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1. 发明申请

US20080020010A1 Pyridinone diketo acids: inhibitors of HIV replication 有权
标题翻译：吡啶酮二酮酸：HIV复制抑制剂
公开(公告)号：US20080020010A1
公开(公告)日：2008-01-24
申请号：US11827959
申请日：2007-07-13
申请人： Vasu Nair , Byung I. Seo , Vinod R. Uchil
发明人： Vasu Nair , Byung I. Seo , Vinod R. Uchil
IPC分类号： A61K31/4412 , A61K9/02 , A61K9/72 , A61P31/18 , C07D211/86
CPC分类号： C07D213/64 , C07D213/68
摘要： A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other integrase-based anti-HIV agents). Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
摘要翻译：描述了在吡啶酮支架上构建的一类新的二酮酸，其通过抑制HIV整合酶设计为HIV复制的抑制剂。这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素联合使用，疫苗和其他治疗剂，特别是其它抗HIV化合物（包括其它基于整合酶的抗HIV药物）。还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。

2. 发明授权

US07888375B2 Pyridinone diketo acids: inhibitors of HIV replication 有权
标题翻译：吡啶酮二酮酸：HIV复制抑制剂
公开(公告)号：US07888375B2
公开(公告)日：2011-02-15
申请号：US11827959
申请日：2007-07-13
申请人： Vasu Nair , Byung I. Seo , Vinod R. Uchil
发明人： Vasu Nair , Byung I. Seo , Vinod R. Uchil
IPC分类号： A61K31/44 , C07D211/86
CPC分类号： C07D213/64 , C07D213/68
摘要： A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other integrase-based anti-HIV agents). Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
摘要翻译：描述了在吡啶酮支架上构建的一类新的二酮酸，其通过抑制HIV整合酶被设计为HIV复制的抑制剂。这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素联合使用，疫苗和其他治疗剂，特别是其它抗HIV化合物（包括其它基于整合酶的抗HIV药物）。还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。

3. 发明申请

US20100092427A1 Pyridinone Diketo Acids: Inhibitors of HIV Replication in Combination Therapy 审中-公开
标题翻译：吡啶酮二酮酸：联合治疗HIV复制抑制剂
公开(公告)号：US20100092427A1
公开(公告)日：2010-04-15
申请号：US12309017
申请日：2007-07-13
申请人： Vasu Nair , Byung I. Seo , Vinod R. Uchil , Guochen Chi
发明人： Vasu Nair , Byung I. Seo , Vinod R. Uchil , Guochen Chi
IPC分类号： A61K31/4412 , C07D213/64 , A61K38/21 , A61K39/395 , A61P31/18
CPC分类号： C07D213/64 , C07D213/68
摘要： A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HTV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described. Compounds of the present application include those of formula I and include tautomers, regioisomers, geometric isomers, and pharmaceutically acceptable salts thereof, wherein the pyridinone scaffold and R groups are as otherwise defined in the specification. These are combined, with any number of typical other anti-HIV agents (including other integrase-based anti-HIV agents) and other combination therapeutic agents described herein, to provide an effective treatment modality for HIV infections, including AIDS and ARC.
摘要翻译：描述了在吡啶酮支架上构建的一类新的二酮酸，其通过抑制HIV整合酶设计为HTV复制的抑制剂。这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素联合使用，疫苗和其他治疗剂，特别是可用于产生组合抗HIV鸡尾酒的其它抗HIV化合物（包括其它抗HIV整合酶试剂）。还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。本申请的化合物包括式I的化合物，并且包括互变异构体，区域异构体，几何异构体及其药学上可接受的盐，其中吡啶酮支架和R基团如本说明书另有定义。将这些与任何数量的典型的其它抗HIV剂（包括其它基于整合酶的抗HIV剂）和本文所述的其它组合治疗剂组合起来，为HIV感染（包括AIDS和ARC）提供有效的治疗方式。

4. 发明授权

US07569573B2 Diketo acids with nucleobase scaffolds: anti-HIV replication inhibitors targeted at HIV integrase 失效
标题翻译：具有核碱基支架的二酮酸：靶向HIV整合酶的抗HIV复制抑制剂
公开(公告)号：US07569573B2
公开(公告)日：2009-08-04
申请号：US11820444
申请日：2007-06-19
申请人： Vasu Nair , Guochen Chi , Vinod R. Uchil
发明人： Vasu Nair , Guochen Chi , Vinod R. Uchil
IPC分类号： C07D473/28 , C07D473/36 , C07D473/40 , C07D473/00 , A61K31/52 , A61P31/18 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D419/04
CPC分类号： C07D473/30 , C07D239/54 , C07D473/00 , C07F9/6512 , C07F9/65616
摘要： A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
摘要翻译：描述了通过抑制HIV整合酶设计为抑制HIV复制的核碱基支架上构建的一类新的二酮酸。这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素联合使用，疫苗和其他治疗剂。还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。

5. 发明授权

US07250421B2 Diketo acids with nucleobase scaffolds: anti-HIV replication inhibitors targeted at HIV integrase 失效
标题翻译：具有核碱基支架的二酮酸：靶向HIV整合酶的抗HIV复制抑制剂
公开(公告)号：US07250421B2
公开(公告)日：2007-07-31
申请号：US11047229
申请日：2005-01-31
申请人： Vasu Nair , Guochen Chi , Vinod R. Uchil
发明人： Vasu Nair , Guochen Chi , Vinod R. Uchil
IPC分类号： C07D239/52 , A61K31/505 , A61K31/506 , A61P31/18 , C07D401/04 , C07D403/04 , C07D405/04 , C07D415/04 , C07D417/04 , C07D419/04
CPC分类号： C07D473/30 , C07D239/54 , C07D473/00 , C07F9/6512 , C07F9/65616
摘要： A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
摘要翻译：描述了通过抑制HIV整合酶设计为抑制HIV复制的核碱基支架上构建的一类新的二酮酸。这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素联合使用，疫苗和其他治疗剂。还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。

