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11. 发明授权

US06521744B1 2- or 3-dimensional geometric structures 有权
标题翻译：二维或三维几何结构
公开(公告)号：US06521744B1
公开(公告)日：2003-02-18
申请号：US09656759
申请日：2000-09-07
申请人： Hans-Georg Batz , Troels Koch , Henrik Frydenlund Hansen
发明人： Hans-Georg Batz , Troels Koch , Henrik Frydenlund Hansen
IPC分类号： C07H1900
CPC分类号： B82Y30/00 , C07H21/00 , C07K14/003 , Y10S977/704 , Y10S977/728 , Y10S977/734 , Y10S977/753 , Y10S977/792 , Y10S977/80 , Y10S977/906
摘要： Nucleic acid analogs provide a particularly useful tool for the preparation of complex polymeric structures of defined geometry because they are relatively stable to reaction conditions for the preparation of such structures and provide the opportunity to induce reactive groups which would not be possible with usual nucleic acids.
摘要翻译：核酸类似物为制备具有规定几何结构的复合聚合物结构提供了特别有用的工具，因为它们对于制备这种结构的反应条件相对稳定，并且提供诱导与常规核酸不可能的反应性基团的机会。

12. 发明授权

US09045518B2 Amino-LNA, thio-LNA and alpha-L-oxy-LN 有权
标题翻译：氨基-LNA，硫代-LNA和α-L-氧 - LN
公开(公告)号：US09045518B2
公开(公告)日：2015-06-02
申请号：US10535472
申请日：2003-11-18
申请人： Signe M. Christensen , Nikolaj Dam Mikkelsen , Miriam Frieden , Henrik Frydenlund Hansen , Troels Koch , Daniel Sejer Pedersen , Christoph Rosenbohm , Charlotte Albaek Thrue , Majken Westergaard
发明人： Signe M. Christensen , Nikolaj Dam Mikkelsen , Miriam Frieden , Henrik Frydenlund Hansen , Troels Koch , Daniel Sejer Pedersen , Christoph Rosenbohm , Charlotte Albaek Thrue , Majken Westergaard
IPC分类号： C07H21/04 , C07H19/16 , A61K31/7088 , C07H21/00 , C12N15/11 , C07H19/04 , C12N15/113 , C07H19/06 , C07H21/02
CPC分类号： C12N15/113 , A61K31/7088 , C07H19/04 , C07H19/06 , C07H19/16 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/111 , C12N15/1137 , C12N2310/11 , C12N2310/315 , C12N2310/3231 , C12N2310/341 , C12N2310/344 , C12N2320/30 , C12N2320/51
摘要： A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.
摘要翻译：一种新型的药物，其包含可用于反义治疗的锁定核酸（LNA）。这些新型寡核苷酸具有改善的反义性质。所述新型寡核苷酸由至少一种选自β-D-thio / amino-LNA或α-L-氧基/硫代/氨基-LNA的LNA组成。包含LNA的寡核苷酸还可以包括DNA和/或RNA核苷酸。

13. 发明申请

US20100062994A1 Adenosine Receptor Antagonists 审中-公开
标题翻译：腺苷受体拮抗剂
公开(公告)号：US20100062994A1
公开(公告)日：2010-03-11
申请号：US12373640
申请日：2007-07-06
申请人： Jacob Ravn , Christoph Rosenbohm , Katrine Qvortrup , Troels Koch
发明人： Jacob Ravn , Christoph Rosenbohm , Katrine Qvortrup , Troels Koch
IPC分类号： A61K31/52 , C07H19/167 , A61P43/00
CPC分类号： C07D473/00 , C07H19/16
摘要： The present application discloses locked nucleoside compounds of the Formula I which act as antagonists of adenosine receptors, in particular the adenosine A3 receptor, and the use of such adenosine A3 receptor compounds in medicine, e.g. for the treatment or alleviation or prophylaxis of selected from the group consisting of pain; inflammatory diseases, arthritis, multiple sclerosis, inflammation, asthma and psoriasis; gastro-intestinal disorders; allergy; disorders associated with mast cell or eosinophil activation and degranulation; cardio-vascular disorders; cutaneous diseases; wound healing; opthalmological disorders; respiratory disorders; kidney diseases; central nervous system disorders; Alzheimer's disease, Creutzfeldt-Jacob disease, Huntington's disease and Parkinson's disease; trauma and seizure; diabetes; osteoporosis; diseases of the immune system; cancers, infections; high blood pressure, locomotor hyperactivity, hypertension and depression; acute hypoxia; neonatal hypoxia, hypoxia and chronic hypoxia; and infertility.
摘要翻译：本申请公开了作为腺苷受体，特别是腺苷A3受体的拮抗剂的式I的锁定核苷化合物，以及这些腺苷A3受体化合物在医学中的应用。用于治疗或减轻或预防选自疼痛的组; 炎性疾病，关节炎，多发性硬化，炎症，哮喘和银屑病; 胃肠道疾病; 过敏; 与肥大细胞或嗜酸性粒细胞活化和脱颗粒相关的疾病; 心血管疾病; 皮肤病; 伤口愈合; 眼科疾病; 呼吸系统疾病; 肾脏疾病; 中枢神经系统疾病; 阿尔茨海默病，克雅氏病，亨廷顿氏病和帕金森病; 创伤和癫痫发作; 糖尿病; 骨质疏松症免疫系统疾病; 癌症，感染; 高血压，运动过度活动，高血压和抑郁; 急性缺氧新生儿缺氧，缺氧和慢性缺氧; 和不育症。

