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公开(公告)号：US5629454A
公开(公告)日：1997-05-13
申请号：US311425
申请日：1994-09-23
申请人： Victor E. Marquez , Juan B. Rodriguez , Marc C. Nicklaus , Joseph J. Barchi, Jr. , Maqbool A. Siddiqui
发明人： Victor E. Marquez , Juan B. Rodriguez , Marc C. Nicklaus , Joseph J. Barchi, Jr. , Maqbool A. Siddiqui
IPC分类号： C07D239/26 , A61K31/70 , A61K31/7088 , A61P31/18 , C07D239/46 , C07D239/54 , C07D473/18 , C07D473/34 , C07H19/04 , C07H21/00 , C07C49/172 , C07C41/06 , C07C43/196
CPC分类号： C07D239/47 , C07D239/54 , C07D473/18 , C07D473/34 , C07H19/04 , C07H21/00
摘要： Conformationally locked 4',6'-cyclopropane-fused carbocyclic nucleoside analogues. The compounds are prepared by condensing a cyclopropane-fused carbocyclic allylic alcohol with substituted purine or pyrimidine bases. The condensation products are then modified to produce the adenosine, guanosine, cytidine, thymidine and uracil nucleoside analogues. The compounds are therapeutically useful as antimetabolites, or in the preparation of anti-metabolic agents.
摘要翻译： 构象锁定的4'，6'-环丙烷稠合的碳环核苷类似物。 通过将环丙烷稠合的碳环烯丙醇与取代的嘌呤或嘧啶碱缩合来制备化合物。 然后对缩合产物进行改性以产生腺苷，鸟苷，胞苷，胸苷和尿嘧啶核苷类似物。 该化合物在治疗上可用作抗代谢物，或用于制备抗代谢药物。
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公开(公告)号：US5869666A
公开(公告)日：1999-02-09
申请号：US818563
申请日：1997-03-14
申请人： Victor E. Marquez , Juan B. Rodriguez , Marc C. Nicklaus , Joseph J. Barchi, Jr. , Maqbool A. Siddiqui
发明人： Victor E. Marquez , Juan B. Rodriguez , Marc C. Nicklaus , Joseph J. Barchi, Jr. , Maqbool A. Siddiqui
IPC分类号： C07D239/26 , A61K31/70 , A61K31/7088 , A61P31/18 , C07D239/46 , C07D239/54 , C07D473/18 , C07D473/34 , C07H19/04 , C07H21/00 , C07D239/47
CPC分类号： C07D239/47 , C07D239/54 , C07D473/18 , C07D473/34 , C07H19/04 , C07H21/00
摘要： Conformationally locked 4',6'-cyclopropane-fused carboxylic nucleoside analogues. The compounds are prepared by condensing a cyclopropane-fused carbocyclic allylic alcohol with substituted purine or pyrimidine bases. The condensation products are then modified to produce the adenosine, guanosine, cytidine, thymidine, and uracil nucleoside analogues. The compounds are therapeutically useful as antimetabolites, or in the preparation of anti-metabolic agents.
摘要翻译： 构象锁定的4'，6'-环丙烷稠合的羧基核苷类似物。 通过将环丙烷稠合的碳环烯丙醇与取代的嘌呤或嘧啶碱缩合来制备化合物。 然后对缩合产物进行改性以产生腺苷，鸟苷，胞苷，胸苷和尿嘧啶核苷类似物。 该化合物在治疗上可用作抗代谢物，或用于制备抗代谢药物。
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3.发明授权公开(公告)号：US08513214B2
公开(公告)日：2013-08-20
申请号：US12741873
申请日：2008-11-10
IPC分类号： A01N43/04 , A61K31/70 , C07H19/16 , C07H19/167 , C07H19/173 , C12Q1/70
CPC分类号： C07D473/34 , C07H19/16
摘要： The invention provides for novel 2-Deoxyadenosine compounds, which can treat HIV infection at low cytotoxicity values. Substitution at the 4′-position provided compounds which demonstrated low cytotoxicity values in an ATP-based cytotoxicity assay.
摘要翻译： 本发明提供新的2-脱氧腺苷化合物，其可以以低细胞毒性值治疗HIV感染。 在4'-位上的取代提供了在基于ATP的细胞毒性测定中证实低细胞毒性值的化合物。
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4.发明申请公开(公告)号：US20110190226A1
公开(公告)日：2011-08-04
申请号：US12741873
申请日：2008-11-10
CPC分类号： C07D473/34 , C07H19/16
摘要： The invention provides for novel 2-Deoxyadenosine compounds, which can treat HIV infection at low cytotoxicity values. Substitution at the 4′-position provided compounds which demonstrated low cytotoxicity values in an ATP-based cytotoxicity assay.
摘要翻译： 本发明提供新的2-脱氧腺苷化合物，其可以以低细胞毒性值治疗HIV感染。 在4'-位上的取代提供了在基于ATP的细胞毒性测定中证实低细胞毒性值的化合物。
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5.发明授权2'-fluorofuranosyl derivatives and novel method of preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides 失效2'-氟代呋喃糖苷衍生物和制备2'-氟嘧啶和2'-氟嘌呤核苷的新方法
公开(公告)号：US5336764A
公开(公告)日：1994-08-09
申请号：US968567
申请日：1992-10-29
IPC分类号： C07H1/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7076 , A61P31/12 , A61P31/18 , C07H13/08 , C07H15/04 , C07H15/203 , C07H19/06 , C07H19/10 , C07H19/16 , C07H23/00 , C07G3/00
摘要： A compound has the formula ##STR1## wherein R is selected from the group consisting of (C.sub.7 -C.sub.20)aroyl, (C.sub.6 -C.sub.20)aryl, aralkyl and alkylaryl, and (C.sub.1 -C.sub.10)alkyl-di(C.sub.6 -C.sub.20)aryl Si, R' is selected from the group consisting of (C.sub.1 -C.sub.10)alkyl, (C.sub.7 -C.sub.20)aroyl and (C.sub.2 -C.sub.12)acyl, all of which may be further substituted with O, S, N or alkyl, and R'" is selected from the group consisting of halogen, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.10)acyloxy, O-methane-sulfonyl and O-p-toluenesulfonyl. A composition of matter comprises 0.001 to 99.999 wt % of the above compound.
摘要翻译： 化合物具有下式（IMAGE），其中R选自（C 7 -C 20）芳酰基，（C 6 -C 20）芳基，芳烷基和烷芳基，和（C 1 -C 10）烷基 - 二（C 6 -C 20）芳基 Si，R'选自（C 1 -C 10）烷基，（C 7 -C 20）芳酰基和（C 2 -C 12）酰基，所有这些可以进一步被O，S，N或烷基取代，R “选自卤素，（C 1 -C 10）烷氧基，（C 1 -C 10）酰氧基，O-甲磺酰基和对甲苯磺酰基。 物质组合物含有0.001〜99.999重量％的上述化合物。
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