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11.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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12.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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公开(公告)号：US07842672B2
公开(公告)日：2010-11-30
申请号：US11825395
申请日：2007-07-06
申请人： Constantine G. Boojamra , James M. Chen , Alan X. Huang , Choung U. Kim , Kuei-Ying Lin , Richard L. Mackman , David A. Oare , Jason K. Perry , Oliver L. Saunders , Sundaramoorthi Swaminathan , Lijun Zhang
发明人： Constantine G. Boojamra , James M. Chen , Alan X. Huang , Choung U. Kim , Kuei-Ying Lin , Richard L. Mackman , David A. Oare , Jason K. Perry , Oliver L. Saunders , Sundaramoorthi Swaminathan , Lijun Zhang
CPC分类号： C07H19/00
摘要： A compound of Formula I, Formula II, Formula III, or Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, therapeutic compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
摘要翻译： 式I，式II，式III或式IV化合物或其药学上可接受的盐，溶剂化物和/或酯，含有这些化合物的治疗组合物，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：US08318701B2
公开(公告)日：2012-11-27
申请号：US11658419
申请日：2005-07-26
申请人： Constantine G. Boojamra , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Oleg V. Petrakovsky , Adrian S. Ray , Lijun Zhang
发明人： Constantine G. Boojamra , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Oleg V. Petrakovsky , Adrian S. Ray , Lijun Zhang
IPC分类号： C07F9/6561 , A61P31/18 , A61K31/675 , C07D473/40 , C07D473/30
CPC分类号： C07H19/16 , A61K31/341 , A61K31/513 , A61K31/662 , A61K31/675 , A61K31/683 , A61K45/06 , C07F9/65616 , C07H19/00 , C07H19/20 , A61K2300/00
摘要： The invention is related to phosphorus substituted anti-viral inhibitory compounds, 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： 本发明涉及磷取代的抗病毒抑制化合物，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：US20090202470A1
公开(公告)日：2009-08-13
申请号：US11658419
申请日：2005-07-26
申请人： Constantine G. Boojamra , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Oleg V. Petrakosvsky , Adrian S. Ray , Lijun Zhang
发明人： Constantine G. Boojamra , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Oleg V. Petrakosvsky , Adrian S. Ray , Lijun Zhang
CPC分类号： C07H19/16 , A61K31/341 , A61K31/513 , A61K31/662 , A61K31/675 , A61K31/683 , A61K45/06 , C07F9/65616 , C07H19/00 , C07H19/20 , A61K2300/00
摘要： The invention is related to phosphorus substituted anti-viral inhibitory compounds, 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： 本发明涉及磷取代的抗病毒抑制化合物，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：US08329926B2
公开(公告)日：2012-12-11
申请号：US11658628
申请日：2005-07-27
申请人： Constantine G. Boojamra , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Oleg V. Petrakovsky , Adrian S. Ray , Lijun Zhang
发明人： Constantine G. Boojamra , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Oleg V. Petrakovsky , Adrian S. Ray , Lijun Zhang
IPC分类号： C07F9/06 , C07F9/02 , C07D473/00
CPC分类号： C07H19/16 , A61K31/341 , A61K31/513 , A61K31/662 , A61K31/675 , A61K31/683 , A61K45/06 , C07F9/65616 , C07H19/00 , C07H19/20 , A61K2300/00
摘要： The invention is related to phosphorus substituted anti-viral inhibitory compounds, 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： 本发明涉及磷取代的抗病毒抑制化合物，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：US20090012037A1
公开(公告)日：2009-01-08
申请号：US11658628
申请日：2005-07-27
申请人： Constantine G. Boojamra , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Oleg V. Petrakovsky , Adrian S. Ray , Lijun Zhang
发明人： Constantine G. Boojamra , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Oleg V. Petrakovsky , Adrian S. Ray , Lijun Zhang
IPC分类号： A61K31/7076 , C07H19/19 , C07H19/20
CPC分类号： C07H19/16 , A61K31/341 , A61K31/513 , A61K31/662 , A61K31/675 , A61K31/683 , A61K45/06 , C07F9/65616 , C07H19/00 , C07H19/20 , A61K2300/00
摘要： The invention is related to phosphorus substituted anti-viral inhibitory compounds, 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： 本发明涉及磷取代的抗病毒抑制化合物，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：US20080107628A1