6. 发明授权

US4992427A 2-substituted inosines and their use as antiviral agents 失效
标题翻译： 2-取代的肌苷及其作为抗病毒剂的用途
公开(公告)号：US4992427A
公开(公告)日：1991-02-12
申请号：US366425
申请日：1989-06-15
申请人： Vasu Nair
发明人： Vasu Nair
IPC分类号： C07H19/16
CPC分类号： C07H19/16
摘要： Certain functionalized inosines, preferably C.sub.2 alkylated inosines, are prepared as new compounds having use as antiviral agents against viruses.
摘要翻译：某些官能化的肌苷，优选C2烷基化的肌苷被制备为具有用作抗病毒药物作为病毒的新化合物。

7. 发明申请

US20060172973A1 Diketo acids with nucleobase scaffolds: anti-HIV replication inhibitors targeted at HIV integrase 失效
公开(公告)号：US20060172973A1
公开(公告)日：2006-08-03
申请号：US11047229
申请日：2005-01-31
申请人： Vasu Nair , Guochen Chi , Vinod Uchil
发明人： Vasu Nair , Guochen Chi , Vinod Uchil
IPC分类号： A61K31/675 , C07F9/6512
CPC分类号： C07D473/30 , C07D239/54 , C07D473/00 , C07F9/6512 , C07F9/65616
摘要： A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.

8. 发明授权

US06316228B1 Efficient synthesis of nucleosides 失效
标题翻译：高效合成核苷
公开(公告)号：US06316228B1
公开(公告)日：2001-11-13
申请号：US09341473
申请日：1999-07-12
申请人： Vasu Nair , Suresh Pal
发明人： Vasu Nair , Suresh Pal
IPC分类号： C12P1938
CPC分类号： C12P19/38 , Y10S435/822 , Y10S435/832
摘要： Methods and compositions, including cell cultures, for producing nucleosides are provided which comprise contacting a nucleoside precursor and a sugar moiety donor with a cell containing a nucleoside phosphorylase. The nucleoside precursor can be a purine or pyrimidine base and the sugar moiety donor can comprise a ribose, a deoxyribose, including 2-deoxyribose, or other sugar of choice. The methods and composition can be used to make thymidine from thymine and 2-deoxyinosine or 2′-deoxyadenosine. Other nucleosides, including those having anticancer and/or antiviral properties, also can be obtained according to the invention.
摘要翻译：提供了用于产生核苷的方法和组合物，包括细胞培养物，其包括使核苷前体和糖部分供体与含有核苷磷酸化酶的细胞接触。核苷前体可以是嘌呤或嘧啶碱基，糖部分供体可以包含核糖，脱氧核糖，包括2-脱氧核糖，或其它选择的糖。方法和组成可用于制备胸腺嘧啶和2-脱氧肌苷或2'-脱氧腺苷的胸苷。还可以根据本发明获得其它核苷，包括具有抗癌和/或抗病毒性质的核苷。

9. 发明授权

US5013829A Stable congener of 2',3'-dideoxyadenosine 失效
标题翻译： 2'，3'-双脱氧腺苷的稳定同源物
公开(公告)号：US5013829A
公开(公告)日：1991-05-07
申请号：US343334
申请日：1989-04-26
申请人： Vasu Nair , Greg S. Buenger
发明人： Vasu Nair , Greg S. Buenger
IPC分类号： C07D473/00 , C07H19/16
CPC分类号： C07D473/00 , C07H19/16
摘要： The preseent invention is concerned with congeners of 2',3'-dideoxyadenosine (ddA) with modifications at the 2- and 8- positions to increase stability of the compounds from the standpoint of resistance to deamination and hydrolytic cleavage of the glycosidic bond.
摘要翻译：本发明涉及2'，3'-二脱氧腺苷（ddA）的同源物，其在2-和8-位上具有修饰，以提高化合物的稳定性，从耐脱氨基和糖苷键的水解切割的观点出发。

10. 发明授权

US08703801B2 Pyridinone hydroxycyclopentyl carboxamides: HIV integrase inhibitors with therapeutic applications 有权
标题翻译：吡啶酮羟基环戊基甲酰胺：具有治疗应用的HIV整合酶抑制剂
公开(公告)号：US08703801B2
公开(公告)日：2014-04-22
申请号：US13513448
申请日：2010-12-07
申请人： Vasu Nair , Maurice O. Okello , Abdumalik A. Nishonov , Sanjaykumar Mishra
发明人： Vasu Nair , Maurice O. Okello , Abdumalik A. Nishonov , Sanjaykumar Mishra
IPC分类号： C07D213/64 , C07D401/12 , A61K31/44
CPC分类号： C07D401/12 , A61K31/4412 , A61K31/4439 , C07D213/63
摘要： New chiral and achiral oxy-substituted cyclopentyl pyridinone diketocarboxamides and their derivatives and methods for their preparations are disclosed. The compounds include tautomers, regioisomers and geometric isomers. These complex carboxamides are designed as inhibitors of HIV replication through inhibition of HIV integrase. The compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
摘要翻译：公开了新的手性和非手性氧取代的环戊基吡啶酮二酮甲酰胺及其衍生物及其制备方法。化合物包括互变异构体，区域异构体和几何异构体。这些复合甲酰胺通过抑制HIV整合酶被设计为HIV复制的抑制剂。这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素组合使用，疫苗和其他治疗剂，特别是可用于产生组合抗HIV鸡尾酒的其它抗HIV化合物（包括其它抗HIV整合酶试剂）。还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。

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