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    Bicyclonucleoside analogues
    3.
    发明授权
    Bicyclonucleoside analogues 失效
    双环核苷类似物

    公开(公告)号：US07994145B2

    公开(公告)日：2011-08-09

    申请号：US11700361

    申请日：2007-01-31

    申请人： Takeshi Imanishi ,  Satoshi Obika

    发明人： Takeshi Imanishi ,  Satoshi Obika

    IPC分类号： A61K48/00 ,  C07H21/02

    CPC分类号： C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  Y02P20/55

    摘要： Oligonucleotide analogues which have anti-sense or anti-gene activity, as well as in vivo stability, or pharmaceutically acceptable salts thereof. The oligonucleotide analogues have one or more structural units represented by the following formula (1a): provided that when the oligonucleotide has two or more structural units of formula (1a), each B is the same or different, wherein B represents a purin-9-yl group or a 2-oxo-1,2-dihydropyrimidin-1-yl group.

    摘要翻译： 具有反义或抗基因活性的寡核苷酸类似物，以及体内稳定性或其药学上可接受的盐。 寡核苷酸类似物具有一个或多个由下式（1a）表示的结构单元：条件是当寡核苷酸具有两个或更多个式（1a）的结构单元时，每个B相同或不同，其中B表示嘌呤-9 - 基或2-氧代-1,2-二氢嘧啶-1-基。

    Novel artificial nucleic acids of n-o bond crosslinkage type
    5.
    发明申请
    Novel artificial nucleic acids of n-o bond crosslinkage type 有权
    新型n-o键交联型人造核酸

    公开(公告)号：US20070167387A1

    公开(公告)日：2007-07-19

    申请号：US10569949

    申请日：2004-08-25

    申请人： Takeshi Imanishi ,  Satoshi Obika ,  Kazuyuki Miyashita

    发明人： Takeshi Imanishi ,  Satoshi Obika ,  Kazuyuki Miyashita

    IPC分类号： A61K48/00 ,  C07H21/02 ,  C07H19/04 ,  C07H19/048 ,  C07H19/22

    CPC分类号： C07H19/04 ,  C07H21/00 ,  Y02P20/55

    摘要： An oligonucleotide analogue useful for the antisense method, etc., having excellent enzyme resistance, having potent selective binding affinity for single-stranded RNA, and further having an excellent triplex-forming capacity with double-stranded DNA, and a nucleoside analogue useful for its production are provided. Nucleoside analogues, which are compounds of the general formula (I) and salts thereof, and oligonucleotide analogues containing one or more of the nucleoside analogues: where Base is an aromatic heterocyclic group or the like optionally having a substituent; R1, R2 and R3 are each a hydrogen atom, a protective group for an amino group, a protective group for a hydroxyl group, a phosphate group, or —P(R4)R5 [where R4 and R5 are each a hydroxyl group, a protected hydroxyl group, a mercapto group, a protected mercapto group, etc.]; m=0 to 2; and n=1 to 3].

    摘要翻译： 可用于反义方法等的寡核苷酸类似物具有优异的耐酶性，对单链RNA具有强选择性结合亲和力，并且还具有双链DNA具有优异的三链体形成能力，以及可用于其的核苷类似物 提供生产。 核苷类似物，其是通式（I）的化合物及其盐，以及含有一个或多个核苷类似物的寡核苷酸类似物：其中，碱是任选具有取代基的芳族杂环基等; R 1，R 2和R 3各自为氢原子，氨基保护基，羟基保护基 ，磷酸基或-P（R 4）R 5 [其中R 4和R 5'是 每个羟基，被保护的羟基，巯基，保护的巯基等]; m = 0〜2; n = 1〜3]。

    Bicyclonucleoside analogues
    6.
    发明授权
    Bicyclonucleoside analogues 失效
    双环核苷类似物

