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1. 发明申请

WO2017157672A1 ACYL-PROTECTED L-LNA-GUANOSINE MONOMERS 审中-公开
标题翻译： ACYL保护的L-LNA-鸟苷单体
公开(公告)号：WO2017157672A1
公开(公告)日：2017-09-21
申请号：PCT/EP2017/054841
申请日：2017-03-02
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： ALBAEK, Nanna , FUNDER, Erik , RAVN, Jacob
IPC分类号： C07H19/06
CPC分类号： C07H19/06
摘要： The present invention relates to the field of stereodefined phosphorothioate oligonucleotidess and to nucleoside monomers and methods of synthesis thereof. Herein are disclosed acyl protected L-LNA-G monomers which have improved solubility and stability characteristics, and result in improved efficacy in oligonucleotide synthesis.
摘要翻译：本发明涉及立体定义的硫代磷酸寡核苷酸和核苷单体领域及其合成方法。本文公开了酰基保护的L-LNA-G单体，其具有改善的溶解度和稳定性特征，并且导致寡核苷酸合成中的功效提高。

2. 发明申请

WO2017178656A1 TRITYL-MONO-GalNAc COMPOUNDS AND THEIR USE 审中-公开
标题翻译： TRITYL-MONO-GalNAc化合物及其用途
公开(公告)号：WO2017178656A1
公开(公告)日：2017-10-19
申请号：PCT/EP2017/059080
申请日：2017-04-18
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： ALBAEK, Nanna , RAVN, Jacob
IPC分类号： C07H15/18 , C07H21/00 , A61K31/7088 , A61P3/06 , A61P31/12
摘要： This invention generally relates to the field of phosphoramidite derivatives. In particular, the invention relates to N- Acetylgalactosamine (GalNAc) compounds, in particular phosphoramidite or phosphonoamidite molecules of formula (I) with only one GalNAc moiety (formula II) and to conjugates of nucleic acid molecules with such N-Acetylgalactosamine containing molecules. Also provided are methods for preparation of these molecules and possible uses thereof, in particular in medicine. Wherein R 1 is H or C 1 - 6 alkyl; R 2 is a triphenylmethyl-based hydroxyl protecting group R 3 is a phosphorus-containing group, particularly a phosphoramidite or a phosphonoamidite group, and K is represented by the general formula (II).
摘要翻译：本发明一般涉及亚磷酰胺衍生物领域。特别地，本发明涉及N-乙酰半乳糖胺（GalNAc）化合物，特别是仅具有一个GalNAc部分（式II）的式（I）的亚磷酰胺或膦酰胺化物分子，以及核酸分子与这种含有N-乙酰半乳糖胺的分子的偶联物。还提供了用于制备这些分子的方法及其可能的用途，特别是在医学中。其中R 1是H或C 1 -C 6烷基; R 2是基于三苯甲基的羟基保护基团R 3是含磷基团，特别是亚磷酰胺或亚膦酰胺基团，并且K由通式（ II）。

3. 发明申请

WO2016096938A1 CHIRAL TOXICITY SCREENING METHOD 审中-公开
标题翻译： CHIRAL毒性筛选方法
公开(公告)号：WO2016096938A1
公开(公告)日：2016-06-23
申请号：PCT/EP2015/079915
申请日：2015-12-16
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： ALBAEK, Nanna , GUBLER, Marcel , HAGEDORN, Peter , HANSEN, Henrik, Frydenlund , KOCH, Troels , MOISAN, Annie , RAVN, Jacob , ROSENBOHM, Christoph , SEWING, Sabine
IPC分类号： C12N15/11 , C12N15/113
CPC分类号： C12N15/113 , C12N15/111 , C12N2310/11 , C12N2310/315 , C12N2310/3231 , C12N2310/341 , C12N2310/345 , C12N2310/346 , C12N2320/53 , C12N2330/31 , G01N33/5014 , G01N33/5088
摘要： The invention relates to a method of identifying stereodefined phosphrothioate oligonucleotide variants with reduced toxicity by creating and screening libraries of stereodefined chiral phosphorothioate variants for compounds with reduced toxicity, either in vitro or in vivo.
摘要翻译：本发明涉及通过在体外或体内产生和筛选具有降低的毒性的化合物的立体定向手性硫代磷酸酯变体文库来鉴定具有降低的毒性的立体定向磷酸硫酸酯寡核苷酸变体的方法。

