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41.发明授权
公开(公告)号：US5955591A
公开(公告)日：1999-09-21
申请号：US816570
申请日：1997-03-13
IPC分类号： A61K31/7125 , A61K48/00 , A61K49/00 , C07F9/6561 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04 , C07H19/06 , C07H19/16
CPC分类号： C07H19/10 , C07F9/65616 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： Oligonucleotides having bioreversible phosphate blocking groups can be used as pro drugs for the oligonucleotides. The bio-reversible blocking groups can be removed by intercellular enzymes, particularly carboxyesterases, to provide the unprotected oligonucleotide. The oligonucleotides can be prepared via post synthesis alkylation reactions or utilizing amidite type chemistry wherein the bioreversible phosphorus protecting group is formed as an integral part of the amidite reagent.
摘要翻译： 具有生物可逆性磷酸酯封闭基团的寡核苷酸可用作寡核苷酸的前药。 生物可逆阻断基团可以通过细胞间酶，特别是羧酸酯酶除去，以提供未保护的寡核苷酸。 寡核苷酸可以通过后合成烷基化反应或利用其中生物可逆磷保护基形成为脒矿试剂的组成部分的脒矿化学方法来制备。
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公开(公告)号：US5639873A
公开(公告)日：1997-06-17
申请号：US284484
申请日：1994-08-04
IPC分类号： G01N33/566 , A61K31/70 , A61P31/04 , A61P31/12 , A61P33/00 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/09 , C12N15/113 , C12Q1/68 , C12Q1/70 , G01N33/58
CPC分类号： C12N15/113 , C07H21/00 , C07H21/02 , C07H21/04 , C12Q1/6816 , C12N2310/32 , C12N2310/322 , C12N2310/337 , C12N2310/353 , C12N2310/3531
摘要： Chemical compounds consisting of an alpha or beta oligo-4'-thioribonucleotide or oligo-4'-thio-2'-deoxyribonucleotide characterized in that they comprise a concatenation of 4'-thioribonucleotides or 4'-thio-2'deoxyribonucleotides, respectively. The concatenation is optionally linked to an effector, in particular a radical corresponding to an intercalating agent or a photoactivatable or chemical radical, e.g. a radical carrying a function which reacts directly or indirectly with the nucleotide chains, or a radical whose presence enables easy and sensitive detection. Methods for preparing said compounds, and their uses in therapeutics, diagnostics and as laboratory reagents, are also described.
摘要翻译： PCT No.PCT / FR93 / 00115 Sec。 371日期：1994年8月4日 102（e）日期1994年8月4日PCT提交1993年2月4日PCT公布。 出版物WO93 / 16095 日期：1993年10月19日由α或β寡核苷酸-4'-硫代核糖核苷酸或寡聚-4'-硫代-2'-脱氧核糖核苷酸组成的化学化合物，其特征在于它们包含4'-硫代核苷酸或4'-硫代-2'-脱氧核糖核苷酸的连接 '脱氧核糖核苷酸。 连接任选地与效应子连接，特别是与插入剂或可光活化或化学基团相对应的基团，例如。 具有直接或间接与核苷酸链反应的功能的基团，或其存在使得易于和灵敏检测的基团。 还描述了制备所述化合物的方法及其在治疗学，诊断学和实验室试剂中的用途。
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公开(公告)号：US08304532B2
公开(公告)日：2012-11-06
申请号：US13115845
申请日：2011-05-25
申请人： Ilaria Adamo , Cecile Dueymes , Andreas Schonberger , Jean-Louis Imbach , Albert Meyer , Francois Morvan , Francoise Debart , Jean-Jacques Vasseur , Meinolf Lange , Fritz Link
发明人： Ilaria Adamo , Cecile Dueymes , Andreas Schonberger , Jean-Louis Imbach , Albert Meyer , Francois Morvan , Francoise Debart , Jean-Jacques Vasseur , Meinolf Lange , Fritz Link
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , C07H21/02 , C07H21/04 , Y02P20/55 , Y02P20/582
摘要： A solution phase synthesis method for preparing an oligonucleotide, wherein at least some of the reagents are solid supported. The method suitable for large-scale synthesis comprises coupling a protected compound with a nucleotide derivative having a protection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond; optionally processing the elongated oligonucleotide by capping by reaction with a solid supported capping agent and/or by oxidizing or sulfurizing by reaction of the oligonucleotide with a solid supported oxidizing or sulfurization reagent; and removing the protection group. The coupling may include reacting a 3′-protected compound of formula: with a nucleotide derivative having a 5′-protection group, or reacting a 5′-protected compound of formula with a nucleotide derivative having a 3′-protection group.
