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1. 发明授权

US08680260B2 18F-labeled azide compound, reagent for 18F-labeling and method for 18F-labeling of alkyne compound using same 失效
标题翻译： 18F标记的叠氮化合物，用于18F标记的试剂和使用其的18E-标记炔化合物的方法
公开(公告)号：US08680260B2
公开(公告)日：2014-03-25
申请号：US13320421
申请日：2010-05-14
申请人： Yasuyoshi Watanabe , Masaaki Suzuki , Hisashi Doi , Takeshi Kuboyama , Satoshi Obika , Takeshi Imanishi
发明人： Yasuyoshi Watanabe , Masaaki Suzuki , Hisashi Doi , Takeshi Kuboyama , Satoshi Obika , Takeshi Imanishi
IPC分类号： C07H21/00
CPC分类号： A61K51/0453 , A61K51/0491 , C07B59/005 , C07B2200/05 , C07C247/16 , C07D249/06
摘要： The present invention provides an 18F-labeled azide compound usable in the Huisgen reaction which enables 18F-labeling although only a small quantity of alkyne compound is available as a counterpart substrate, more specifically the 18F-labeled azide compound enabling the PET to be applied to peptides or oligonucleotides and enabling the 18F-labeling of any sites of oligonucleotide other than the 5′ end or 3′ end thereof, a reagent for 18F-labeling, and a method for 18F-labeling of an alkyne compound using the same.
摘要翻译：本发明提供了可用于Huisgen反应的18F标记的叠氮化合物，其能够进行18F标记，尽管只有少量的炔化合物可用作对应的基质，更具体地说，18F-标记的叠氮化合物使PET能够应用于肽或寡核苷酸，并且能够进行除了5'末端或3'末端以外的寡核苷酸的任何位点的18F标记，用于18F标记的试剂，以及使用其的18E-标记的炔化合物的方法。

2. 发明申请

US20120101266A1 18F-LABELED AZIDE COMPOUND, REAGENT FOR 18F-LABELING AND METHOD FOR 18F-LABELING OF ALKYNE COMPOUND USING SAME 失效
标题翻译： 18F标记的AZIDE化合物，18F标记试剂和使用其的18K标记的烷基化合物的方法
公开(公告)号：US20120101266A1
公开(公告)日：2012-04-26
申请号：US13320421
申请日：2010-05-14
申请人： Yasuyoshi Watanabe , Masaaki Suzuki , Hisashi Doi , Takeshi Kuboyama , Satoshi Obika , Takeshi Imanichi
发明人： Yasuyoshi Watanabe , Masaaki Suzuki , Hisashi Doi , Takeshi Kuboyama , Satoshi Obika , Takeshi Imanichi
IPC分类号： C07H1/00 , C07D249/06 , C07D249/04
CPC分类号： A61K51/0453 , A61K51/0491 , C07B59/005 , C07B2200/05 , C07C247/16 , C07D249/06
摘要： [OBJECT]The present invention provides an 18F-labeled azide compound usable in the Huisgen reaction which enables 18F-labeling although only a small quantity of alkyne compound is available as a counterpart substrate, more specifically the 18F-labeled azide compound enabling the PET to be applied to peptides or oligonucleotides and enabling the 18F-labeling of any sites of oligonucleotide other than the 5′ end or 3′ end thereof, a reagent for 18F-labeling, and a method for 18F-labeling of an alkyne compound using the same.[SOLVING MEANS]An 18F-labeled azide compound according to the present invention is expressed by the following structural formula 1.[SELECTED DRAWING] None
摘要翻译：本发明提供了可用于Huisgen反应的18F标记的叠氮化合物，其能够进行18F标记，尽管只有少量的炔化合物可用作对应的底物，更具体地说，18F-标记的叠氮化合物使PET能够应用于肽或寡核苷酸，并且使得除了5'末端或3'末端以外的寡核苷酸的任何位点的18F标记，用于18F标记的试剂和使用其的18E-标记的炔化合物的方法。 [解决方案]根据本发明的18F标记的叠氮化合物由以下结构式1表示。[选择的图]无

3. 发明授权

US07994145B2 Bicyclonucleoside analogues 失效
标题翻译：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。

