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公开(公告)号：US06875751B2
公开(公告)日：2005-04-05
申请号：US09883033
申请日：2001-06-15
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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公开(公告)号：US06245749B1
公开(公告)日：2001-06-12
申请号：US09112878
申请日：1998-07-09
IPC分类号： A61K3170
CPC分类号： A61K31/70 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21 , A61K47/544 , A61K2300/00
摘要： A method for the treatment of a host, and in particular, a human, infected with hepatitis B virus (HBV) is provided that includes administering an effective amount of a nucleotide prodrug of &bgr;- L-2′, 3′-dideoxyadenosine, wherein the prodrug component of the nucleotide provides controlled delivery of the active species.
摘要翻译： 提供了治疗感染乙型肝炎病毒（HBV）的宿主，特别是人的方法，其包括施用有效量的β-L-2'，3'-二脱氧腺苷的核苷酸前药，其中 核苷酸的前药组分提供活性物质的受控递送。
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公开(公告)号：US5770725A
公开(公告)日：1998-06-23
申请号：US416515
申请日：1995-04-04
申请人： Gilles Gosselin , Jean-Louis Imbach
发明人： Gilles Gosselin , Jean-Louis Imbach
CPC分类号： C07H19/10 , C07F9/65616 , C07H19/20 , C07H21/00
摘要： Compounds of formula RO--P(.dbd.O)(OR)--Nu where: each R is, independently, --(CH.sub.2).sub.n --S--X; X is --C(.dbd.Z) (Y) or --S--U; Z is O or S; Y and U are alkyl, aryl or saccharide groups optionally substituted with OH, SH or NH groups; n is 1 to 4; and Nu is a nucleoside which comprises a ribose or deoxyribose sugar portion covalently bound to a base portion.
摘要翻译： 式RO-P（= O）（OR）-Nu的化合物其中：各R独立地为 - （CH 2）n -S-X; X是-C（= Z）（Y）或-S-U; Z是O或S; Y和U是任选被OH，SH或NH基取代的烷基，芳基或糖基; n为1〜4; 并且Nu是核苷，其包含共价结合到基部的核糖或脱氧核糖。
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公开(公告)号：US5627185A
公开(公告)日：1997-05-06
申请号：US465450
申请日：1995-06-05
申请人： Gilles Gosselin , Jean-Louis Imbach
发明人： Gilles Gosselin , Jean-Louis Imbach
CPC分类号： C07F9/65616 , C07H19/04 , C07H19/10 , C07H19/20 , C07H21/00 , Y10S514/885 , Y10S514/894
摘要： Derivatives of Acyclovir are provided having patent antiviral inhibitory activity. Phosphotriester derviatives are preferred which have the structure: ##STR1## where R is alkyl, especially CH.sub.3 or (CH.sub.3).sub.3 C.
摘要翻译： 阿昔洛韦的衍生物具有专利抗病毒抑制活性。 磷酸三酯是优选的，具有以下结构：CH3）3C。
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25.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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26.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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28.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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