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81.发明授权公开(公告)号：US06569837B1
公开(公告)日：2003-05-27
申请号：US10022276
申请日：2001-12-14
IPC分类号： A61K3170
CPC分类号： C07H19/06 , A61K31/70 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K45/06 , C07H19/16 , 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.
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：US06399589B1
公开(公告)日：2002-06-04
申请号：US09209080
申请日：1998-12-10
IPC分类号： A61K3170
CPC分类号： C07H19/10 , C07F9/65616 , C07H19/04 , C07H19/20 , C07H21/00
摘要： Compounds of formula RS—P(═O)(QR)—Nu where: R is a radical —(CH2)n—W—X; X is a radical —C(═Z) (Y) or —S—U; Z is O or S; W is O or S; Q is O or S; Y and U are an alkyl, aryl or saccharide radical which is optionally substituted with, for example, an OH, SH or NH group; n is equal to 1 to 4, preferably 1 or 2; and Nu is a radical consisting of a residue of a biologically active compound or the dephosphorylated residue of a compound which is biologically active when it bears a phosphate or phosphonate group.
摘要翻译： 式RS-P（= O）（QR）-Nu的化合物，其中：R是基团 - （CH 2）n -W-X; X是基团-C（= Z）（Y）或-S-U; Z是O或S; W为O或S; Q是O或S; Y和U是任选被例如OH，SH或NH基团取代的烷基，芳基或糖基; n等于1至4，优选1或2; 并且Nu是由生物活性化合物的残基组成的基团或当其具有磷酸酯或膦酸酯基团时具有生物活性的化合物的去磷酸化残基。
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公开(公告)号：US06395716B1
公开(公告)日：2002-05-28
申请号：US09371747
申请日：1999-08-10
IPC分类号： A61K3170
CPC分类号： C07H19/06 , A61K31/70 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K45/06 , C07H19/16 , 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.
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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84.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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85.发明申请公开(公告)号：US20110243886A1
公开(公告)日：2011-10-06
申请号：US13077733
申请日：2011-03-31
IPC分类号： A61K38/20 , C07H1/00 , A61K31/708 , A61K38/21 , A61K31/7056 , A61K31/7105 , A61K31/713 , A61P31/14
CPC分类号： C07H17/02 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7105 , A61K31/713 , C07F9/24 , C07H19/10 , C07H19/20
摘要： Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
摘要翻译： 本文提供了用于治疗肝脏疾病（包括HCV感染）的化合物，组合物和方法。 在一个实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。
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86.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：US20080064655A1
公开(公告)日：2008-03-13
申请号：US11929807
申请日：2007-10-30
IPC分类号： A61K31/7072 , A61P31/12
CPC分类号： C07H19/06 , A61K31/70 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K45/06 , C07H19/16 , 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-axyl, 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-烷基，CO-烷氧基烷基，CO-芳氧基烷基， CO取代的芳基，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，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体药物可以单独给药或与另外2'-脱氧-β-L-赤藓糖呋喃核苷一起施用，或与另一种抗肝炎 B代理。
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公开(公告)号：US20060084624A1
公开(公告)日：2006-04-20
申请号：US11232818
申请日：2005-09-22
IPC分类号： A61K31/7076
CPC分类号： C07H19/06 , A61K31/70 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K45/06 , C07H19/16 , 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-eythro-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-选择性 - 戊呋喃核苷或其药学上可接受的盐或前体药物可以单独给药或与其它2'-脱氧-β-L-赤藓寡糖核苷或其它抗肝炎联合施用 B代理。
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公开(公告)号：US06946450B2
公开(公告)日：2005-09-20
申请号：US10437802
申请日：2003-05-13
IPC分类号： A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , C07H19/06 , C07H19/16 , A61K31/70 , C07H19/073
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：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：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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