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    Method for preparing oligonucleotides
    1.
    发明申请
    Method for preparing oligonucleotides 审中-公开
    寡核苷酸的制备方法

    公开(公告)号：US20100069623A1

    公开(公告)日：2010-03-18

    申请号：US12417750

    申请日：2009-04-03

    申请人： Ilaria Adamo ,  Cècile Dueymes ,  Andreas Schönberger ,  Jean-Louis Imbach ,  Albert Meyer ,  Francois Morvan ,  Francoise Debart ,  Jean-Jacques Vasseur ,  Meinolf Lange ,  Fritz Link

    发明人： Ilaria Adamo ,  Cècile Dueymes ,  Andreas Schönberger ,  Jean-Louis Imbach ,  Albert Meyer ,  Francois Morvan ,  Francoise Debart ,  Jean-Jacques Vasseur ,  Meinolf Lange ,  Fritz Link

    IPC分类号： C07H21/04

    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。

    Method for preparing oligonucleotides
    2.
    发明授权
    Method for preparing oligonucleotides 失效
    寡核苷酸的制备方法

    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。

    Method for preparing oligonucleotides
    3.
    发明申请
    Method for preparing oligonucleotides 审中-公开
    寡核苷酸的制备方法

    公开(公告)号：US20060089494A1

    公开(公告)日：2006-04-27

    申请号：US10522854

    申请日：2003-07-30

    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： C07H21/02 ,  C07H21/04

    CPC分类号： C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  Y02P20/55 ,  Y02P20/582

    摘要： A method for preparing an oligonucleotide comprising the steps of a) providing a 3-protected compound having the formula: wherein B is a heterocyclic base R2 is H, a protected 2-hydroxyl group, F, a protected amino group, an O-alkyl group, an O-substituted alkyl, a substituted alkylamino or a C4′-O2′methylen linkage R3 is OR′3, NHR″3, NR″3R′″3, a 3′-protected nucleotide or a 3′-protected oligonucleotide, R′3 is a hydroxyl protecting group, R″3, R′″3 are independently an amine protecting group, b) reacting said compound with a nucleotide derivative having a 5-proctection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond c) optionally processing the elongated oligonucleotide with a P(III)-internucleotide bond by either or both of steps c1) and c2) in any sequence c1) capping preferably by reacting with a solid supported capping agent c2) oxidizing preferably by reacting the oligonucleotide with a solid supported oxidizing reagent d) removing the 5′-protection group.

    摘要翻译： 一种制备寡核苷酸的方法，包括以下步骤：a）提供具有下式的3-保护的化合物：其中B是杂环基R2是H，被保护的2-羟基，F，保护的氨基，O-烷基 基团，O-取代的烷基，取代的烷基氨基或C4'-O2'亚甲基键R3是OR'3，NHR'3，NR'3R“'，3'-保护的核苷酸或3' R'3是羟基保护基，R“3”，“3”独立地是胺保护基，b）使所述化合物与具有5-取代基的核苷酸衍生物在 c）通过任何序列c1）和c2）中任一或两个步骤c1）和c2）任选地用P（III） - 核苷酸键处理细长寡核苷酸 优选通过与固体支持的封端剂c2反应，优选通过使寡核苷酸与固体支持物反应来进行氧化 d）除去5'-保护基。

    Beta-L-2'-deoxy-nucleosides for the treatment of hepatitis B
    5.
    发明申请
    Beta-L-2'-deoxy-nucleosides for the treatment of hepatitis B 审中-公开

    公开(公告)号：US20060025375A1

    公开(公告)日：2006-02-02

    申请号：US11230944

    申请日：2005-09-20

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Martin Bryant

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Martin Bryant

    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.

    &bgr;-L-2′-deoxy-nucleosides for the treatment of hepatitis B
    7.
    发明授权
    &bgr;-L-2′-deoxy-nucleosides for the treatment of hepatitis B 有权
    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。

    Biologically active phosphotriester-type compounds
    8.
    发明授权
    Biologically active phosphotriester-type compounds 失效
    生物活性磷酸三酯类化合物

    公开(公告)号：US06555676B2

    公开(公告)日：2003-04-29

    申请号：US09961154

    申请日：2001-09-21

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Christian Perigaud

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Christian Perigaud

    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。

    Pharmaceutical compositions based on xylosides and lyxosides of purine and pyrimidine bases used in a method of treating viruses
    9.
    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

    申请人： Jean-Louis Imbach ,  Gilles Gosselin ,  Jean De Rudder

    发明人： Jean-Louis Imbach ,  Gilles Gosselin ,  Jean De Rudder

    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

    CPC分类号： 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