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1. 发明申请

US20060264404A1 Therapeutic phosphonate compounds 有权
标题翻译：治疗性膦酸酯化合物
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。

2. 发明申请

US20060079478A1 Anti-cancer phosphonate analogs 失效
标题翻译：抗癌膦酸类似物
公开(公告)号：US20060079478A1
公开(公告)日：2006-04-13
申请号：US10833293
申请日：2004-04-26
申请人： Constantine Boojamra , Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Maria Fardis , Alan Huang , Choung Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher Lee , Kuei-Ying Lin , Richard Mackman , David Markevitch , Peter Nelson , David Oare , Vidya Prasad , Hyung-Jung Pyun , Adrian Ray , Sundaramoorthi Swaminathan , William Watkins , Jennifer Zhang , Lijun Zhang
发明人： Constantine Boojamra , Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Maria Fardis , Alan Huang , Choung Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher Lee , Kuei-Ying Lin , Richard Mackman , David Markevitch , Peter Nelson , David Oare , Vidya Prasad , Hyung-Jung Pyun , Adrian Ray , Sundaramoorthi Swaminathan , William Watkins , Jennifer Zhang , Lijun Zhang
IPC分类号： A61K31/7076 , A61K31/7072 , C07H19/04 , A61K31/675
CPC分类号： A61K31/7076 , A61K31/675 , A61K31/7072 , A61K47/548 , C07H19/04
摘要： The invention is related to phosphorus substituted anti-cancer 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癌化合物，含有这些化合物的组合物和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。

3. 发明授权

US07645747B2 Therapeutic phosphonate compounds 有权
标题翻译：治疗性膦酸酯化合物
公开(公告)号：US07645747B2
公开(公告)日：2010-01-12
申请号：US11258621
申请日：2005-10-25
申请人： Constantine G. Boojamra , Carina E. Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Craig S. Gibbs , Ralph F. Hirschmann , Alan X. Huang , Haolun Jin , Choung U. Kim , Thorsten A. Kirschberg , Steven Krawczyk , Christopher P. Lee , William A. Lee , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Peter H. Nelson , David A. Oare , Vidya K. Prasad , Hyung-Jung Pyun , Adrian S. Ray , Rosemarie Sherlock , Sundaramoorthi Swaminathan , William J. Watkins , Jennifer R. Zhang , Lijun Zhang
发明人： Constantine G. Boojamra , Carina E. Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Craig S. Gibbs , Ralph F. Hirschmann , Alan X. Huang , Haolun Jin , Choung U. Kim , Thorsten A. Kirschberg , Steven Krawczyk , Christopher P. Lee , William A. Lee , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Peter H. Nelson , David A. Oare , Vidya K. Prasad , Hyung-Jung Pyun , Adrian S. Ray , Rosemarie Sherlock , Sundaramoorthi Swaminathan , William J. Watkins , Jennifer R. Zhang , Lijun Zhang
IPC分类号： A61K31/661 , A61K31/662 , C07F9/06 , C07F9/28
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。

4. 发明申请

US20100022467A1 ANTI-CANCER PHOSPHONATE ANALOGS 审中-公开
标题翻译：抗癌剂磷酸酯类似物
公开(公告)号：US20100022467A1
公开(公告)日：2010-01-28
申请号：US12202719
申请日：2008-09-02
申请人： Constantine G. Boojamra , Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Maria Fardis , Alan X. Huang , Choung U. Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher P. Lee , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Peter H. Nelson , David A. Oare , Vidya K. Prasad , Hyung-Jung Pyun , Adrian S. Ray , Sundaramoorthi Swaminathan , William J. Watkins , Jennifer R. Zhang , Lijun Zhang
发明人： Constantine G. Boojamra , Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Maria Fardis , Alan X. Huang , Choung U. Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher P. Lee , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Peter H. Nelson , David A. Oare , Vidya K. Prasad , Hyung-Jung Pyun , Adrian S. Ray , Sundaramoorthi Swaminathan , William J. Watkins , Jennifer R. Zhang , Lijun Zhang
IPC分类号： A61K31/7076 , C07H19/20 , A61P35/00
CPC分类号： A61K31/7076 , A61K31/675 , A61K31/7072 , A61K47/548 , C07H19/04
摘要： The invention is related to phosphorus substituted anti-cancer 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癌化合物，含有这些化合物的组合物和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。

