561 , C12N9/16 , C12Q1/18 , C12Q1/37 , C12Q1/44 , C40B40/04 , G01N33/5038 , G01N2333/16 , G01N2500/04
摘要： Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit 5 HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.
摘要翻译： 公开了具有用作治疗剂和其它工业目的的具有HIV蛋白酶抑制性质的膦酸酯取代的化合物。 该组合物抑制5种HIV蛋白酶活性和/或用于治疗AIDS和其它抗病毒感染以及用于检测HIV蛋白酶的测定。
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4.发明申请公开(公告)号：US20050239054A1
公开(公告)日：2005-10-27
申请号：US10740694
申请日：2003-12-22
申请人： Murty Arimilli , Mark Becker , Gabriel Birkus , Clifford Bryant , James Chen , Xiaowu Chen , Tomas Cihlar , Azar Dastgah , Eugene Eisenberg , Maria Fardis , Marcos Hatada , Gong-Xin He , Haolun Jin , Choung Kim , William Lee , Christopher Lee , Kuei-Ying Lin , Hongtao Liu , Richard MacKman , Martin McDermott , Michael Mitchell , Peter Nelson , Hyung-Jung Pyun , Tanisha Rowe , Mark Sparacino , Sundaramoorthi Swaminathan , James Tario , Jianying Wang , Matthew Williams , Lianhong Xu , Zheng-Yu Yang , Richard Yu , Jiancun Zhang , Lijun Zhang
发明人： Murty Arimilli , Mark Becker , Gabriel Birkus , Clifford Bryant , James Chen , Xiaowu Chen , Tomas Cihlar , Azar Dastgah , Eugene Eisenberg , Maria Fardis , Marcos Hatada , Gong-Xin He , Haolun Jin , Choung Kim , William Lee , Christopher Lee , Kuei-Ying Lin , Hongtao Liu , Richard MacKman , Martin McDermott , Michael Mitchell , Peter Nelson , Hyung-Jung Pyun , Tanisha Rowe , Mark Sparacino , Sundaramoorthi Swaminathan , James Tario , Jianying Wang , Matthew Williams , Lianhong Xu , Zheng-Yu Yang , Richard Yu , Jiancun Zhang , Lijun Zhang
IPC分类号： C12N9/99 , A61K31/4155 , A61K31/66 , A61K31/665 , A61K31/675 , A61P31/18 , A61P43/00 , C07D213/75 , C07D213/85 , C07D231/12 , C07D231/20 , C07D233/42 , C07D239/48 , C07D239/80 , C07D243/04 , C07D265/18 , C07D307/68 , C07D401/06 , C07D403/06 , C07D471/14 , C07D491/04 , C07F20060101 , C07F9/02 , C07F9/38 , C07F9/40 , C07F9/44 , C07F9/58 , C07F9/62 , C07F9/645 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/653 , C07F9/6533 , C07F9/655 , C07F9/6558 , C07F9/6561 , C07F9/6584 , C12N9/16 , C12Q1/18 , C12Q1/37 , C12Q1/44 , C12Q1/70 , G01N33/04 , G01N33/50
CPC分类号： A61K31/66 , A61K31/675 , C07D213/75 , C07D213/85 , C07D231/12 , C07D231/20 , C07D233/42 , C07D239/49 , C07D239/80 , C07D243/04 , C07D265/18 , C07D307/68 , C07D401/06 , C07D403/06 , C07D471/14 , C07D491/04 , C07F9/4006 , C07F9/58 , C07F9/645 , C07F9/6506 , C07F9/650905 , C07F9/650947 , C07F9/6512 , C07F9/65128 , C07F9/65335 , C07F9/65515 , C07F9/65583 , C07F9/6561 , C12N9/16 , C12Q1/18 , C12Q1/37 , C12Q1/44 , C40B40/04 , G01N33/5038 , G01N2333/16 , G01N2500/04 , G01N2500/20
摘要： Methods are provided for identifying anti-HIV therapeutic compounds substituted with carboxyl ester or phosphonate ester groups. Libraries of such compounds are screened optionally using the novel enzyme GS-7340 Ester Hydrolase. Compositions and methods relating to GS-7340 Ester Hydrolase also are provided.