摘要翻译： 一种制备寡核苷酸的溶液相合成方法，其中至少一些试剂是固体负载的。 适用于大规模合成的方法包括在保持固体的活化剂存在下将受保护的化合物与具有保护基团的核苷酸衍生物偶联，得到具有P（III） - 核苷酸键的细长寡核苷酸; 任选地通过与固体支持的封端剂反应进行加帽和/或通过寡核苷酸与固体支持的氧化或硫化试剂的反应进行氧化或硫化来加工细长的寡核苷酸; 并移除保护组。 偶联可以包括使下式的3'-保护的化合物与具有5'-保护基团的核苷酸衍生物反应，或使5受保护的式的化合物与具有3'-保护基团的核苷酸衍生物反应。
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44.发明申请Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B 审中-公开用于治疗乙型肝炎的β-L-2'-Deoxy-Nucleosides公开(公告)号：US20110195922A9
公开(公告)日：2011-08-11
申请号：US12633719
申请日：2009-12-08
IPC分类号： A61K31/7064 , A61P31/12 , A61K31/7076 , A61K31/7068 , C07H19/16
CPC分类号： C07H19/16 , A61K31/70 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , C07H19/06 , A61K2300/00
摘要： This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.
摘要翻译： 本发明涉及一种用于治疗感染乙型肝炎的宿主的方法，其包括给予有效量的抗HBV生物活性2'-脱氧-α-胆红素 - 戊呋喃核苷或其药学上可接受的盐或前药，其中 2-脱氧-β-赤 - 戊呋喃核苷具有下式：其中R选自H，直链，支链或环状烷基，CO-烷基，CO-芳基，CO-烷氧基烷基，CO 芳基磺酰基，氨基酸残基，单，二或三磷酸酯，或磷酸酯衍生物; 并且BASE是嘌呤或嘧啶碱基，其可任选被取代。 2'-脱氧-β-赤 - 戊呋喃核苷或其药学上可接受的盐或前药可以单独给药或与另外2'-脱氧-α-赤 - 戊呋喃核苷一起施用或与另一种 抗乙型肝炎药。
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45.发明申请公开(公告)号：US20070087995A1
公开(公告)日：2007-04-19
申请号：US11558288
申请日：2006-11-09
IPC分类号： A61K31/7076 , A61K31/7072
CPC分类号： C07H19/16 , A61K31/70 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , C07H19/06 , A61K2300/00
摘要： This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.
摘要翻译： 本发明涉及一种用于治疗感染乙型肝炎的宿主的方法，其包括施用有效量的抗HBV生物活性2'-脱氧-β-L-赤 - 戊呋喃核苷或其药学上可接受的盐或前药，其中 2'-脱氧-β-L-赤 - 戊呋喃核苷具有下式：其中R选自H，直链，支链或环状烷基，CO-烷基，CO-芳基，CO-烷氧基烷基，CO-芳氧基烷基 烷基磺酰基，芳基磺酰基，芳烷基磺酰基，氨基酸残基，单，二或三磷酸酯，或磷酸酯衍生物; 并且BASE是嘌呤或嘧啶碱基，其可任选被取代。 2'-脱氧-β-L-赤 - 戊呋喃核苷或其药学上可接受的盐或前药可以单独或与其它2'-脱氧-β-L-赤 - 戊呋喃核苷组合或与另一种抗 - 乙型肝炎药。
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公开(公告)号：US20050113330A1
公开(公告)日：2005-05-26
申请号：US10972695
申请日：2004-10-25
IPC分类号： C07H19/06 , C07H19/16 , A61K31/7076 , A61K31/513 , A61K31/522 , A61K31/7072
摘要： The present invention relates to compounds, compositions and methods for the treatment of a host infected with a hepatitis B virus. Specifically, compound and compositions of 3′-esters of 2′-deoxy-β-L-nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents. Compound and compositions of 3′,5′-diesters of 2′-deoxy-β-L-nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents, are also disclosed.
