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公开(公告)号：US06555676B2
公开(公告)日：2003-04-29
申请号：US09961154
申请日：2001-09-21
IPC分类号： C07H1904
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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2.发明授权Biologically active phosphotriester-type nucleosides and methods for preparing same 失效生物活性磷酸三酯型核苷及其制备方法
公开(公告)号：US5849905A
公开(公告)日：1998-12-15
申请号：US712926
申请日：1996-09-13
CPC分类号： C07H19/10 , C07F9/65616 , C07H19/04 , C07H19/20 , C07H21/00
摘要： Compounds of formula RS--P(.dbd.O) (QR)--Nu where: R is a radical --(CH.sub.2)n-W--X; X is a radical --C(.dbd.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：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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4.发明授权2′ or 3′ -deoxy and 2′, 3′-dideoxy-β-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，特别是作为抗病毒剂公开(公告)号：US07439351B2
公开(公告)日：2008-10-21
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 F. Schinazi
发明人： Gilles Gosselin , Jean-Louis Imbach , Anne-Marie Aubertin , Jean-Pierre Sommmadossi , Raymond F. Schinazi
IPC分类号： C07H19/073 , C07H19/173
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：US20060025375A1
公开(公告)日：2006-02-02
申请号：US11230944
申请日：2005-09-20
IPC分类号： A61K31/7072 , A61K31/7076
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.
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公开(公告)号：US06896900B2
公开(公告)日：2005-05-24
申请号：US10175365
申请日：2002-06-18
IPC分类号： A61K31/7068 , A61P31/18 , A61K9/20 , A61K9/48 , A61M37/00
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 β-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，其中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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公开(公告)号：US06566344B1
公开(公告)日：2003-05-20
申请号：US10022148
申请日：2001-12-14
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。
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8.发明授权Pharmaceutical compositions based on xylosides and lyxosides of purine and pyrimidine bases used in a method of treating viruses 失效用于治疗病毒的方法中使用的基于嘌呤和嘧啶碱基的木糖苷和lyxosides的药物组合物
公开(公告)号：US4659698A
公开(公告)日：1987-04-21
申请号：US734846
申请日：1985-05-16
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/06 , C07H19/16
摘要： Pharmaceutical compositions which contain a xyloside or a lyxoside of a purine or pyrimidine base selected from the following compounds:1-(.beta.-D-xylofuranosyl)-cytosine, 1-(.beta.-D-xylofuranosyl)-thymine, 9-(.alpha.-D-xylofuranosyl)-adenine, 9-(.alpha.-D-xylofuranosyl)-guanine, 1-(.alpha.-D-xylofuranosyl)-cytosine, 1-(.alpha.-D-xylofuranosyl)-thymine, 1-(.beta.-D-lyxofuranosyl)-adenine, 9-(.beta.-D-lyxofuranosyl)-guanine, 1-(.beta.-D-lyxofuranosyl)-cytosine, 1-(.beta.-D-lyxofuranosyl)-thymine, 9-(.alpha.-D-lyxofuranosyl)-adenine, 1-(.alpha.-D-lyxofuranosyl)-guanine, 1-(.alpha.-D-lyxofuranosyl)-cytosine and 1-(.alpha.-D-lyxofuranosyl)-thymine, have been found to be useful in therapy for treating various viral diseases.
摘要翻译： 选自以下化合物的嘌呤或嘧啶碱基的木糖苷或睾酮的药物组合物：1-（β--D-木糖呋喃糖基） - 胞嘧啶，1-（β--D-木糖呋喃糖基） - 胸腺嘧啶，9-（α- 鸟嘌呤，1-（α-D-呋喃核糖基） - 鸟嘌呤，1-（α-D-木糖呋喃糖基） - 胞嘧啶，1-（α-D-木糖呋喃糖基） - 胸腺嘧啶，1-（β-D- 鸟嘌呤，1-（β-D-吡喃孢呋喃糖基） - 胞嘧啶，1-（β--D-裂解呋喃糖基） - 胸腺嘧啶，9-（α-D-吡喃孢呋喃糖基） - 腺嘌呤，9- 腺嘌呤，1-（α-D-吡喃孢子糖基） - 鸟嘌呤，1-（α-D-裂解呋喃糖基） - 胞嘧啶和1-（α-D-吡喃孢子糖基） - 胸腺嘧啶已被发现可用于治疗各种 病毒性疾病
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公开(公告)号：US07795238B2
公开(公告)日：2010-09-14
申请号：US11929798
申请日：2007-10-30
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。
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10.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：US20100152126A1
公开(公告)日：2010-06-17
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-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。
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