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1. 发明授权

US4910310A Synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives 失效
标题翻译： N-取代的1,5-二脱氧-1,5-亚氨基-L-岩藻糖醇衍生物的合成
公开(公告)号：US4910310A
公开(公告)日：1990-03-20
申请号：US252846
申请日：1988-10-03
申请人： Arthur L. Campbell , James R. Behling , Kevin A. Babiak , John S. Ng , Richard A. Mueller , George W. J. Fleet
发明人： Arthur L. Campbell , James R. Behling , Kevin A. Babiak , John S. Ng , Richard A. Mueller , George W. J. Fleet
IPC分类号： C07D307/62 , C07C211/46 , C07D211/46 , C07D491/04 , C07D491/056 , C07D493/04 , C07H9/04
CPC分类号： C07D491/04 , C07D211/46
摘要： Novel intermediates and method for the chemical synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives are provided. A preferred intermediate is 1,5-dideoxy-1,5-imino-3, 4-O-isopropylidene-L-fucitol which is used to prepare the HIV inhibitor 1,5-dideoxy-1,5-imino-[N-.omega.-methyl caproate]-L-fucitol. These compounds are prepared in a short synthesis from the known compound 2,3-O-isopropylidene-D-lyxono-1,4-lactone or in a multi-step synthesis from D-galactose.

2. 发明授权

US5286877A Synthesis of 1,4-dideoxy-1,4-imino-L-arabinitol 失效
标题翻译： 1,4-二脱氧-1,4-亚氨基-L-阿拉伯糖醇的合成
公开(公告)号：US5286877A
公开(公告)日：1994-02-15
申请号：US12077
申请日：1993-02-01
申请人： James R. Behling , John R. Medich , Kevin A. Babiak , George W. J. Fleet
发明人： James R. Behling , John R. Medich , Kevin A. Babiak , George W. J. Fleet
IPC分类号： C07D207/12 , C07D319/06 , C07D407/04 , C07D491/04 , C07D493/04 , C07D207/24 , C07D207/36
CPC分类号： C07D407/04 , C07D207/12 , C07D319/06 , C07D491/04 , C07D493/04
摘要： 1,4-Dideoxy-1,4-imino-L-arabinitol is chemically synthesized from D-lyxonolactone by formation of the pyrrolidine ring by joining the nitrogen between C-1 and C-4 and inversion of configuration at both C-2 and C-4, with the C-3 and C-5 hydroxyl groups being protected throughout the synthesis sequence by benzylidenation. The product is preferably isolated as the hydrochloride salt and is useful as an inhibitor of .alpha.-glucosidase and human immunodeficiency virus (HIV).
摘要翻译： 1,4-二脱氧-1,4-亚氨基-L-阿拉伯糖醇由D-赖索内酯通过连接C-1和C-4之间的氮而形成吡咯烷环并在C-2和 C-4，其中C-3和C-5羟基通过亚苄基化在整个合成序列中被保护。该产物优选作为盐酸盐分离，并且可用作（α） - 葡糖苷酶和人类免疫缺陷病毒（HIV）的抑制剂。

3. 发明授权

US5096909A Fucosidase inhibitor 失效
标题翻译：岩藻糖苷酶抑制剂
公开(公告)号：US5096909A
公开(公告)日：1992-03-17
申请号：US600941
申请日：1990-10-22
申请人： George W. J. Fleet , Sung K. Namgoong
发明人： George W. J. Fleet , Sung K. Namgoong
IPC分类号： C07D211/46
CPC分类号： C07D211/46
摘要： The synthesis of the novel fucosidase inhibitor, 2,6-imino-2,6,7-trideoxy-D-glycero-D-gluco heptitol, is disclosed.
摘要翻译：公开了新型岩藻糖苷酶抑制剂2,6-亚氨基-2,6,7-三脱氧-D-甘油-D-葡糖七糖醇的合成。

