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1.发明授权
公开(公告)号：US5250703A
公开(公告)日：1993-10-05
申请号：US954199
申请日：1992-09-29
IPC分类号： C07D207/12 , C07D407/06
CPC分类号： C07D207/12
摘要： Novel heptitol analogues of mannofuranose and their syntheses from .delta.-lactones of heptonic acids are disclosed. The novel heptitols are (A) 2,5-dideoxy-2,5-imino-D-glycero-D-talo-heptitol and (b) 1-amino-2,5-anhydro-1-deoxy-D-glycero-D-talo-heptitol. These novel heptitol compounds are useful inhibitors of glycosidases.
摘要翻译： 公开了甘露糖醛糖的新型七糖醇类似物及其由庚糖酸的β-内酯的合成。 新型的庚硫醇是（A）2,5-二脱氧-2,5-亚氨基-D-甘油基-D-木糖醇和（b）1-氨基-2,5-脱水-1-脱氧-D-甘油基 - D-谷 - 七糖醇。 这些新型的庚糖醇化合物是糖苷酶的有用抑制剂。
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公开(公告)号：US5300659A
公开(公告)日：1994-04-05
申请号：US75940
申请日：1993-06-14
IPC分类号： C07D207/12 , C07D407/06
CPC分类号： C07D207/12
摘要： Novel heptitol analogues of mannofuranose and their syntheses from .delta.-lactones of heptonic acids are disclosed. The novel heptitols are (A) 2,5-dideoxy-2,5-imino-D-glycero-D-talo-heptitol and (b) 1-amino-2,5-anhydro-1-deoxy-D-glycero-D-talo-heptitol. These novel heptitol compounds are useful inhibitors of glycosidases.
摘要翻译： 公开了甘露糖醛糖的新型七糖醇类似物及其由庚糖酸的β-内酯的合成。 新型的庚硫醇是（A）2,5-二脱氧-2,5-亚氨基-D-甘油基-D-木糖醇和（b）1-氨基-2,5-脱水-1-脱氧-D-甘油基 - D-谷 - 七糖醇。 这些新型的庚糖醇化合物是糖苷酶的有用抑制剂。
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公开(公告)号：US5384417A
公开(公告)日：1995-01-24
申请号：US181716
申请日：1994-01-18
IPC分类号： C07D207/12 , C07D307/20
CPC分类号： C07D207/12
摘要： Novel heptitol analogues of mannofuranose and their syntheses from .delta.-lactones of heptonic acids are disclosed. The novel heptitols are (A) 2,5-dideoxy-2,5-imino-D-glycero-D-talo-heptitol and (b) 1-amino-2,5-anydro-1-deoxy-D-glycero-D-talo-heptitol. These novel heptitol compounds are useful inhibitors of glycosidases.
摘要翻译： 公开了甘露糖醛糖的新型七糖醇类似物及其由庚糖酸的β-内酯的合成。 新型的庚硫醇是（A）2,5-二脱氧-2,5-亚氨基-D-甘油基-D-木糖醇和（b）1-氨基-2,5-脱氧-1-脱氧-D-甘油基 - D-谷 - 七糖醇。 这些新型的庚糖醇化合物是糖苷酶的有用抑制剂。
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公开(公告)号：US5210089A
公开(公告)日：1993-05-11
申请号：US830826
申请日：1992-02-04
IPC分类号： C07D211/76
CPC分类号： C07D211/76
摘要： The novel D-rhamnono-? ,5-lactone and a novel method of synthesis of said compound from the monoacetonide of L-gulono-.gamma.-lactone is disclosed. D-Rhamnono-1,5-lactone is a potent inhibitor of .alpha.-and .beta.-mannosidases but not of .alpha.-rhamnosidase.
摘要翻译： 小说D-rhamnono- 公开了从L-古洛糖-γ-内酯的单丙酮化合物合成所述化合物的新方法。 D-鼠李糖-1,5-内酯是α-和β-甘露糖苷酶的有效抑制剂，但不是α-鼠李糖苷酶。
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公开(公告)号：US5096909A
公开(公告)日：1992-03-17
申请号：US600941
申请日：1990-10-22
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。
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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 。
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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.
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公开(公告)号：US5089520A
公开(公告)日：1992-02-18
申请号：US584982
申请日：1990-09-20
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。
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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。
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公开(公告)号：US5017704A
公开(公告)日：1991-05-21
申请号：US372415
申请日：1989-06-27
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.
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