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1. 发明授权

US4904770A Production of 2',3'-dideoxy-2',3'-didehydronucleosides 失效
标题翻译： 2'，3'-二脱氧-2'，3'-二脱氢核苷的生产
公开(公告)号：US4904770A
公开(公告)日：1990-02-27
申请号：US173473
申请日：1988-03-24
申请人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
发明人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
IPC分类号： C07D405/04 , C07H19/04 , C07H19/073
CPC分类号： C07D405/04 , C07H19/04
摘要： There are disclosed novel processes for producing 2',3'-dideoxy-2'3'-didehydronucleosides, for example, 2',3'-dideoxy-2',3'-didehydrothymidine in high yields and on a large scale. The compounds so-produced are useful as antiviral agents, especially as agents effective against the human immunodeficiency viruses (HIV).

2. 发明授权

US5130421A Production of 2',3'-dideoxy-2',3'-didehydronucleosides 失效
标题翻译： 2'，3'-二脱氧-2'，3'-二脱氢核苷的生产
公开(公告)号：US5130421A
公开(公告)日：1992-07-14
申请号：US697512
申请日：1991-04-29
申请人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
发明人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
IPC分类号： C07D405/04 , C07H19/04
CPC分类号： C07D405/04 , C07H19/04
摘要： There are disclosed novel processes for producing 2',3'-dideoxy-2'3'-didehydronucleosides, for example, 2',3'-dideoxy-2',3'-didehydrothymidine in high yields and on a large scale. The compounds so-produced are useful as antiviral agents, especially as agents effective against the human immunodeficiency viruses (HIV).
摘要翻译：公开了以高产率和大规模生产2'，3'-二脱氧-2'3'-二脱氢核苷，例如2'，3'-二脱氧-2'，3'-二脱氢胸苷的新方法。如此制备的化合物可用作抗病毒剂，特别是作为有效抵抗人类免疫缺陷病毒（HIV）的药剂。

3. 发明授权

US5212294A Production of 2',3'-dideoxy-2',3'-didehydronucleosides 失效
标题翻译： 2'，3'-二脱氧-2'，3'-二脱氢核苷的生产
公开(公告)号：US5212294A
公开(公告)日：1993-05-18
申请号：US860938
申请日：1992-03-31
申请人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
发明人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
IPC分类号： C07D405/04 , C07H19/04
CPC分类号： C07D405/04 , C07H19/04
摘要： There are disclosed novel processes for producing 2',3'-dideoxy-2'3'-didehydronucleosides, for example, 2',3'-dideoxy-2',3'-didehydrothymidine in high yields and on a large scale. The compounds so-produced are useful as antiviral agents, especially as agents effective against the human immunodeficiency viruses (HIV).
摘要翻译：公开了以高产率和大规模生产2'，3'-二脱氧-2'3'-二脱氢核苷，例如2'，3'-二脱氧-2'，3'-二脱氢胸苷的新方法。如此制备的化合物可用作抗病毒剂，特别是作为有效抵抗人类免疫缺陷病毒（HIV）的药剂。

4. 发明授权

US5792756A Prodrugs of phosphonates 失效
标题翻译：膦酸盐的前药
公开(公告)号：US5792756A
公开(公告)日：1998-08-11
申请号：US481715
申请日：1995-06-07
申请人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , David R. Tortolani , Joanne J. Bronson
发明人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , David R. Tortolani , Joanne J. Bronson
IPC分类号： A61K31/675 , A61K31/66 , A61K31/70 , A61P31/12 , A61P35/00 , C07F9/6512 , C07F9/6561 , C07F9/6571 , C07F9/6574 , C07F9/6584 , C07H13/10 , C07H19/10 , C07H19/20 , C07F9/02
CPC分类号： C07F9/65742 , C07F9/65121 , C07F9/65616 , C07F9/657181 , C07F9/6584
摘要： There are disclosed novel oral prodrugs of phosphonate nucleotide analogs which are hydrolyzable under physiological conditions to yield compounds which are useful as antiviral agents, especially as agents effective against RNA and DNA viruses. They may also find use as antitumor agents.
摘要翻译：公开了在生理条件下可水解的新型口服前药的膦酸酯核苷酸类似物，以产生可用作抗病毒剂的化合物，特别是作为对RNA和DNA病毒有效的试剂。它们也可以用作抗肿瘤剂。