4. 发明授权

US5068243A Bicyclic tetrahydroxypyrrolizidine 失效
标题翻译：双环四羟基吡咯烷啶
公开(公告)号：US5068243A
公开(公告)日：1991-11-26
申请号：US564009
申请日：1990-08-07
申请人： George W. J. Fleet
发明人： George W. J. Fleet
IPC分类号： C07D317/10 , C07D487/04 , C07D491/04 , C07D491/22 , C07D493/04 , C07F7/18
CPC分类号： C07D487/04 , C07D317/10 , C07D491/04 , C07D493/04 , C07F7/1856 , Y02P20/55
摘要： Novel bicyclic tetrahydroxylated pyrrolizidines are disclosed which are inhibitors of glycosidase enzymes. A preferred inhibitor is (1S,2R,6R,7S)-1,2,6,7-tetrahydroxypyrrolizidine. It is synthesized from D-glycero-D-talo-heptono-1,4-lactone and utilizes the novel intermediate compounds, 7-O-tert-butyldiphenylsilyl-2,3:5,6-di-O-isopropylidene-D- glycero-D-talo-heptono-1,4-lactone and (1S,2R,6R,7S)-1,2:6,7-di-O-isopropylidene-1,2,6,7-tetrahydroxypyrrolizidine, as follows:a) reacting D-glycero-D-talo-heptono-1,4-lactone with 2,2-dimethoxypropane to provide a fully protected lactone,b) selectively removing the acetonide group at C-6,7 to give a C-2,3 protected heptonolactone,c) reacting the C-2,3 protected lactone with a silyl blocking agent to protect the primary hydroxyl group and give a C-2,3,7 protected lactone,d) reacting the protected lactone with 2,2-dimethoxypropane to provide a fully protected lactone,e) reacting the fully protected lactone with fluoride ion to cleave at C7 and thereby provide access to nitrogen in the ring and give a primary alcohol,f) esterifying the primary alcohol with triflic anhydride to afford a triflate,g) reacting the triflate with azide ion to give an azidolactone,h) reducing the azidolactone to give an azidodiol,i) reacting the azidodiol with methanesulfonyl chloride to provide an axidodimesylate,j) catalytically hydrogenating the azidodimesylate in ethanol at ambient temperature,k) heating the resulting product in ethanol in the presence of sodium acetate to give a tetracyclic pyrrolizidine, andl) removing the acetonide protecting groups of the tetracyclic pyrrolizidine by acid hydrolysis to give (1S,2R,6R,7S)-1,2,6,7-tetrahydroxypyrrolizidine.
摘要翻译：公开了作为糖苷酶的抑制剂的新型二环四羟甲基化的吡咯烷子。优选的抑制剂是（1S，2R，6R，7S）-1,2,6,7-四羟基吡咯烷啶。由D-甘油基-D-庚内酰-1,4-内酯合成并利用新的中间体化合物7-O-叔丁基二苯基甲硅烷基-2,3：5,6-二-O-异亚丙基-D- 甘油基-D-庚内酰-1,4-内酯和（1S，2R，6R，7S）-1,2：6,7-二-O-异亚丙基-1,2,6,7-四羟基吡咯烷脒，为如下：a）使D-甘油基-D-庚内酰-1,4-内酯与2,2-二甲氧基丙烷反应，得到完全保护的内酯，b）选择性地除去C-6,7上的丙酮化合物，得到C -2,3保护的庚内酯，c）使C-2,3保护的内酯与甲硅烷基封闭剂反应以保护伯羟基并得到C-2,3,7保护的内酯，d）使保护的内酯与2 的2-二甲氧基丙烷，以提供完全保护的内酯，e）使完全保护的内酯与氟离子反应以在C7处裂解，从而提供进入环中的氮并获得伯醇，f）用三氟甲磺酸酯化伯醇得到三氟甲磺酸酯，g）使三氟甲磺酸酯反应用叠氮化物离子，得到叠氮内酯，h）还原叠氮内酯得到叠氮基二醇，i）叠氮二醇与甲磺酰氯反应，得到二硫代二季铵盐，j）在环境温度下催化氢化叠氮二季戊酸酯在乙醇中，k）加热得到的产物在乙酸乙酯中，在乙酸钠存在下反应，得到四环吡咯烷啶，并且l）通过酸水解除去四环吡咯烷子酮的丙酮化合物保护基，得到（1S，2R，6R，7S）-1,2,6,7-四羟基吡咯烷。

5. 发明授权

US4994572A Synthesis of nojirimycin derivatives 失效
标题翻译： nojirimycin衍生物的合成
公开(公告)号：US4994572A
公开(公告)日：1991-02-19
申请号：US420424
申请日：1989-10-12
申请人： George W. J. Fleet
发明人： George W. J. Fleet
IPC分类号： C07D211/46 , C07D211/76 , C07D307/33 , C07H9/04 , C07H15/18
CPC分类号： C07D307/33 , C07D211/46 , C07D211/76 , C07H15/18
摘要： Nojirimycin .delta.-lactam and deoxynojirimycin are each synthesized from 5,6-anhydro-3-O-benzyl-1,2-O-isopropylidene-L-idofuranose as a divergent intermediate by a method which comprises formation of the piperidine ring by connection of nitrogen between C-1 and C-5 with inversion of configuration at C-5 to form nojirimycin .delta.-lactam or between C-2 and C-6 with inversion of configuration at C-2.