14. 发明申请

US20080249039A1 Modified Short Interfering Rna (Modified Sirna) 审中-公开
标题翻译：改良短干扰Rna（修饰Sirna）
公开(公告)号：US20080249039A1
公开(公告)日：2008-10-09
申请号：US10587775
申请日：2005-01-28
申请人： Joacim Elmen , Claes Wahlestedt , Zicai Liang , Henrik Orum , Troels Koch
发明人： Joacim Elmen , Claes Wahlestedt , Zicai Liang , Henrik Orum , Troels Koch
IPC分类号： A61K31/7105 , C07H21/04
CPC分类号： C07H21/04 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/315 , C12N2310/3231 , C12N2310/3341 , C12N2320/51
摘要： The present invention is directed to modified siRNA which are significantly impaired in their ability to support cleavage of mRNA when incorporated into a RISC complex. Such modified siRNA may be useful as therapeutic agents, e.g., in the treatment of various cancer forms. More particularly, the modified siRNA comprises a sense strand and an antisense strand, wherein the sense strand contains a modified RNA nucleotide in at least one of positions 8-14, calculated from the 5′-end.
摘要翻译：本发明涉及修饰的siRNA，当掺入到RISC复合物中时，其显着损害其支持mRNA切割的能力。这样的修饰的siRNA可用作治疗剂，例如治疗各种癌症形式。更具体地，修饰的siRNA包含有义链和反义链，其中有义链含有从5'-末端计算的位置8-14中的至少一个中的修饰的RNA核苷酸。

15. 发明申请

US20070191294A1 Short interfering rna (sirna) analogues 有权
标题翻译：短干扰rna（sirna）类似物
公开(公告)号：US20070191294A1
公开(公告)日：2007-08-16
申请号：US10550152
申请日：2004-03-22
申请人： Joacim Elmen , Claes Wahlestedt , Zicai Liang , Anders Sorensen , Henrik Orum , Troels Koch
发明人： Joacim Elmen , Claes Wahlestedt , Zicai Liang , Anders Sorensen , Henrik Orum , Troels Koch
IPC分类号： A61K48/00 , A61K31/7072 , A61K31/704 , A61K38/14 , A61K31/337 , A61K38/09
CPC分类号： C12N15/1131 , A61K38/00 , A61K38/09 , A61K38/2013 , A61K38/212 , A61K38/31 , C12N15/111 , C12N15/1135 , C12N2310/14 , C12N2310/315 , C12N2310/3231 , C12N2310/3233 , C12N2310/3341 , C12N2310/53 , C12N2320/51 , C12N2330/30 , Y02A50/465 , A61K2300/00
摘要： The present invention is directed to novel double-stranded short interfering (siRNA) analogues comprising locked nucleic acid (LNA) monomers. Such compounds induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). The compounds disclosed herein has improved properties compared to non-modified siRNAs and may, accordingly, be useful as therapeutic agents, e.g., in the treatment of various cancer forms. More particularly, the present invention is directed to siRNA analogues comprising a sense strand and an antisense strand, wherein each strand comprises 12-35 nucleotides and wherein the siRNA analogues comprise at least one locked nucleic acid (LNA) monomer.
摘要翻译：本发明涉及包含锁定核酸（LNA）单体的新型双链短干扰（siRNA）类似物。这种化合物通过称为RNA干扰（RNAi）的方法在许多生物体中诱导序列特异性的转录后基因沉默。本文公开的化合物与未修饰的siRNA相比具有改善的性质，因此可用作治疗剂，例如用于治疗各种癌症形式。更具体地，本发明涉及包含有义链和反义链的siRNA类似物，其中每条链包含12-35个核苷酸，并且其中siRNA类似物包含至少一个锁定核酸（LNA）单体。

16. 发明授权

US06998484B2 Synthesis of purine locked nucleic acid analogues 有权
公开(公告)号：US06998484B2
公开(公告)日：2006-02-14
申请号：US09971364
申请日：2001-10-04
申请人： Troels Koch , Flemming Ressig Jensen
发明人： Troels Koch , Flemming Ressig Jensen
IPC分类号： C07D473/18 , C07D473/40 , C07D473/16 , C07D473/22
CPC分类号： C07H19/04
摘要： The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.

