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1. 发明授权

US06566344B1 &bgr;-L-2′-deoxy-nucleosides for the treatment of hepatitis B 有权
标题翻译： β-L-2'-脱氧核苷用于治疗乙型肝炎
公开(公告)号：US06566344B1
公开(公告)日：2003-05-20
申请号：US10022148
申请日：2001-12-14
申请人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
发明人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
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-pentoftiranonucleoside 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-赤式 - 戊烯基核苷具有下式：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。

2. 发明授权

US06946450B2 β-L-2′-deoxy-nucleosides for the treatment of hepatitis B 有权
标题翻译： β-L-2'-脱氧核苷用于治疗乙型肝炎
公开(公告)号：US06946450B2
公开(公告)日：2005-09-20
申请号：US10437802
申请日：2003-05-13
申请人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
发明人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
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。

3. 发明授权

US06875751B2 3′-prodrugs of 2′-deoxy-β-L-nucleosides 有权
标题翻译： 2'-脱氧-β-L-核苷的3'-前药
公开(公告)号：US06875751B2
公开(公告)日：2005-04-05
申请号：US09883033
申请日：2001-06-15
申请人： Jean-Louis Imbach , Martin L. Bryant , Gilles Gosselin
发明人： Jean-Louis Imbach , Martin L. Bryant , Gilles Gosselin
IPC分类号： C07H19/06 , C07H19/16 , A61K31/70
CPC分类号： C07H19/16 , C07H19/06
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。

4. 发明授权

US07795238B2 β-L-2′-deoxy-nucleosides for the treatment of hepatitis B 有权
标题翻译：＆bgr; -L-2'-脱氧核苷用于治疗乙型肝炎
公开(公告)号：US07795238B2
公开(公告)日：2010-09-14
申请号：US11929798
申请日：2007-10-30
申请人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
发明人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
IPC分类号： A61K31/70
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。

5. 发明申请

US20100152126A1 Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B 审中-公开
标题翻译：用于治疗乙型肝炎的β-L-2'-Deoxy-Nucleosides
公开(公告)号：US20100152126A1
公开(公告)日：2010-06-17
申请号：US12633719
申请日：2009-12-08
申请人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
发明人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
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-β-赤 - 戊呋喃核苷一起施用或与另一种组合施用抗乙型肝炎药。

6. 发明授权

US07585851B2 3′-prodrugs of 2′-deoxy-β-L-nucleosides 有权
标题翻译： 2'-脱氧-β-L-核苷的3'-前药
公开(公告)号：US07585851B2
公开(公告)日：2009-09-08
申请号：US10972695
申请日：2004-10-25
申请人： Martin L. Bryant , Gilles Gosselin , Jean-Louis Imbach
发明人： Martin L. Bryant , Gilles Gosselin , Jean-Louis Imbach
IPC分类号： A61K31/70 , C07H19/073 , C07H19/10
CPC分类号： C07H19/16 , C07H19/06
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-pyrimidine 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-pyrimidine nucleosides are also disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents.
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-嘧啶核苷的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。还公开了2'-脱氧-β-L-嘧啶核苷的3'，5'-二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。

7. 发明申请

US20080188440A1 Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B 有权
标题翻译：用于治疗乙型肝炎的β-L-2'-Deoxy-Nucleosides
公开(公告)号：US20080188440A1
公开(公告)日：2008-08-07
申请号：US11929798
申请日：2007-10-30
申请人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
发明人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
IPC分类号： A61K31/7072 , A61P31/20
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。

8. 发明申请

US20120264707A1 BETA-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B 审中-公开
标题翻译：用于治疗乙型肝炎的BETA-L-2'-DEOXY-NUCLEOSIDES
公开(公告)号：US20120264707A1
公开(公告)日：2012-10-18
申请号：US13464674
申请日：2012-05-04
申请人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
发明人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
IPC分类号： A61K31/708 , C07H19/173 , A61K31/7072 , A61P31/20 , A61K31/7076 , A61K31/7068
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-β-赤 - 戊呋喃核苷一起施用或与另一种组合施用抗乙型肝炎药。

9. 发明申请

US20110257120A1 BETA-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B 审中-公开
标题翻译：用于治疗乙型肝炎的BETA-L-2'-DEOXY-NUCLEOSIDES
公开(公告)号：US20110257120A1
公开(公告)日：2011-10-20
申请号：US13170118
申请日：2011-06-27
申请人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
发明人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
IPC分类号： A61K31/7076 , A61P31/12 , A61K31/7068 , C07H19/16 , A61K31/7064 , A61K31/708
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。

10. 发明授权

US07304043B2 β-L-2′-deoxy-nucleosides for the treatment of hepatitis B 有权
标题翻译： β-L-2'-脱氧核苷用于治疗乙型肝炎
公开(公告)号：US07304043B2
公开(公告)日：2007-12-04
申请号：US11232818
申请日：2005-09-22
申请人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
发明人： Gilles Gosselin , Jean-Louis Imbach , Martin L. Bryant
IPC分类号： A61K31/70 , A61K9/22
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：

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