摘要翻译： 本发明涉及用于治疗感染乙型肝炎病毒的宿主的化合物，组合物和方法。 具体地，公开了2'-脱氧-β-L-核苷的3'-酯的化合物和组合物，其可以单独施用或与其它抗乙型肝炎药物组合施用。 公开了可以单独施用或与其它抗乙型肝炎试剂组合施用的2'-脱氧-β-L-核苷的3'，5'-二酯的化合物和组合物。
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47.发明申请2' or 3' -deoxy and 2' , 3' -dideoxy-beta-L-pentofuranonucleo-side compounds, method of preparation and application in therapy, especially as anti-viral agents 有权2'或3'-脱氧和2'，3'-二脱氧-β-L-戊呋喃核苷酸化合物，其制备方法和在治疗中的应用，特别是抗病毒剂公开(公告)号：US20050101776A1
公开(公告)日：2005-05-12
申请号：US10672585
申请日：2003-09-26
申请人： Gilles Gosselin , Jean-Louis Imbach , Anne-Marie Aubertin , Jean-Pierre Sommmadossi , Raymond Schinazi
发明人： Gilles Gosselin , Jean-Louis Imbach , Anne-Marie Aubertin , Jean-Pierre Sommmadossi , Raymond Schinazi
IPC分类号： C07D405/04 , C07D473/00 , C07H19/04 , C07H19/22 , C07H19/048
CPC分类号： C07D473/00 , C07D405/04 , C07H19/04
摘要： Method for the sterospecific preparation of 2′ or 3′ deoxy and 2′,3′-dideoxy-β-L-pentafuranonucleoside compounds. 2′ or 3′ deoxy and 2′,3′-dideoxy-β-L-pentofuranonucleoside compounds are also described. Finally, the invention concerns the use of these compounds, and particularly 2′,3′dideoxy-β-L-fluorocytidine, as drugs, and especially as anti-viral agents.
摘要翻译： 2'或3'脱氧和2'，3'-二脱氧-β-L-五氟硼核苷化合物的高效特异性制备方法。 还描述了2'或3'脱氧和2'，3'-二脱氧-β-L-戊呋喃核苷化合物。 最后，本发明涉及这些化合物，特别是2'，3'-脱氧-β-L-氟胞嘧啶作为药物，特别是作为抗病毒剂的用途。
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公开(公告)号：US06458773B1
公开(公告)日：2002-10-01
申请号：US09435261
申请日：1999-11-05
IPC分类号： A61K3170
摘要： Compounds and pharmaceutical compositions active against hepatitis B virus are provided, as is a method for the treatment of hepatitis B virus infection in humans and other host animals is provided comprising administering an effective amount of a &bgr;-L-(2′or 3′-azido)-2′,3′-dideoxy-5-fluorocytosine of the formula wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R′is H, acyl, or alkyl.
摘要翻译： 提供了针对乙型肝炎病毒的化合物和药物组合物，提供了在人和其他宿主动物中治疗乙型肝炎病毒感染的方法，包括施用有效量的β-L-（2'-3'- 叠氮基）-2'，3'-二脱氧-5-氟胞嘧啶R是H，酰基，单磷酸，二磷酸或三磷酸，或稳定的磷酸酯衍生物（形成稳定的核苷酸前药），R'H， 酰基或烷基。
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公开(公告)号：US06444652B1
公开(公告)日：2002-09-03
申请号：US09459150
申请日：1999-12-10
IPC分类号： A61K3170
CPC分类号： C07H19/16 , A61K31/70 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , C07H19/06 , A61K2300/00
摘要： This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.
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公开(公告)号：US06407077B1
公开(公告)日：2002-06-18
申请号：US09435268
申请日：1999-11-05
IPC分类号： A61K317068
CPC分类号： A61K31/7068
摘要： Compounds and pharmaceutical compositions active against HIV are provided, as is a method for the treatment of HIV infection in humans and other host animals is provided comprising administering an effective amount of a &bgr;-L-(2′ or 3′-azido)-2′,3′-dideoxy-5-fluorocytosine of the formula wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R′ is H, acyl, or alkyl.
摘要翻译： 提供了对HIV有活性的化合物和药物组合物，如在人和其他宿主动物中治疗HIV感染的方法一样，提供有效量的β-L-（2'或3'-叠氮基）-2 '，3' - 二脱氧-5-氟胞嘧啶R是H，酰基，单磷酸，二磷酸或三磷酸，或稳定的磷酸酯衍生物（形成稳定的核苷酸前药），R'是H，酰基或烷基 。
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