5. 发明授权

US07452901B2 Anti-cancer phosphonate analogs 失效
标题翻译：抗癌膦酸类似物
公开(公告)号：US07452901B2
公开(公告)日：2008-11-18
申请号：US10833293
申请日：2004-04-26
申请人： Constantine G. Boojamra , Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Maria Fardis , Alan X. Huang , Choung U. Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher P. Lee , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Peter H. Nelson , David A. Oare , Vidya K. Prasad , Hyung-Jung Pyun , Adrian S. Ray , Sundaramoorthi Swaminathan , William J. Watkins , Jennifer R. Zhang , Lijun Zhang
发明人： Constantine G. Boojamra , Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Maria Fardis , Alan X. Huang , Choung U. Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher P. Lee , Kuei-Ying Lin , Richard L. Mackman , David Y. Markevitch , Peter H. Nelson , David A. Oare , Vidya K. Prasad , Hyung-Jung Pyun , Adrian S. Ray , Sundaramoorthi Swaminathan , William J. Watkins , Jennifer R. Zhang , Lijun Zhang
IPC分类号： A61K31/44 , C07D239/00
CPC分类号： A61K31/7076 , A61K31/675 , A61K31/7072 , A61K47/548 , C07H19/04
摘要： The invention is related to phosphorus substituted anti-cancer 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癌化合物，含有这些化合物的组合物和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。

6. 发明申请

US20050227947A1 Phosphonate analogs for treating metabolic diseases 失效
标题翻译：用于治疗代谢性疾病的膦酸酯类似物
公开(公告)号：US20050227947A1
公开(公告)日：2005-10-13
申请号：US10832817
申请日：2004-04-26
申请人： James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Maria Fardis , Thorsten Kirschberg , Steven Krawczyk , Hyung-Jung Pyun , William Watkins
发明人： James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Maria Fardis , Thorsten Kirschberg , Steven Krawczyk , Hyung-Jung Pyun , William Watkins
IPC分类号： A61K31/66 , A61K31/675
CPC分类号： A61K31/66 , A61K31/675 , A61K47/548
摘要： The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, 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：本发明涉及具有用于治疗代谢性疾病和/或病症（例如糖尿病和高胆固醇血症）的活性的磷取代的化合物，以及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此类化合物。

7. 发明申请

US20090131372A1 PHOSPHONATE ANALOGS FOR TREATING METABOLIC DISEASES 审中-公开
标题翻译：用于治疗代谢性疾病的磷酸酯类似物
公开(公告)号：US20090131372A1
公开(公告)日：2009-05-21
申请号：US12145329
申请日：2008-06-24
申请人： James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Maria Fardis , Thorsten Kirschberg , Steven Krawczyk , Hyung-Jung Pyun , William J. Watkins
发明人： James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Maria Fardis , Thorsten Kirschberg , Steven Krawczyk , Hyung-Jung Pyun , William J. Watkins
IPC分类号： A61K31/675 , C07F9/38 , A61P3/00
CPC分类号： A61K31/66 , A61K31/675 , A61K47/548
摘要： The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, 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：本发明涉及具有用于治疗代谢性疾病和/或病症（例如糖尿病和高胆固醇血症）的活性的磷取代的化合物，以及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此类化合物。

8. 发明授权

US07407965B2 Phosphonate analogs for treating metabolic diseases 失效
标题翻译：用于治疗代谢性疾病的膦酸酯类似物
公开(公告)号：US07407965B2
公开(公告)日：2008-08-05
申请号：US10832817
申请日：2004-04-26
申请人： James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Maria Fardis , Thorsten Kirschberg , Steven Krawczyk , Hyung-Jung Pyun , William J. Watkins
发明人： James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Maria Fardis , Thorsten Kirschberg , Steven Krawczyk , Hyung-Jung Pyun , William J. Watkins
IPC分类号： A61K31/505 , C07F9/02
CPC分类号： A61K31/66 , A61K31/675 , A61K47/548
摘要： The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, 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：本发明涉及具有用于治疗代谢性疾病和/或病症（例如糖尿病和高胆固醇血症）的活性的磷取代的化合物，以及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此类化合物。