4. 发明申请

WO2017032726A1 LNA-G PROCESS 审中-公开
标题翻译： LNA-G工艺
公开(公告)号：WO2017032726A1
公开(公告)日：2017-03-02
申请号：PCT/EP2016/069765
申请日：2016-08-22
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： HANSEN, Dennis Jul , HOERNSCHEMEYER, Joerg , RAVN, Jacob , ROSENBOHM, Christoph
IPC分类号： C12N15/11 , C07D473/18
CPC分类号： C12N15/111 , A61K31/7088 , C07H1/00 , C07H21/00 , C12N2310/3231 , C12N2310/336 , C12N2310/351 , C12N2330/30
摘要： Recent advancements in LNA oligonucleotides include the use of amine linkers to link an LNA antisense oligonucleotide to a conjugate group. For example please see WO2014/118267. The present invention originates from the identification of a problem when de-protecting LNA oligonucleotides which comprise an aliphatic amine group and DMF protected LNA G nucleoside, which results in the production of a +28 Da impurity. This problem is solved by using acyl protection groups on the exocyclic nitrogen of the LNA-G residue, rather than the standard DMF protection group.
摘要翻译： LNA寡核苷酸的最新进展包括使用胺连接体将LNA反义寡核苷酸连接至缀合基团。例如，请参见WO2014 / 118267。本发明源于鉴定当包含脂族胺基和DMF保护的LNA G核苷的LNA寡核苷酸脱保护时导致产生+ 28Da杂质的问题。通过在LNA-G残基的环外氮上使用酰基保护基，而不是标准的DMF保护基来解决这个问题。

5. 发明申请

WO2021249993A1 GUANOSINE ANALOGUES FOR USE IN THERAPEUTIC POLYNUCLEOTIDES 审中-公开
公开(公告)号：WO2021249993A1
公开(公告)日：2021-12-16
申请号：PCT/EP2021/065266
申请日：2021-06-08
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： ALBAEK, Nanna , HAGEDORN, Peter , LADEFOGED, Mette , PEDERSEN, Lykke , RAVN, Jacob
IPC分类号： C12N15/113 , A61K31/7115 , C12Q1/68 , A61P25/00 , C12N15/111 , C12N2310/11 , C12N2310/14 , C12N2310/315 , C12N2310/3231 , C12N2310/336 , C12N2310/341 , C12N2320/53
摘要： The present invention relates to a polynucleotide that comprises at least one phosphorothioate internucleoside linkage and at least one guanosine analogue comprising a guanine nucleobase analogue selected from the group consisting of: formula (I) and formula (II). Polynucleotides comprising such guanosine analogues show a relative reduced neurotoxicity compared to polynucleotides with natural guanosine.

6. 发明申请

WO2016079181A1 LNA GAPMER OLIGONUCLEOTIDES COMPRISING CHIRAL PHOSPHOROTHIOATE LINKAGES 审中-公开
标题翻译： LNA GAPMER OLIGONUCLEOTIDES包含CHIRAL PHOSPHOROTHIOATE链接
公开(公告)号：WO2016079181A1
公开(公告)日：2016-05-26
申请号：PCT/EP2015/076967
申请日：2015-11-18
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： ALBÆK, Nanna , HANSEN, Henrik Frydenlund , KOCH, Troels , RAVN, Jacob , ROSENBOHM, Christoph , HAGEDORN, Peter , SEWING, Sabine , MOISAN, Annie
IPC分类号： C07H21/00 , A61K31/712 , A61K31/7125
CPC分类号： C12N15/117 , C07H21/00 , C12N15/111 , C12N15/113 , C12N2310/11 , C12N2310/17 , C12N2310/315 , C12N2310/3231 , C12N2310/33 , C12N2310/341 , C12N2310/346 , C12N2310/351 , C12N2320/53 , C12N2330/30
摘要： The present relates to LNA gapmer antisense oligonucleotides which comprise stereodefined phosphoramidite linkages. The use of stereodefined phosphoramidite linkages in LNA gapmers has been found to provide enhanced RNaseH activity, and modifying stereospecificity enables the reduced toxicity, altered biodistribution, and enhanced mismatch discrimination.
摘要翻译：本发明涉及包含立体定向亚磷酰胺键的LNA gapmer反义寡核苷酸。已经发现在LNA间隙物中使用立体定向亚磷酰胺键可提供增强的RNA酶H活性，并且改变立体定向性使得能够降低毒性，改变生物分布和增强错配鉴别。