6. 发明授权

US5089520A Method of inhibiting virus 失效
标题翻译：抑制病毒的方法
公开(公告)号：US5089520A
公开(公告)日：1992-02-18
申请号：US584982
申请日：1990-09-20
申请人： George W. J. Fleet , Thomas W. Rademacher , Raymond A. Dwek
发明人： George W. J. Fleet , Thomas W. Rademacher , Raymond A. Dwek
IPC分类号： A61K31/40 , A61K31/445 , C07D207/12 , C07D211/46 , C07D211/88
CPC分类号： A61K31/40 , A61K31/445 , C07D207/12 , C07D211/46 , C07D211/88
摘要： A group of five- and six-membered heterocyclic compounds having a nitrogen in the ring and 2 to 3 hydroxyl substituents on the ring are effective inhibitory agents of human immunodeficiency virus.
摘要翻译：一组在环中具有氮和环上2至3个羟基取代基的五元和六元杂环化合物是人类免疫缺陷病毒的有效抑制剂。

7. 发明授权

US5026870A Method of preparing bicyclic tetrahydroxylated pyrrolizidines 失效
标题翻译：制备双环四羟甲基化吡咯嗪的方法
公开(公告)号：US5026870A
公开(公告)日：1991-06-25
申请号：US587144
申请日：1990-09-24
申请人： George W. J. Fleet
发明人： George W. J. Fleet
IPC分类号： C07D317/10 , C07D491/04 , C07D491/22 , C07D493/04
CPC分类号： C07D491/04 , C07D317/10 , C07D493/04
摘要： Novel bicyclic tetrahydroxylated pyrrolizidines are disclosed which are inhibitors of glycosidase enzymes. A preferred inhibitor is 1.alpha.,2.alpha.,6.alpha.,7.alpha.,7.alpha..beta.-1,2,6-7-tetrahydroxypyrrolizidine. It is synthesized from D-glycero-D-gulo-heptono-1,4-lactone.
摘要翻译：公开了作为糖苷酶的抑制剂的新型二环四羟甲基化的吡咯烷子。优选的抑制剂是1α，2α，6α，7α，7αβ-1,2,6,7-四氢吡咯烷啶。由D-甘油基-D-庚内酰-1,4-内酯合成。

8. 发明授权

US5017704A Fucosidase inhibitor 失效
标题翻译：岩藻糖苷酶抑制剂
公开(公告)号：US5017704A
公开(公告)日：1991-05-21
申请号：US372415
申请日：1989-06-27
申请人： George W. J. Fleet , Sung K. Namgoong
发明人： George W. J. Fleet , Sung K. Namgoong
IPC分类号： C07D211/40 , A61K31/445 , A61P43/00 , C07D211/46
CPC分类号： C07D211/46
摘要： The synthesis of the novel fucosidase inhibitor, 2,6-imino-2,6,7-trideoxy-D-glycero-D-gluco heptitol, is disclosed.

9. 发明授权

US4996329A Derivatives of 1,4-dideoxy-1,4-imino-D-mannitol and a process for their preparation 失效
标题翻译： 1,4-二脱氧-1,4-亚氨基-D-甘露糖醇的衍生物及其制备方法
公开(公告)号：US4996329A
公开(公告)日：1991-02-26
申请号：US461859
申请日：1990-01-08
申请人： George W. J. Fleet , Bryan Winchester , Neil M. Carpenter
发明人： George W. J. Fleet , Bryan Winchester , Neil M. Carpenter
IPC分类号： A61K31/00 , A61K31/40 , A61P31/00 , A61P31/12 , A61P43/00 , C07D207/12 , C07D317/28 , C07D407/04 , C07D491/056 , C07D493/04
CPC分类号： C07D407/04 , C07D207/12 , C07D317/28 , C07D493/04 , Y02P20/582
摘要： Novel derivatives of 1,4-dideoxy-1,4-imino-D-mannitol and method for their synthesis from 4,5-anhydro-1-azido-1-deoxy-2,3-O-isopropylidene-D-talitol or its triflate derivative are disclosed. The novel derivatives, 6-fluoro-1,4-imino-1,4,6-trideoxy-D-mannitol and the N-butyl and N-benzyl derivatives of 1,4-dideoxy-1,4-amino-D-mannitol, have useful mannosidase inhibitory activity.

10. 发明授权

US4992460A Bicyclic tetrahydroxylated pyrrolizidines 失效
标题翻译：双环四羟甲基化吡咯烷子
公开(公告)号：US4992460A
公开(公告)日：1991-02-12
申请号：US404800
申请日：1989-09-08
申请人： George W. J. Fleet
发明人： George W. J. Fleet
IPC分类号： C07D487/04 , A61K31/40 , A61P3/08 , C07D317/10 , C07D491/04 , C07D491/22 , C07D493/04
CPC分类号： C07D491/04 , C07D317/10 , C07D493/04
摘要： Novel bicyclic tetrahydroxylated pyrrolizidines are disclosed which are inhibitors of glycosidase enzymes. A preferred inhibitor is 1.alpha., 2.alpha., 6.alpha., 7.alpha., 7.alpha..beta.-1,2,6,7-tetrahydroxypyrrolizidine. It is synthesized from D-glycero-D-gulo-heptono-1,4-lactone.Novel Intermediate compounds prepared during this synthesis are 7-O-tert-butyldiphenylsilyl-2,3:5,6-di-O-isopropylidene-D-glycero-D-gulo-hept ono-1,4-lactone and 1.alpha., 2.alpha., 6.alpha., 7.alpha., 7.alpha..beta.-1,2:6,7-di-O-isopropylidene-1,2,6,7-tetrahydroxypyrrolizidine.

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