5. 发明授权

US5663159A Prodrugs of phosphonates 失效
标题翻译：膦酸盐的前药
公开(公告)号：US5663159A
公开(公告)日：1997-09-02
申请号：US320632
申请日：1994-10-11
申请人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , David R. Tortolani , Joanne J. Bronson
发明人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , David R. Tortolani , Joanne J. Bronson
IPC分类号： A61K31/675 , A61K31/66 , A61K31/70 , A61P31/12 , A61P35/00 , C07F9/6512 , C07F9/6561 , C07F9/6571 , C07F9/6574 , C07F9/6584 , C07H13/10 , C07H19/10 , C07H19/20
CPC分类号： C07F9/65742 , C07F9/65121 , C07F9/65616 , C07F9/657181 , C07F9/6584
摘要： There are disclosed novel oral prodrugs of phosphonate nucleotide analogs which are hydrolyzable under physiological conditions to yield compounds which are useful as antiviral agents, especially as agents effective against RNA and DNA viruses. They may also find use as antitumor agents.
摘要翻译：公开了在生理条件下可水解的新型口服前药的膦酸酯核苷酸类似物，以产生可用作抗病毒剂的化合物，特别是作为对RNA和DNA病毒有效的试剂。它们也可以用作抗肿瘤剂。

6. 发明授权

US5744600A Phosphonomethoxy carbocyclic nucleosides and nucleotides 失效
标题翻译：膦基甲氧基碳环核苷酸和核苷酸
公开(公告)号：US5744600A
公开(公告)日：1998-04-28
申请号：US357561
申请日：1994-12-16
申请人： Muzammil M. Mansuri , John C. Martin , Thomas W. Hudyma , Joanne J. Bronson , Louis M. Ferrara
发明人： Muzammil M. Mansuri , John C. Martin , Thomas W. Hudyma , Joanne J. Bronson , Louis M. Ferrara
IPC分类号： C07F9/6512 , A61K31/675 , C07F9/6561 , C07D473/18 , C07D473/34
CPC分类号： C07F9/65121
摘要： A compound of the Formula I or Formula II ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, hydroxy, chlorine, fluorine, bromine, or an organic substituent having 1 to 5 carbon atoms and selected from acyloxy having a hydrocarbon stem of 1 to 4 carbon atoms, alkoxy, alkylthio, amino, alkylamino and dialkylamino; R.sup.3 and R.sup.4 are independently hydrogen, or organic phosphonic ester substituents having 1 to 12 carbon atoms and selected from alkyl, alkenyl, aryl, and aralkyl; and B is a heterocyclic group selected from the group consisting of pyrimidine, purine, triazine, deazapurine, and triazole, attached through a ring nitrogen atom thereof optionally substituted with 1 to 3 substituents selected from the group consisting of hydroxy, mercapto, amino, hydrazino, fluoro, chloro, bromo, iodo, C.sub.1 to C.sub.3 alkyl, C2-C3 alkenyl, C2-C3 haloalkenyl, C1-C3 alkoxy, and C1-C3 alkylthio; and the pharmaceutically acceptable acid addition, metal, and amine salts thereof. The compositions of the invention are useful for, among other things, antiviral agents.
摘要翻译：式I或式II的化合物其中R 1和R 2独立地是氢，羟基，氯，氟，溴或具有1至5个碳原子并且选自具有烃的酰氧基的有机取代基 1至4个碳原子的烷氧基，烷硫基，氨基，烷基氨基和二烷基氨基; R3和R4独立地是氢，或具有1至12个碳原子并且选自烷基，烯基，芳基和芳烷基的有机膦酸酯取代基; 并且B是选自嘧啶，嘌呤，三嗪，脱氮嘌呤和三唑的杂环基，其通过环氮原子连接，任选被1-3个选自羟基，巯基，氨基，肼基的取代基取代，氟，氯，溴，碘，C 1至C 3烷基，C 2 -C 3烯基，C 2 -C 3卤代烯基，C 1 -C 3烷氧基和C 1 -C 3烷硫基; 及其药学上可接受的酸加成盐，金属盐和胺盐。本发明的组合物尤其可用于抗病毒剂。