7. 发明申请

WO2015113922A1 POLY OLIGOMER COMPOUND WITH BIOCLEAVABLE CONJUGATES 审中-公开
标题翻译：具有生物相容性的聚低聚物化合物
公开(公告)号：WO2015113922A1
公开(公告)日：2015-08-06
申请号：PCT/EP2015/051442
申请日：2015-01-26
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： ALBÆK, Nanna , HANSEN, Henrik Frydenlund , KAMMLER, Susanne , LINDOW, Morten , RAVN, Jacob , TURNER, Mark
IPC分类号： C12N15/113
CPC分类号： C12N15/113 , C12N2310/113 , C12N2310/315 , C12N2310/341 , C12N2310/345 , C12N2310/351 , C12N2310/51
摘要： The invention relates to the field of oligonucleotide therapeutics, and in particular to poly oligo oligonucleotides conjugates where two or more antisense oligonucleotides are covalently linked by physiologically labile linkers, and to a biocleavable functional group such as a conjugate group.
摘要翻译：本发明涉及寡核苷酸治疗领域，特别涉及其中两个或更多个反义寡核苷酸通过生理不稳定连接体共价连接的聚寡核苷酸缀合物以及可生物可清除的官能团如共轭基团。

8. 发明申请

WO2019224172A1 NOVEL PROCESS FOR MAKING ALLOFURANOSE FROM GLUCOFURANOSE 审中-公开
公开(公告)号：WO2019224172A1
公开(公告)日：2019-11-28
申请号：PCT/EP2019/063044
申请日：2019-05-21
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： RAVN, Jacob , ROSENBOHM, Christoph , REDDY, Prasad
IPC分类号： C07H9/04 , C07H19/06 , C07H19/16
摘要： The present invention relates to the manufacture of allofuranose from glucofuranose as defined in the description and in the claim. Allofuranos is an intermediate in the manufacture of oligonucleotides which can be used as a medicament.

9. 发明申请

WO2017194498A1 ENHANCED COUPLING OF STEREODEFINED OXAZAPHOSPHOLIDINE PHOSPHORAMIDITE MONOMERS TO NUCLEOSIDE OR OLIGONUCLEOTIDE 审中-公开
标题翻译：立体限定的氮杂吗啉鎓亚磷酰胺单体与核苷或寡核苷酸的增强偶联
公开(公告)号：WO2017194498A1
公开(公告)日：2017-11-16
申请号：PCT/EP2017/060985
申请日：2017-05-09
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： RAVN, Jacob , FUNDER, Erik
IPC分类号： C07H1/02 , C07H19/06 , C07H19/16
摘要： The present invention relates to the field of stereodefined phosphorothioate oligonucleotides and to stereodefining nucleoside monomers and methods of synthesis of stereodefined oligonucleotides. Herein are disclosed solvent compositions which provide enhanced solubility and stability of stereodefining nucleoside monomers, and can be used to improve the coupling efficacy of such monomers in oligonucleotide synthesis.
摘要翻译：本发明涉及立体定义的硫代磷酸寡核苷酸领域，并涉及立体定义核苷单体和合成立体定义的寡核苷酸的方法。本文公开了提供立体定向核苷单体的增强的溶解性和稳定性的溶剂组合物，并且可用于改善这种单体在寡核苷酸合成中的偶联效率。

10. 发明申请

WO2016079183A1 LNA CHIRAL PHOSPHOROTHIOATES 审中-公开
公开(公告)号：WO2016079183A1
公开(公告)日：2016-05-26
申请号：PCT/EP2015/076971
申请日：2015-11-18
申请人： ROCHE INNOVATION CENTER COPENHAGEN A/S
发明人： ALBÆK, Nanna , HANSEN, Henrik Frydenlund , KOCH, Troels , RAVN, Jacob , ROSENBOHM, Christoph , HAGEDORN, Peter , SEWING, Sabine , MOISAN, Annie
IPC分类号： A61K31/7125 , C07H21/00
CPC分类号： C12N15/117 , C07H21/00 , C12N15/111 , C12N15/113 , C12N2310/11 , C12N2310/17 , C12N2310/315 , C12N2310/3231 , C12N2310/33 , C12N2310/341 , C12N2310/346 , C12N2310/351 , C12N2320/53 , C12N2330/30
摘要： The present invention provides stereodefined phosphorothioate LNA oligonucleotide, comprising at least one stereodefined phosphorothioate linkage between a LNA nucleoside and a subsequent (3') nucleoside.
摘要翻译：本发明提供立体定向硫代磷酸酯LNA寡核苷酸，其包含LNA核苷和随后的（3'）核苷之间的至少一种立体定向的硫代磷酸酯键。

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