    公开(公告)号：US07217805B2

    公开(公告)日：2007-05-15

    申请号：US10054300

    申请日：2002-01-22

    申请人： Takeshi Imanishi ,  Satoshi Obika

    发明人： Takeshi Imanishi ,  Satoshi Obika

    IPC分类号： C07H19/00 ,  C07H21/00 ,  C07H19/048

    CPC分类号： C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  Y02P20/55

    摘要： Bicyclonucleoside analogues which exhibit anti-AIDS activity and intermediates to produce oligonucleotide analogues which have anti-sense or anti-gene activity as well as in vivo stability. Compounds of the following formula (1) or their pharmaceutically acceptable salts. wherein R1 represents a hydrogen atom or a protecting group for a hydroxy group, R2 represents an azido group or an optionally protected amino group or the like, B represents a purin-9-yl or a 2-oxo-1,2-dihydropyrimidin-1-yl group, which are optionally substituted with substituents selected from the group consisting of a halogen atom, an alkyl group having 1–6 carbon atoms, a hydroxy group, a mercapto group and an amino group.

    摘要翻译： 具有抗艾滋病活性的双环核苷类似物和产生具有反义或抗基因活性以及体内稳定性的寡核苷酸类似物的中间体。 下式（1）的化合物或其药学上可接受的盐。 其中R 1表示氢原子或羟基的保护基，R 2表示叠氮基或任选保护的氨基等，B表示嘌呤 -9-基或2-氧代-1,2-二氢嘧啶-1-基，其任选被选自以下的取代基取代：卤素原子，具有1-6个碳原子的烷基，羟基 ，巯基和氨基。

    Novel anitsense oligonucleotide derivatives against to hepatitis c virus
    7.
    发明申请
    Novel anitsense oligonucleotide derivatives against to hepatitis c virus 审中-公开
    针对丙型肝炎病毒的新型琥珀酸寡核苷酸衍生物

    公开(公告)号：US20050059617A1

    公开(公告)日：2005-03-17

    申请号：US10489771

    申请日：2002-09-17

    申请人： Takeshi Imanishi ,  Satoshi Obika ,  Yoshiyuki Ohsugi

    发明人： Takeshi Imanishi ,  Satoshi Obika ,  Yoshiyuki Ohsugi

    IPC分类号： A61K31/14 ,  A61K31/712 ,  A61K38/00 ,  A61P31/14 ,  C07H21/00 ,  C12N15/113 ,  A61K48/00 ,  C07H21/02

    CPC分类号： C07H21/00 ,  A61K31/712 ,  A61K38/00 ,  C12N15/1131 ,  C12N2310/11 ,  C12N2310/3231

    摘要： An antisense oligonucleotide derivative against HCV is provided which contains one or more nucleotide analogue units having a modified sugar portion and represented by the following general formula where B denotes a pyrimidine or purine nucleic acid base or an analogue thereof. The derivative of the present invention is an antisense against hepatitis C virus (HCV) gene, binds to HCV-RNA with high affinity within cells, can control and inhibit the expression of its gene with high efficiency, and shows high resistance to nucleases. The BNA antisense oligonucleotide of the present invention is also effective in an antisense method targeting HCV, no matter what secondary structures, such as loops or stems, in a target RNA nucleic acid are.

    摘要翻译： 提供了针对HCV的反义寡核苷酸衍生物，其含有一个或多个具有修饰的糖部分的核苷酸类似物单元，并由以下通式表示，其中B表示嘧啶或嘌呤核酸碱基或其类似物。 本发明的衍生物是针对丙型肝炎病毒（HCV）基因的反义，与细胞内高亲和力的HCV-RNA结合，可以高效控制和抑制其基因的表达，并显示出对核酸酶的高抗性。 本发明的BNA反义寡核苷酸在靶向HCV的反义方法中也是有效的，无论靶RNA核酸中的二级结构如环或茎如何。