17. 发明授权

US06858726B2 Synthesis of allofuranose 有权
标题翻译：异戊二烯的合成
公开(公告)号：US06858726B2
公开(公告)日：2005-02-22
申请号：US10165768
申请日：2002-06-07
申请人： Troels Koch , Henrik Frydenlund Hansen
发明人： Troels Koch , Henrik Frydenlund Hansen
IPC分类号： C07H1/00
CPC分类号： C07H1/00
摘要： The present invention provides a novel strategy for the synthesis of allofuranose using glucofuranose as starting material in a one-pot reaction. The novel finding is that it is possible to carry out the oxidation of 1,2:5,6-di-O-isopropylidene-α-D-glucofuranose with DMSO/acetic anhydride and a reduction reaction in one pot obtaining high yields of recrystallised and analytical pure 1,2:5,6-di-O-isopropylidene-α-D-allofuranose.
摘要翻译：本发明提供了在一锅反应中使用呋喃糖作为原料合成异戊二醛的新策略。该新发现是可以用DMSO /乙酸酐进行1,2：5,6-二-O-异亚丙基-α-D-吡喃葡萄糖的氧化，并在一锅中进行还原反应，得到高产率的重结晶和分析纯的1,2：5,6-二-O-异亚丙基-α-D-异戊二醛。

18. 发明授权

US06310179B1 2-or 3-dimensional geometric structures 失效
标题翻译： 2维或3维几何结构
公开(公告)号：US06310179B1
公开(公告)日：2001-10-30
申请号：US09087514
申请日：1998-05-28
申请人： Hans-Georg Batz , Troels Koch , Henrik Frydenlund Hansen
发明人： Hans-Georg Batz , Troels Koch , Henrik Frydenlund Hansen
IPC分类号： C07K104
CPC分类号： B82Y30/00 , C07H21/00 , C07K14/003 , Y10S977/704 , Y10S977/728 , Y10S977/734 , Y10S977/753 , Y10S977/792 , Y10S977/80 , Y10S977/906
摘要： Nucleic acid analogues provide a particularly useful tool for the preparation of complex polymeric structures of defined geometry because they are relatively stable to reaction conditions for the preparation of such structures and provide the opportunity to introduce reactive groups which would not be possible with usual nucleic acids. These supramolecular structures can be used to form fine networks in nanometer size, for the preparation of e.g., computer chips, new materials/polymers with conductivity and/or insulator properties, and robot arms in nanometer scale.
摘要翻译：核酸类似物为制备具有规定几何形状的复合聚合物结构提供了特别有用的工具，因为它们对于制备这种结构的反应条件相对稳定，并且提供引入与常规核酸不可能的反应性基团的机会。这些超分子结构可用于形成纳米尺寸的精细网络，用于制备例如计算机芯片，具有导电性和/或绝缘体特性的新材料/聚合物以及纳米尺度的机器人手臂。

19. 发明授权

US08492390B2 Synthesis of locked nucleic acid derivatives 有权
标题翻译：锁定核酸衍生物的合成
公开(公告)号：US08492390B2
公开(公告)日：2013-07-23
申请号：US13336303
申请日：2011-12-23
申请人： Mads Detlef Sorensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
发明人： Mads Detlef Sorensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
IPC分类号： C07D473/06 , C07D473/16 , C07D473/18 , C07D473/34 , C07D473/40 , C07D239/70 , C07D239/52 , A61P31/22
CPC分类号： C07H19/20 , C07H19/00 , C07H19/04 , C07H19/048
摘要： The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α-L-oxy-LNA, amino-LNA, α-L-amino-LNA, thio-LNA, α-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
摘要翻译：本发明涉及一种用于合成锁定核酸衍生物的新策略，例如α-L-氧-LNA，氨基-LNA，α-L-氨基-LNA，硫代-LNA，α-L-硫代-LNA，硒代-LNA和亚甲基LNA，其利用也可以产生其他LNA类似物如oxy-LNA的中间体提供可伸缩的高产反应。此外，式X的化合物是可能与各种亲核试剂反应的重要中间体，导致各种各样的LNA类似物。

20. 发明申请

US20100216983A1 SYNTHESIS OF LOCKED NUCLEIC ACID DERIVATIVES 有权
标题翻译：闭锁核酸衍生物的合成
公开(公告)号：US20100216983A1
公开(公告)日：2010-08-26
申请号：US12534711
申请日：2009-08-03
申请人： Mads Detlef Sorensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
发明人： Mads Detlef Sorensen , Jesper Wengel , Troels Koch , Signe M. Christensen , Christoph Rosenbohm , Daniel Sejer Pedersen
IPC分类号： C07H21/00
CPC分类号： C07H19/20 , C07H19/00 , C07H19/04 , C07H19/048
摘要： The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α-L-oxy-LNA, amino-LNA, α-L-amino-LNA, thio-LNA, α-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
摘要翻译：本发明涉及一种合成锁定核酸衍生物的新策略，如α-L-氧-LNA，氨基-LNA，α-L-氨基-LNA，硫代-LNA，α-L-硫代-LNA，硒代-LNA和亚甲基LNA，其利用也可以产生其他LNA类似物如oxy-LNA的中间体提供可伸缩的高产反应。此外，式X的化合物是可能与各种亲核试剂反应的重要中间体，导致各种各样的LNA类似物。

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