9. 发明申请

US20050059637A1 Nucleobase phosphonate analogs for antiviral treatment 有权
标题翻译：用于抗病毒治疗的核碱基膦酸酯类似物
公开(公告)号：US20050059637A1
公开(公告)日：2005-03-17
申请号：US10903288
申请日：2004-07-30
申请人： Steven Krawczyk
发明人： Steven Krawczyk
IPC分类号： C07F9/6561 , A61K31/675
CPC分类号： C07F9/65616 , A61K31/675
摘要： The present invention provides novel compounds with activity against infectious viruses. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication of the virus. They are useful for treating human patients infected with a human retrovirus, such as human immunodeficiency virus (strains of HIV-1 or HIV-2) or human T-cell leukemia viruses (HTLV-I or HTLV-II) which results in acquired immunodeficiency syndrome (AIDS) and/or related diseases. The present invention also relates generally to the accumulation or retention of therapeutic compounds inside cells. The invention is more particularly related to attaining high concentrations of active metabolite molecules in HIV infected cells. Intracellular targeting may be achieved by methods and compositions which allow accumulation or retention of biologically active agents inside cells. Such effective targeting may be applicable to a variety of therapeutic formulations and procedures.
摘要翻译：本发明提供具有抗感染性病毒活性的新型化合物。本发明的化合物可以抑制逆转录病毒逆转录酶，从而抑制病毒的复制。它们可用于治疗感染人类逆转录病毒的人类患者，例如导致获得性免疫缺陷的人类免疫缺陷病毒（HIV-1或HIV-2的菌株）或人T细胞白血病病毒（HTLV-1或HTLV-II）综合征（AIDS）和/或相关疾病。本发明一般还涉及细胞内治疗化合物的积聚或保留。本发明更具体地涉及在HIV感染细胞中获得高浓度的活性代谢物分子。细胞内靶向可以通过允许生物活性剂在细胞内积累或保留的方法和组合物来实现。这种有效靶向可以适用于多种治疗剂型和方法。

10. 发明申请

US20060252729A1 Nucleobase phosphonate analogs for antiviral treatment 审中-公开
标题翻译：用于抗病毒治疗的核碱基膦酸酯类似物
公开(公告)号：US20060252729A1
公开(公告)日：2006-11-09
申请号：US10566819
申请日：2004-07-30
申请人： Steven Krawczyk
发明人： Steven Krawczyk
IPC分类号： C07F9/6512 , A61K31/675
CPC分类号： C07F9/65616 , A61K31/675
摘要： The present invention provides novel compounds with activity against infectious viruses. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication of the virus. They are useful for treating human patients infected with a human retrovirus, such as human immunodeficiency virus (strains of HIV-1 or HIV-2) or human T-cell leukemia viruses (HTLV-I or HTLV-II) which results in acquired immunodeficiency syndrome (AIDS) and/or related diseases. The present invention also relates generally to the accumulation or retention of therapeutic compounds inside cells. The invention is more particularly related to attaining high concentrations of active metabolite molecules in HIV infected cells. Intracellular targeting may be achieved by methods and compositions which allow accumulation or retention of biologically active agents inside cells. Such effective targeting may be applicable to a variety of therapeutic formulations and procedures.
摘要翻译：本发明提供具有抗感染性病毒活性的新型化合物。本发明的化合物可以抑制逆转录病毒逆转录酶，从而抑制病毒的复制。它们可用于治疗感染人类逆转录病毒的人类患者，例如导致获得性免疫缺陷的人类免疫缺陷病毒（HIV-1或HIV-2的菌株）或人T细胞白血病病毒（HTLV-1或HTLV-II）综合征（AIDS）和/或相关疾病。本发明一般还涉及细胞内治疗化合物的积聚或保留。本发明更具体地涉及在HIV感染细胞中获得高浓度的活性代谢物分子。细胞内靶向可以通过允许生物活性剂在细胞内积累或保留的方法和组合物来实现。这种有效靶向可以适用于多种治疗剂型和方法。

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