    Bicyclonucleoside and oligonucleotide analogues
    8.
    再颁专利
    Bicyclonucleoside and oligonucleotide analogues 失效
    双环核苷和寡核苷酸类似物

    公开(公告)号：USRE44779E1

    公开(公告)日：2014-02-25

    申请号：US13533781

    申请日：2012-06-26

    申请人： Takeshi Imanishi ,  Satoshi Obika

    发明人： Takeshi Imanishi ,  Satoshi Obika

    IPC分类号： C07H19/06 ,  C07H19/16 ,  C07H21/00

    CPC分类号： C07H19/16 ,  C07H19/06

    摘要： An oligo- or polynucleotide analogue having one or more structures of the general formula where B is a pyrimidine or purine nucleic acid base, or an analogue thereof, is disclosed. The use of this analogue provides an oligonucleotide analogue antisense molecule, which is minimally hydrolyzable with an enzyme in vivo, has a high sense strand binding ability, and is easily synthesized.

    摘要翻译： 公开了具有一个或多个通式结构的寡核苷酸或多核苷酸类似物，其中B是嘧啶或嘌呤核酸碱基，或其类似物。 该类似物的使用提供了寡核苷酸类似物反义分子，其在体内用酶最低限度地水解，具有高有义链结合能力，并且易于合成。

    Nucleoside analogues whose sugar moieties are bound in s-form and oligonucleotide derivatives comprising nucleotide analogues thereof
    10.
    发明申请
    Nucleoside analogues whose sugar moieties are bound in s-form and oligonucleotide derivatives comprising nucleotide analogues thereof 审中-公开
    其糖部分以S-形式结合的核苷类似物和包含其核苷酸类似物的寡核苷酸衍生物

    公开(公告)号：US20050176941A1

    公开(公告)日：2005-08-11

    申请号：US10504479

    申请日：2003-02-13

    申请人： Takeshi Imanishi ,  Satoshi Obika

    发明人： Takeshi Imanishi ,  Satoshi Obika

    IPC分类号： A61K31/712 ,  A61K48/00 ,  A61P31/16 ,  A61P35/00 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  C07H21/04 ,  C07D473/10 ,  C07D493/02 ,  C07H19/00 ,  C07H19/048

    CPC分类号： C07H19/06 ,  A61K31/712 ,  A61K48/00 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  Y02P20/55

    摘要： Compounds of the following general formula (1) and salts thereof: where A represents an alkylene group having 1 to 2 carbon atoms, etc.; B represents an aromatic heterocyclic group which may have a substituent, etc.; R1 and R2 each represent a hydrogen atom, a protective group for a hydroxyl group for synthesis of nucleic acid, a phosphate group, or —P(R4)R5 [where R4 and R5 are the same or different, and each represent a hydroxyl group, a hydroxyl group protected with a protective group for synthesis of nucleic acid, a mercapto group, a mercapto group protected with a protective group for synthesis of nucleic acid, etc.]; and R3 represents a hydrogen atom, a halogen atom, a hydroxyl group, a hydroxyl group protected with a protective group for synthesis of nucleic acid, etc. These compounds are useful for producing oligonucleotide analogues useful for the antisense method, antigene method, etc., and for producing their intermediates.

    摘要翻译： 下列通式（1）的化合物及其盐：其中A表示碳原子数1〜2的亚烷基等; B表示可具有取代基的芳香族杂环基等。 R 1和R 2各自表示氢原子，用于合成核酸的羟基的保护基，磷酸基或-P（R） R 5）R 5其中R 4和R 5相同或不同，并且各自表示羟基， 用保护基团保护的羟基，用于合成核酸，巯基，用保护基保护的用于合成核酸的巯基等]。 R 3表示氢原子，卤素原子，羟基，被保护基团保护的羟基，用于合成核酸等。这些化合物可用于制备可用于核酸的寡核苷酸类似物 反义方法，反苯乙烯法等，并制备其中间体。