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公开(公告)号：EP0413674A2
公开(公告)日：1991-02-20
申请号：EP90870126.1
申请日：1990-08-13
申请人： MONSANTO COMPANY
摘要： A method is provided for converting therapeutic glycosidase inhibitors to novel prodrugs by phosphorylation of a free hydroxyl group on the molecule to substantially reduce the glycosidase inhibitory activity without thereby substantially reducing the therapeutic activity.
摘要翻译： 提供了一种通过磷酸化分子上的游离羟基而将治疗性糖苷酶抑制剂转化为新型前药的方法，以显着降低糖苷酶抑制活性，而不会显着降低治疗活性。
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公开(公告)号：EP0215766A3
公开(公告)日：1988-07-27
申请号：EP86870123
申请日：1986-09-05
申请人： Monsanto Company
摘要： A preparative scale method for the isolation of unreduced oligosaccharides of glycoproteins and glycohormones having a N-linked oligosaccharide structure is disclosed. The method employs hydrazinolysis of the glycoprotein or glycohormone under reaction conditions to cause cleavage at the N-linked sites, producing a mixture having as a major component a de-N-acetylated hydrazone derivative of the oligosaccharides, followed by N-acylation of the hydrazone derivative, acid-catalysis of the hydrazone derivative to produce unreduced oligosaccharides, and subjecting the resulting unreduced oligosaccharides to cellulose column chromatography to remove contaminants and to recover the unreduced oligosaccharides.
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3.发明授权Use of the N-n-butyl derivative of desoxynojirimycin in the manufacture of a medicament inhibiting HIV-Virus 失效脱氧野尻霉素的N-正丁基衍生物在制备药物中的HIV病毒的抑制应用
公开(公告)号：EP0324328B1
公开(公告)日：1997-10-22
申请号：EP88870191.9
申请日：1988-12-20
申请人： Monsanto Company
IPC分类号： A61K31/445
CPC分类号： A61K31/445
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公开(公告)号：EP0413674A3
公开(公告)日：1991-07-17
申请号：EP90870126.1
申请日：1990-08-13
申请人： MONSANTO COMPANY
摘要： A method is provided for converting therapeutic glycosidase inhibitors to novel prodrugs by phosphorylation of a free hydroxyl group on the molecule to substantially reduce the glycosidase inhibitory activity without thereby substantially reducing the therapeutic activity.
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公开(公告)号：EP0215766A2
公开(公告)日：1987-03-25
申请号：EP86870123.6
申请日：1986-09-05
申请人： Monsanto Company
摘要： A preparative scale method for the isolation of unreduced oligosaccharides of glycoproteins and glycohormones having a N-linked oligosaccharide structure is disclosed. The method employs hydrazinolysis of the glycoprotein or glycohormone under reaction conditions to cause cleavage at the N-linked sites, producing a mixture having as a major component a de-N-acetylated hydrazone derivative of the oligosaccharides, followed by N-acylation of the hydrazone derivative, acid-catalysis of the hydrazone derivative to produce unreduced oligosaccharides, and subjecting the resulting unreduced oligosaccharides to cellulose column chromatography to remove contaminants and to recover the unreduced oligosaccharides.
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公开(公告)号：EP0322395B1
公开(公告)日：1993-03-24
申请号：EP88870192.7
申请日：1988-12-20
申请人： Monsanto Company
IPC分类号： A61K31/40 , A61K31/445 , C07D207/12 , C07D211/46 , C07D211/76
CPC分类号： C07D211/46 , A61K31/40 , A61K31/445 , C07D207/12 , C07D211/88
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9.发明公开Use of the N-n-butyl derivative of desoxynojirimycin in the manufacture of a medicament inhibiting HIV-Virus 失效在药物制造中使用脱氧吉西他滨的N-N-BUTYL衍生物
公开(公告)号：EP0324328A3
公开(公告)日：1990-06-20
申请号：EP88870191.9
申请日：1988-12-20
申请人： Monsanto Company
IPC分类号： A61K31/445
CPC分类号： A61K31/445
摘要： The N-n-butyl derivative of deoxynojirimycin or a pharmaceutically acceptable salt derivative thereof is useful for the manufacture of a medicament for the treatment of AIDS.
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10.发明公开Use of the N-n-butyl derivative of desoxynojirimycin in the manufacture of a medicament inhibiting HIV-Virus 失效Anwendung des N-n-butyl-Derivates von Desoxynojirimycin zur Herstellung eines Arzneimittels。
公开(公告)号：EP0324328A2
公开(公告)日：1989-07-19
申请号：EP88870191.9
申请日：1988-12-20
申请人： Monsanto Company
IPC分类号： A61K31/445
CPC分类号： A61K31/445
摘要： The N-n-butyl derivative of deoxynojirimycin or a pharmaceutically acceptable salt derivative thereof is useful for the manufacture of a medicament for the treatment of AIDS.
摘要翻译： 脱氧野尻霉素的N-正丁基衍生物或其药学上可接受的盐衍生物可用于制备用于治疗AIDS的药物。
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