7. 发明授权

US5218106A 2',3'-dideoxy-2'-fluoronucleosides 失效
标题翻译： 2'，3'-二脱氧-2'-氟核苷
公开(公告)号：US5218106A
公开(公告)日：1993-06-08
申请号：US857850
申请日：1992-03-26
申请人： Roman Z. Sterzycki , Muzammil M. Mansuri , John C. Martin
发明人： Roman Z. Sterzycki , Muzammil M. Mansuri , John C. Martin
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/04 , C07H19/056 , C07H19/06 , C07H19/16 , C07H19/19
CPC分类号： C07H19/06 , C07H19/04 , Y02P20/55
摘要： There are disclosed novel 2',3'-dideoxy-2'-fluoronucleosides and 2'-3'-dideoxy-2',3'-didehydro-2'-fluoronucleosides and processes for their preparation. The compounds so produced exhibit therapeutically useful antiviral and, more particularly, anti-HIV effects.
摘要翻译：公开了新的2'，3'-二脱氧-2'-氟核苷和2'-3'-二脱氧-2'，3'-二脱氢-2'-氟核苷及其制备方法。如此制备的化合物显示出治疗上有用的抗病毒，更具体地，抗HIV作用。

8. 发明授权

US5126506A 2',3'-Dideoxy-2'-fluoronucleosides 失效
标题翻译： 2'，3'-二脱氧-2'-氟核苷
公开(公告)号：US5126506A
公开(公告)日：1992-06-30
申请号：US581941
申请日：1990-09-13
申请人： Roman Z. Sterzycki , Muzammil M. Mansuri , John C. Martin
发明人： Roman Z. Sterzycki , Muzammil M. Mansuri , John C. Martin
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/04 , C07H19/056 , C07H19/06 , C07H19/16 , C07H19/19
CPC分类号： C07H19/06 , C07H19/04 , Y02P20/55
摘要： There are disclosed novel 2',3'-dideoxy-2'-fluoronucleosides and 2'-3'-dideoxy-2',3'-didehydro-2'-fluoronucleosides and processes for their preparation. The compounds so produced exhibit therapeutically useful antiviral and, more particularly, anti-HIV effects.
摘要翻译：公开了新的2'，3'-二脱氧-2'-氟核苷和2'- 3'-二脱氧-2'，3'-二脱氢-2'-氟核苷及其制备方法。如此制备的化合物显示出治疗有用的抗病毒，更具体地，抗HIV作用。

9. 发明授权

US4908440A 2',3'-dideoxy-2'-fluoroarabinopyrimidine nucleosides 失效
标题翻译： 2'，3'-二脱氧-2'-氟阿拉宾嘧啶核苷
公开(公告)号：US4908440A
公开(公告)日：1990-03-13
申请号：US120051
申请日：1987-11-12
申请人： Roman Z. Sterzycki , Muzammil M. Mansuri , John C. Martin
发明人： Roman Z. Sterzycki , Muzammil M. Mansuri , John C. Martin
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/04 , C07H19/056 , C07H19/06 , C07H19/16 , C07H19/19
CPC分类号： C07H19/06 , C07H19/04 , Y02P20/55
摘要： There are disclosed novel 2',3'-dideoxy-2'-fluoronucleosides and 2'-3'-dideoxy-2',3'-didehydro-2'-fluoronucleosides and processes for their preparation. The compounds so produced exhibit therapeutically useful antiviral and, more particularly, anti-HIV effects.

10. 发明授权

US4973677A 2',3'-dideoxy-2',3'-didehydro-2'-fluoroarabino-nucleosides 失效
标题翻译： 2'，3'-二脱氧-2'，3'-二脱氢-2'-氟代氨基 - 核苷
公开(公告)号：US4973677A
公开(公告)日：1990-11-27
申请号：US378331
申请日：1989-07-11
申请人： Roman Z. Sterzycki , Muzammil M. Mansuri , John C. Martin
发明人： Roman Z. Sterzycki , Muzammil M. Mansuri , John C. Martin
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/04 , C07H19/056 , C07H19/06 , C07H19/16 , C07H19/19
CPC分类号： C07H19/06 , C07H19/04 , Y02P20/55
摘要： There are disclosed novel 2',3'-dideoxy-2'-fluoronucleosides and 2'-3'-dideoxy-2',3'-didehydro-2'-fluoronucleosides and processes for their preparation. The compounds so produced exhibit therapeutically useful antiviral and, more particularly, anti-HIV effects.
摘要翻译：公开了新的2'，3'-二脱氧-2'-氟核苷和2'-3'-二脱氧-2'，3'-二脱氢-2'-氟核苷及其制备方法。如此制备的化合物显示出治疗上有用的抗病毒，更具体地，抗HIV作用。

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