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1. 发明申请

US20100273740A1 Phospholipids for the Treatment of Infection by Togaviruses, Herpes Viruses and Coronaviruses 审中-公开
标题翻译：用于治疗披膜病毒，疱疹病毒和冠状病毒感染的磷脂
公开(公告)号：US20100273740A1
公开(公告)日：2010-10-28
申请号：US12623612
申请日：2009-11-23
申请人： Ronald A. FLEMING , Jan V. Hes , Yunsheng Huang , Russ H. Read , Susan L. Morris-Natschke , Khalid S. Ishaq , Louis S. Kucera , Phillip A. Furman
发明人： Ronald A. FLEMING , Jan V. Hes , Yunsheng Huang , Russ H. Read , Susan L. Morris-Natschke , Khalid S. Ishaq , Louis S. Kucera , Phillip A. Furman
IPC分类号： A61K31/661 , A61P31/22 , A61P31/14
CPC分类号： A61K31/685
摘要： Provided are compounds, methods and pharmaceutical compositions for treating a host, especially a human, infected with a togavirus, herpes virus and/or coronavirus, and in particular SARS-CoV, cytomegalovirus or varicella-zoster virus. The method in one embodiment comprises administering to that host an effective amount of an anti-togavirus, anti-herpes virus and/or anti-coronavirus phospholipid or a pharmaceutically acceptable salt or prodrug thereof. The phospholipid compound is, e.g., a 3-alkylamido-2-alkoxypropylphosphocholine compound or salt thereof. The compound may be administered alone or in combination and/or alternation with one or more other anti-viral agents.
摘要翻译：提供用于治疗感染披膜病毒，疱疹病毒和/或冠状病毒，特别是SARS-CoV，巨细胞病毒或水痘带状疱疹病毒的宿主，特别是人的化合物，方法和药物组合物。在一个实施方案中的方法包括向该宿主施用有效量的抗披叶病毒，抗疱疹病毒和/或抗冠状病毒磷脂或其药学上可接受的盐或前药。磷脂化合物是例如3-烷基酰胺基-2-烷氧基丙基磷酰胆碱化合物或其盐。化合物可以单独施用或与一种或多种其它抗病毒剂组合和/或替代施用。

2. 发明申请

US20100184718A1 Compositions and Methods for Double-Targeting Virus Infections and Targeting Cancer Cells 有权
标题翻译：双重靶向病毒感染和靶向癌细胞的组合物和方法
公开(公告)号：US20100184718A1
公开(公告)日：2010-07-22
申请号：US12629387
申请日：2009-12-02
申请人： Louis S. KUCERA , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
发明人： Louis S. KUCERA , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
IPC分类号： A61K31/7072 , C07F9/06 , A61K31/661 , C07H19/048 , A61P31/12 , A61P35/00
CPC分类号： C07H19/06 , A61K31/66 , A61K31/675 , C07F9/10 , C07H19/10 , C07H19/16 , Y02A50/463
摘要： The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
摘要翻译：本发明包括通过双重靶向病毒（即在病毒生命周期的多于一个阶段靶向病毒）并因此抑制病毒复制而用于治疗哺乳动物病毒感染的组合物和方法。本发明的组合物包括包含与一种或多种抗病毒剂（例如核苷类似物，蛋白酶抑制剂等）共价结合到脂质主链的磷酸胆碱部分的化合物。本发明还包括用于治疗哺乳动物病毒感染的药物组合物和试剂盒。本发明的方法包括将治疗感染的本发明化合物，其药学上可接受的盐或本发明的药物组合物给予感染病毒的哺乳动物。另外，本发明包括可用于对抗哺乳动物中的癌症并促进治疗剂递送至哺乳动物细胞的组合物和方法。本发明的组合物包括包含与抗癌剂（例如核苷类似物）共价缀合的烷基脂质或磷脂部分的化合物。本发明还包括用于对抗癌症并促进治疗剂递送至哺乳动物细胞的药物组合物和试剂盒。本发明的方法包括给予本发明的化合物，其药学上可接受的盐或本发明的药物组合物，其量有效地抵抗癌症或促进治疗剂递送至哺乳动物细胞。