公开(公告)日：2008-05-08
申请号：US11825395
申请日：2007-07-06
申请人： Constantine Boojamra , James Chen , Alan Huang , Choung Kim , Kuei-Ying Lin , Richard Mackman , David Oare , Jason Perry , Oliver Saunders , Sundaramoorthi Swaminathan , Lijun Zhang
发明人： Constantine Boojamra , James Chen , Alan Huang , Choung Kim , Kuei-Ying Lin , Richard Mackman , David Oare , Jason Perry , Oliver Saunders , Sundaramoorthi Swaminathan , Lijun Zhang
IPC分类号： A61K38/21 , C07F9/02 , A61K31/675 , A61P31/00
CPC分类号： C07H19/00
摘要： A compound of Formula I, Formula II, Formula III, or Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, therapeutic compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
摘要翻译： 式I，式II，式III或式IV化合物或其药学上可接受的盐，溶剂合物和/或酯，含有这些化合物的治疗组合物，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：US07871991B2
公开(公告)日：2011-01-18
申请号：US11190225
申请日：2005-07-26
申请人： Constantine G. Boojamra , Kuei-Ying Lin , Richard Mackman , David Y. Markevitch , Oleg V. Petrakovsky , Adrian S. Ray , Lijun Zhang
发明人： Constantine G. Boojamra , Kuei-Ying Lin , Richard Mackman , David Y. Markevitch , Oleg V. Petrakovsky , Adrian S. Ray , Lijun Zhang
IPC分类号： C07F9/6561 , A61K31/675 , A61P31/18 , C07D473/40 , C07D473/34 , C07D473/30
CPC分类号： C07H19/16 , A61K31/341 , A61K31/513 , A61K31/662 , A61K31/675 , A61K31/683 , A61K45/06 , C07F9/65616 , C07H19/00 , C07H19/20 , A61K2300/00
摘要： The invention is related to phosphorus substituted anti-viral inhibitory compounds, 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： 本发明涉及磷取代的抗病毒抑制化合物，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：US06967079B2
公开(公告)日：2005-11-22
申请号：US10294066
申请日：2002-11-14
申请人： Mark Matteucci , Robert J. Jones , Kuei-Ying Lin
发明人： Mark Matteucci , Robert J. Jones , Kuei-Ying Lin
IPC分类号： C12N15/09 , A61K31/565 , A61K31/70 , A61K31/7042 , A61K31/7052 , C07D239/46 , C07D239/47 , C07D239/52 , C07D239/54 , C07D405/04 , C07D487/04 , C07D487/14 , C07D491/14 , C07D498/04 , C07D498/14 , C07F7/22 , C07F9/09 , C07H19/00 , C07H19/04 , C07H19/06 , C07H19/22 , C07H21/00 , C07H21/02 , C12P19/34 , C12Q1/68
CPC分类号： C07D239/47 , C07D239/54 , C07D405/04 , C07D487/04 , C07F7/2208 , C07H19/06 , C07H19/073 , C07H21/00 , C12Q1/6816 , C12Q1/686 , Y02P20/55
摘要： Compounds having particular interest as labels and various novel uses in diagnostics and therapeutics are provided which have structure (1) wherein R1 is a binding partner, a linker or H; a and b are 0 or 1, provided that the total of a and b is 0 or 1; A is N or C; X is S, O, —C(O)—, NH or NCH2R6; Y is —C(O)—; Z is taken together with A to form an aryl or heteroaryl ring structure comprising 5 or 6 ring atoms wherein the heteroaryl ring comprises a single O ring heteroatom, a single N ring heteroatom, a single S ring heteroatom, a single O and a single N ring heteroatom separated by a carbon atom, a single S and a single N ring heteroatom separated by a carbon atom, 2 N ring heteroatoms separated by a carbon atom, or 3 N ring heteroatoms at least two of which are separated by a carbon atom, and wherein the aryl or heteroaryl ring carbon atoms are unsubstituted with other than H or at least 1 nonbridging ring carbon atom is substituted with R6 or ═O; R6 is independently H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, NO2, N(R3)2, C≡N or halo, or an R6 is taken together with an adjacent R6 to complete a ring containing 5 or 6 ring atoms; R3 is a protecting group or H; and tautomers, solvates and salts thereof; and provided that where a is 0, b is 1, and R1 is in which D2 is independently hydroxyl, blocked hydroxyl, mono, di or triphosphate, or an oligodeoxyribonucleotide otherwise containing only the bases A, G, T and C; and D3 is H or OH; then Z is not unsubstituted phenyl. Also provided are novel intermediates and methods for the preparation and use of the structure (1) compounds.
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