4. 发明授权

US09127280B2 Oligonucleotide, and therapeutic agent for dyslipidemia containing oligonucleotide as active ingredient 有权
标题翻译：寡核苷酸和含有寡核苷酸的血脂异常的治疗剂作为活性成分
公开(公告)号：US09127280B2
公开(公告)日：2015-09-08
申请号：US13819722
申请日：2011-08-31
申请人： Satoshi Obika , Takeshi Imanishi , Tsuyoshi Yamamoto , Keisuke Narukawa , Mariko Shiba , Tetsuji Yamaoka , Hidetaka Torigoe , Atsushi Yamashita , Yoichi Tachibana , Sachiro Kakinoki , Kiyomi Sasaki
发明人： Satoshi Obika , Takeshi Imanishi , Tsuyoshi Yamamoto , Keisuke Narukawa , Mariko Shiba , Tetsuji Yamaoka , Hidetaka Torigoe , Atsushi Yamashita , Yoichi Tachibana , Sachiro Kakinoki , Kiyomi Sasaki
IPC分类号： C07H21/04 , A61K31/70 , C12N15/113 , A61K9/00 , A61K9/06 , A61K31/712 , C12Q1/68
CPC分类号： C12N15/1137 , A61K9/0019 , A61K9/0021 , A61K9/06 , A61K31/712 , C12N2310/11 , C12N2310/3231 , C12N2310/351 , C12Y304/21
摘要： An object of the present invention is to provide an oligonucleotide useful as a therapeutic agent for dyslipidemia that has excellent binding affinity to the PCSK9 gene as well as stability and safety. The oligonucleotide of the present invention contains a sugar-modified nucleoside, the sugar-modified nucleoside has a bridging structure between 4′-position and 2′-position, and the oligonucleotide can bind to the human PCSK9 gene. Also, the present invention provides a therapeutic agent for dyslipidemia containing the oligonucleotide as an active ingredient, and the therapeutic agent preferably contains a bioabsorbable material as a carrier. The bioabsorbable material is preferably atelocollagen or peptide gel.
摘要翻译：本发明的目的是提供一种可用作血脂异常的治疗剂的寡核苷酸，其对PCSK9基因具有优异的结合亲和力以及稳定性和安全性。本发明的寡核苷酸含有糖修饰的核苷，糖修饰的核苷具有4'-位和2'-位之间的桥连结构，寡核苷酸可以结合人PCSK9基因。此外，本发明提供了含有寡核苷酸作为活性成分的血脂异常的治疗剂，优选以生物体吸收性材料为载体。生物可吸收材料优选为胶原蛋白或肽凝胶。

5. 发明申请

US20070167387A1 Novel artificial nucleic acids of n-o bond crosslinkage type 有权
标题翻译：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]。

6. 发明授权

US07217805B2 Bicyclonucleoside analogues 失效
标题翻译：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。

7. 发明申请

US20050059617A1 Novel anitsense oligonucleotide derivatives against to hepatitis c virus 审中-公开
标题翻译：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。

8. 发明授权

US07615619B2 Nucleoside analogues and oligonucleotide derivative comprising nucleotide analogue thereof 有权
标题翻译：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：US07615619B2
公开(公告)日：2009-11-10
申请号：US10504165
申请日：2003-02-13
申请人： Takeshi Imanishi , Satoshi Obika
发明人： Takeshi Imanishi , Satoshi Obika
IPC分类号： C07H21/00 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
CPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： A nucleotide analogue compound represented by formula (1) and salts thereof. In formula (1), A represents a direct bond, C1-4 alkylene, etc.; B represents an optionally substituted aromatic heterocyclic groups; and R1, R2, R3 and R4 each represents hydrogen, an amino-protecting group, a hydroxyl-protecting group, a phosphate group, or —P(R7)R8, wherein R7 and R8 each represents hydroxyl, protected hydroxyl, mercapto, protected mercapto, etc. The compounds are useful as nucleotide analogues for producing oligonucleotide analogues useful in an antisense method and for producing intermediates thereof.
摘要翻译：由式（1）表示的核苷酸类似物化合物及其盐。在式（1）中，A表示直接键，C 1-4亚烷基等; B表示任选取代的芳族杂环基; 并且R 1，R 2，R 3和R 4各自表示氢，氨基保护基，羟基保护基，磷酸基或-P（R 7）R 8，其中R 7和R 8各自表示羟基，被保护的羟基，巯基，受保护的巯基等。这些化合物可用作生产寡核苷酸类似物的核苷酸类似物，其可用于反义方法并用于制备其中间体。

9. 发明授权

US07427672B2 Artificial nucleic acids of n-o bond crosslinkage type 有权
标题翻译： n-o键交联型人造核酸
公开(公告)号：US07427672B2
公开(公告)日：2008-09-23
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： C07H19/00 , C07H21/00 , A01N43/04 , A61K31/70
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]。

10. 再颁专利

USRE44779E1 Bicyclonucleoside and oligonucleotide analogues 失效
标题翻译：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。

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