3. 发明授权

US06670341B1 Compositions and methods for double-targeting virus infections and targeting cancer cells 有权
标题翻译：用于双向靶向病毒感染和靶向癌细胞的组合物和方法
公开(公告)号：US06670341B1
公开(公告)日：2003-12-30
申请号：US09693658
申请日：2000-10-19
申请人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
发明人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
IPC分类号： A61K3166
CPC分类号： C07H19/06 , A61K31/66 , A61K31/675 , C07F9/10 , C07H19/10 , C07H19/16 , Y02A50/463
摘要： The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
摘要翻译：本发明包括通过双重靶向病毒（即在病毒生命周期的多于一个阶段靶向病毒）并因此抑制病毒复制而用于治疗哺乳动物病毒感染的组合物和方法。本发明的组合物包括包含与一种或多种抗病毒剂（例如核苷类似物，蛋白酶抑制剂等）共价结合到脂质主链的磷酸胆碱部分的化合物。本发明还包括用于治疗哺乳动物病毒感染的药物组合物和试剂盒。本发明的方法包括将治疗感染的本发明化合物，其药学上可接受的盐或本发明的药物组合物给予感染病毒的哺乳动物。另外，本发明包括可用于对抗哺乳动物中的癌症并促进治疗剂递送至哺乳动物细胞的组合物和方法。本发明的组合物包括包含与抗癌剂（例如核苷类似物）共价缀合的烷基脂质或磷脂部分的化合物。本发明还包括用于对抗癌症并促进治疗剂递送至哺乳动物细胞的药物组合物和试剂盒。本发明的方法包括给予本发明的化合物，其药学上可接受的盐或本发明的药物组合物，其量可以有效地抵抗癌症或促进治疗剂递送至哺乳动物细胞。

4. 发明授权

US07309696B2 Compositions and methods for targeting cancer cells 有权
标题翻译：用于靶向癌细胞的组合物和方法
公开(公告)号：US07309696B2
公开(公告)日：2007-12-18
申请号：US10748738
申请日：2003-12-30
申请人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
发明人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00 , C07H19/048
CPC分类号： C07H19/06 , A61K31/66 , A61K31/675 , C07F9/10 , C07H19/10 , C07H19/16 , Y02A50/463
摘要： The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
摘要翻译：本发明包括通过双重靶向病毒（即在病毒生命周期的多于一个阶段靶向病毒）并因此抑制病毒复制而用于治疗哺乳动物病毒感染的组合物和方法。本发明的组合物包括包含与一种或多种抗病毒剂（例如核苷类似物，蛋白酶抑制剂等）共价结合到脂质主链的磷酸胆碱部分的化合物。本发明还包括用于治疗哺乳动物病毒感染的药物组合物和试剂盒。本发明的方法包括将治疗感染的本发明化合物，其药学上可接受的盐或本发明的药物组合物给予感染病毒的哺乳动物。另外，本发明包括可用于对抗哺乳动物中的癌症并促进治疗剂递送至哺乳动物细胞的组合物和方法。本发明的组合物包括包含与抗癌剂（例如核苷类似物）共价缀合的烷基脂质或磷脂部分的化合物。本发明还包括用于对抗癌症并促进治疗剂递送至哺乳动物细胞的药物组合物和试剂盒。本发明的方法包括给予本发明的化合物，其药学上可接受的盐或本发明的药物组合物，其量有效地抵抗癌症或促进治疗剂递送至哺乳动物细胞。

5. 发明授权

US07026469B2 Compositions and methods of double-targeting virus infections and cancer cells 有权
公开(公告)号：US07026469B2
公开(公告)日：2006-04-11
申请号：US09844201
申请日：2001-04-27
申请人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
发明人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
IPC分类号： C07H17/00 , A61K31/70
CPC分类号： C07H19/06 , A61K31/66 , A61K31/675 , C07F9/10 , C07H19/10 , C07H19/16 , Y02A50/463
摘要： The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds, which comprise a phosphocholine moiety covalently conjugated with one or more therapeutic agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds, which comprise an alkyl lipid or phospholipid moiety covalently conjugated with a therapeutic agent (e.g., a nucleoside analogue). The invention also includes pharmaceutical compositions for combating cancer and facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.

6. 发明授权

US07638528B2 Compositions and methods for targeting cancer cells 有权
标题翻译：用于靶向癌细胞的组合物和方法
公开(公告)号：US07638528B2
公开(公告)日：2009-12-29
申请号：US11398529
申请日：2006-04-06
申请人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
发明人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07H19/06 , A61K31/66 , A61K31/675 , C07F9/10 , C07H19/10 , C07H19/16 , Y02A50/463
摘要： The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
摘要翻译：本发明包括通过双重靶向病毒（即在病毒生命周期的多于一个阶段靶向病毒）并因此抑制病毒复制而用于治疗哺乳动物病毒感染的组合物和方法。本发明的组合物包括包含与一种或多种抗病毒剂（例如核苷类似物，蛋白酶抑制剂等）共价结合到脂质主链的磷酸胆碱部分的化合物。本发明还包括用于治疗哺乳动物病毒感染的药物组合物和试剂盒。本发明的方法包括将治疗感染的本发明化合物，其药学上可接受的盐或本发明的药物组合物给予感染病毒的哺乳动物。另外，本发明包括可用于对抗哺乳动物中的癌症并促进治疗剂递送至哺乳动物细胞的组合物和方法。本发明的组合物包括包含与抗癌剂（例如核苷类似物）共价缀合的烷基脂质或磷脂部分的化合物。本发明还包括用于对抗癌症并促进治疗剂递送至哺乳动物细胞的药物组合物和试剂盒。本发明的方法包括给予本发明的化合物，其药学上可接受的盐或本发明的药物组合物，其量有效地抵抗癌症或促进治疗剂递送至哺乳动物细胞。