摘要翻译： 提供了用于鉴定被羧基酯或膦酸酯基取代的抗HIV治疗化合物的方法。 可以使用新型GS-7340酯水解酶来筛选这些化合物的文库。 还提供了与GS-7340酯水解酶有关的组合物和方法。
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5.发明授权Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds 有权HIV蛋白酶抑制剂化合物的膦酸酯类似物的细胞积累公开(公告)号：US07649015B2
公开(公告)日：2010-01-19
申请号：US10423496
申请日：2003-04-25
申请人： Murty N. Arimili , Xiaowu Chen , Maria Fardis , Gong-Xin He , Haolun Jin , Choung U. Kim , William A. Lee , Kuei-Ying Lin , Hongtao Liu , Richard L. Mackman , Michael L. Mitchell , Hyung-Jung Pyun , Mark Sparacino , Sundaramoorthi Swaminathan , Jianying Wang , Matthew A. Williams , Lianhong Xu , Zheng-Yu Yang , Richard H. Yu , Jiancun Zhang , Lijun Zhang
发明人： Murty N. Arimili , Xiaowu Chen , Maria Fardis , Gong-Xin He , Haolun Jin , Choung U. Kim , William A. Lee , Kuei-Ying Lin , Hongtao Liu , Richard L. Mackman , Michael L. Mitchell , Hyung-Jung Pyun , Mark Sparacino , Sundaramoorthi Swaminathan , Jianying Wang , Matthew A. Williams , Lianhong Xu , Zheng-Yu Yang , Richard H. Yu , Jiancun Zhang , Lijun Zhang
IPC分类号： A61K31/343 , C07F9/28
CPC分类号： A61K31/66 , A61K31/675 , C07D213/75 , C07D213/85 , C07D231/12 , C07D231/20 , C07D233/42 , C07D239/49 , C07D239/80 , C07D243/04 , C07D265/18 , C07D307/68 , C07D401/06 , C07D403/06 , C07D471/14 , C07D491/04 , C07F9/4006 , C07F9/58 , C07F9/645 , C07F9/6506 , C07F9/650905 , C07F9/650947 , C07F9/6512 , C07F9/65128 , C07F9/65335 , C07F9/65515 , C07F9/65583 , C07F9/6561 , C12N9/16 , C12Q1/18 , C12Q1/37 , C12Q1/44 , C40B40/04 , G01N33/5038 , G01N2333/16 , G01N2500/04
摘要： Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.
摘要翻译： 公开了具有用作治疗剂和其它工业目的的具有HIV蛋白酶抑制性质的膦酸酯取代的化合物。 组合物抑制HIV蛋白酶活性和/或可用于治疗AIDS和其它抗病毒感染以及用于检测HIV蛋白酶的测定。
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公开(公告)号：US20090312318A1
公开(公告)日：2009-12-17
申请号：US12307634
申请日：2007-07-24
IPC分类号： A61K31/5377 , C07D493/04 , A61K31/34 , C12N9/99
CPC分类号： C07D493/04
摘要： The present invention provides compounds of Formula (I): wherein A, X, Q, R2-R6, m, and W have the values described herein, as well as compositions comprising such compounds. The compounds are protease inhibitors and are useful for inhibiting the development of drug resistance in animals.