7. 发明授权

US08138200B2 Compositions and methods for double-targeting virus infections and targeting cancer cells 有权
标题翻译：用于双向靶向病毒感染和靶向癌细胞的组合物和方法
公开(公告)号：US08138200B2
公开(公告)日：2012-03-20
申请号：US12629387
申请日：2009-12-02
申请人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
发明人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07H19/06 , A61K31/66 , A61K31/675 , C07F9/10 , C07H19/10 , C07H19/16 , Y02A50/463
摘要： The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
摘要翻译：本发明包括通过双重靶向病毒（即在病毒生命周期的多于一个阶段靶向病毒）并因此抑制病毒复制而用于治疗哺乳动物病毒感染的组合物和方法。本发明的组合物包括包含与一种或多种抗病毒剂（例如核苷类似物，蛋白酶抑制剂等）共价结合到脂质主链的磷酸胆碱部分的化合物。本发明还包括用于治疗哺乳动物病毒感染的药物组合物和试剂盒。本发明的方法包括将治疗感染的本发明化合物，其药学上可接受的盐或本发明的药物组合物给予感染病毒的哺乳动物。另外，本发明包括可用于对抗哺乳动物中的癌症并促进治疗剂递送至哺乳动物细胞的组合物和方法。本发明的组合物包括包含与抗癌剂（例如核苷类似物）共价缀合的烷基脂质或磷脂部分的化合物。本发明还包括用于对抗癌症并促进治疗剂递送至哺乳动物细胞的药物组合物和试剂盒。本发明的方法包括给予本发明的化合物，其药学上可接受的盐或本发明的药物组合物，其量有效地抵抗癌症或促进治疗剂递送至哺乳动物细胞。

8. 发明授权

US07294619B2 Lipid analogs for inhibiting the activity of hepatitis B antigen 失效
公开(公告)号：US07294619B2
公开(公告)日：2007-11-13
申请号：US11588308
申请日：2006-10-27
申请人： Louis S. Kucera , Susan L. Morris-Natschke , Khalid S. Ishaq
发明人： Louis S. Kucera , Susan L. Morris-Natschke , Khalid S. Ishaq
IPC分类号： A61P31/20 , A61K31/685
CPC分类号： C07F9/10 , A61K31/685 , A61K31/7072 , A61K31/7076 , C07F9/091 , C07F9/106 , C07F9/117 , C07F9/65586 , C07F9/65616 , C07H19/10 , C07H19/20
摘要： The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the activity of the viral infection.

9. 发明授权

US07294621B2 Lipid analogs for combating tumors 失效
标题翻译：用于对抗肿瘤的脂质类似物
公开(公告)号：US07294621B2
公开(公告)日：2007-11-13
申请号：US11588313
申请日：2006-10-27
申请人： Louis S. Kucera , Susan L. Morris-Natschke , Khalid S. Ishaq
发明人： Louis S. Kucera , Susan L. Morris-Natschke , Khalid S. Ishaq
IPC分类号： A61P35/00 , A61K31/685
CPC分类号： A61K31/685 , A61K31/675 , A61K31/7072 , A61K31/7076 , C07F9/091 , C07F9/10 , C07F9/106 , C07F9/117 , C07F9/65586 , C07F9/65616 , C07H19/10 , C07H19/20
摘要： The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the activity of the viral infection.
摘要翻译：本发明涉及治疗病毒感染，特别是乙型肝炎病毒的方法。该方法包括向需要这种治疗的受试者施用感染控制量的磷脂或磷脂衍生物以抑制病毒感染的活性。

10. 发明申请

US20080293667A1 Lipid analogs for combating tumors 失效
标题翻译：用于对抗肿瘤的脂质类似物
公开(公告)号：US20080293667A1
公开(公告)日：2008-11-27
申请号：US11980819
申请日：2007-10-31
申请人： Louis S. Kucera , Susan L. Morris-Natschke , Khalid S. Ishaq
发明人： Louis S. Kucera , Susan L. Morris-Natschke , Khalid S. Ishaq
IPC分类号： A61K31/661 , A61P31/12 , A61K31/7076 , A61K31/7064 , C07F9/06 , C07H19/20 , C07H19/10 , A61P35/00
CPC分类号： A61K31/685 , A61K31/675 , A61K31/7072 , A61K31/7076 , C07F9/091 , C07F9/10 , C07F9/106 , C07F9/117 , C07F9/65586 , C07F9/65616 , C07H19/10 , C07H19/20
摘要： The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the activity of the viral infection.
摘要翻译：本发明涉及治疗病毒感染，特别是乙型肝炎病毒的方法。该方法包括向需要这种治疗的受试者施用感染控制量的磷脂或磷脂衍生物以抑制病毒感染的活性。

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