摘要翻译： 本发明提供式（I）的化合物：其中A，X，Q，R 2 -R 6，m和W具有本文所述的值，以及包含这些化合物的组合物。 这些化合物是蛋白酶抑制剂，可用于抑制动物耐药性的发展。
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公开(公告)号：US20060264404A1
公开(公告)日：2006-11-23
申请号：US11258621
申请日：2005-10-25
申请人： Constantine Boojamra , Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Manoj Desai , Maria Fardis , Craig Gibbs , Ralph Hirschmann , Alan Huang , Haolun Jin , Choung Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher Lee , William Lee , Kuei-Ying Lin , Richard Mackman , David Markevitch , Peter Nelson , David Oare , Vidya Prasad , Hyung-Jung Pyun , Adrian Ray , Rosemarie Sherlock , Sundaramoorthi Swaminathan , William Watkins , Jennifer Zhang , Lijun Zhang
发明人： Constantine Boojamra , Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Manoj Desai , Maria Fardis , Craig Gibbs , Ralph Hirschmann , Alan Huang , Haolun Jin , Choung Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher Lee , William Lee , Kuei-Ying Lin , Richard Mackman , David Markevitch , Peter Nelson , David Oare , Vidya Prasad , Hyung-Jung Pyun , Adrian Ray , Rosemarie Sherlock , Sundaramoorthi Swaminathan , William Watkins , Jennifer Zhang , Lijun Zhang
IPC分类号： A61K31/675 , C07F9/6512
CPC分类号： C07F9/65616 , C07F9/4006 , C07F9/4465 , C07F9/5304 , C07F9/650952 , C07F9/653 , C07F9/65507 , C07F9/65515 , C07F9/65517 , C07F9/65583 , C07F9/65586 , C07F9/6561
摘要： The invention is related to phosphorus substituted therapeutic agents, compositions containing such phosphorus substituted agents, and therapeutic methods that include the administration of such phosphorus substituted agents, as well as to processes and intermediates useful for preparing such agents.
摘要翻译： 本发明涉及磷取代的治疗剂，含有这种磷取代剂的组合物，以及包括施用这种磷取代剂的治疗方法，以及可用于制备这种药剂的方法和中间体。
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公开(公告)号：US20060035866A1
公开(公告)日：2006-02-16
申请号：US10833295
申请日：2004-04-26
申请人： Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Manoj Desai , Maria Fardis , Alan Huang , Thorsten Kirschberg , Christopher Lee , Richard Mackman , Peter Nelson , Hyung-Jung Pyun , Adrian Ray , William Watkins , Jennifer Zhang , Sundaramoorthi Swaminathan
发明人： Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Manoj Desai , Maria Fardis , Alan Huang , Thorsten Kirschberg , Christopher Lee , Richard Mackman , Peter Nelson , Hyung-Jung Pyun , Adrian Ray , William Watkins , Jennifer Zhang , Sundaramoorthi Swaminathan
IPC分类号： A61K31/66
CPC分类号： A61K47/548 , A61K47/542
摘要： The invention is related to phosphonate substituted compounds having immuno-modulatory activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明涉及具有免疫调节活性的膦酸酯取代的化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。
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公开(公告)号：US20090099096A1
公开(公告)日：2009-04-16
申请号：US11880067
申请日：2007-07-19
申请人： Carina E. Cannizzaro , James M. Chen , Manoj C. Desai , Michael L. Mitchell , Sundaramoorthi Swaminathan , Lianhong Xu
发明人： Carina E. Cannizzaro , James M. Chen , Manoj C. Desai , Michael L. Mitchell , Sundaramoorthi Swaminathan , Lianhong Xu
CPC分类号： C07D493/04 , C07D405/12 , C07D519/00
摘要： The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，溶剂合物，酯和/或膦酸盐，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法。
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公开(公告)号：US20090306112A1
公开(公告)日：2009-12-10
申请号：US12307674
申请日：2007-07-19
申请人： Carina E. Cannizzaro , James M. Chen , Manoj C. Desai , Michael L. Mitchell , Sundaramoorthi Swaminathan , Lianhong Xu , Zheng-Yu Yang
发明人： Carina E. Cannizzaro , James M. Chen , Manoj C. Desai , Michael L. Mitchell , Sundaramoorthi Swaminathan , Lianhong Xu , Zheng-Yu Yang
IPC分类号： A61K31/505 , C07D405/02 , A61K31/443 , C12N5/00 , C12N7/04 , C07D405/14 , C07D215/38 , A61K31/47 , C07D417/02 , A61K31/4439 , C07D213/02 , A61K31/44 , C07D239/02 , C07D249/08 , A61K31/4196 , C07D257/04 , A61K31/41 , C07D277/22 , A61K31/426
CPC分类号： C07D405/12 , C07D213/56 , C07D401/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D417/12 , C07D493/04 , C07F9/65583 , C07F9/65586 , C07F9/6561
摘要： The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，溶剂化物，酯和/或膦酸酯，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法。
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