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公开(公告)号：US11597926B2
公开(公告)日：2023-03-07
申请号：US15733302
申请日：2018-12-21
发明人： Konrad Bleicher , Joerg Duschmalé , Martina Brigitte Duschmalé , Henrik Frydenlund Hansen , Troels Koch , Meiling Li , Adrian Schaeublin , Xi Shu , Yong Wu
IPC分类号： C07H19/10 , C07H19/20 , C07H21/04 , C12N15/113 , C07H1/00
摘要： The present invention relates to a compound of formula (II) or (IIb) Wherein X, Y, Rx, Ry, R5 and Nu are as defined in the description and in the claims. The compound of formula (II) can be used in the manufacture of oligonucleotides.
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52.发明授权公开(公告)号：US11591362B2
公开(公告)日：2023-02-28
申请号：US16497952
申请日：2018-03-20
摘要： The present invention relates to the field of stereodefined phosphorothioate oligonucleotides and to stereodefining nucleoside monomers comprising an amine containing chiral auxiliary group, and methods of orthogonally protecting the nitrogen of chiral auxiliaries during oligonucleotide synthesis, preventing post elongation chain cleavage, increasing yield and purity of stereodefined phosphorothioate oligonucleotides.
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公开(公告)号：US20230002762A1
公开(公告)日：2023-01-05
申请号：US17720676
申请日：2022-04-14
发明人： Konrad Bleicher , Henrik Frydenlund HANSEN , Troels KOCH , Jesper WORM , Adrian SCHAEUBLIN , Erik FUNDER , Joerg DUSCHMALÉ , Lars JOENSON , Meiling LI , Martina Brigitte DUSCHMALÉ , Yong WU , Xi SHU
摘要： The present invention relates to an oligonucleotide comprising at least one phosphorodithioate internucleoside linkage of formula (I) (I) as defined in the description and in the claim. The oligonucleotide of the invention can be used as a medicement.
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公开(公告)号：US20210363222A1
公开(公告)日：2021-11-25
申请号：US17135980
申请日：2020-12-28
发明人： Henrik Orum , Peter L. Sazani
IPC分类号： C07K14/705 , C12N15/11 , C12N15/113 , C07H21/04 , C07K14/715
摘要： The present invention relates to tumor necrosis factor (TNF) antagonists and corresponding nucleic acids derived from tumor necrosis factor receptors (TNFRs) and their use in the treatment of inflammatory diseases. These proteins are soluble secreted decoy receptors that bind to TNF and prevent TNF from signaling to cells. In particular, the proteins are mammalian TNFRs that lack exon 7 and which can bind TNF and can act as a TNF antagonist.
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公开(公告)号：US11091764B2
公开(公告)日：2021-08-17
申请号：US16560672
申请日：2019-09-04
发明人： Nanna Albæk , Maj Hedtjärn , Marie Wickstrom Lindholm , Niels Fisker Nielsen , Andreas Petri , Jacob Ravn
IPC分类号： C07H21/02 , A61K48/00 , C12N15/113 , A61K47/54 , A61K31/712
摘要： The present invention relates to oligomeric compounds and conjugates thereof that target Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) PCSK9 mRNA in a cell, leading to reduced expression of PCSK9. Reduction of PCSK9 expression is beneficial for a range of medical disorders, such as hypercholesterolemia and related disorders.
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公开(公告)号：US20210180065A1
公开(公告)日：2021-06-17
申请号：US17165841
申请日：2021-02-02
发明人： Richard E. OLSON , Angela M. CACACE , Jere E. MEREDITH, JR. , Nino DEVIDZE , James K. LOY , Carl J. BALDICK , Annapurna PENDRI , Ivar M. McDONALD , Peter HAGEDORN , Marianne Lerbech JENSEN
IPC分类号： C12N15/113
摘要： The present disclosure relates to antisense oligonucleotides, which target SNCA mRNA (e.g., at an intron exon junction) in a cell, leading to reduced expression of SNCA protein. Reduction of SNCA protein expression is beneficial for the treatment of certain medical disorders, e.g., a neurological disorder.
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公开(公告)号：US20210115438A1
公开(公告)日：2021-04-22
申请号：US15733302
申请日：2018-12-21
发明人： Konrad BLEICHER , Joerg DUSCHMALÉ , Martina Brigitte DUSCHMALÉ , Henrik Frydenlund HANSEN , Troels KOCH , Meiling LI , Adrian SCHAEUBLIN , Xi SHU , Yong WU
IPC分类号： C12N15/113 , C07H19/10 , C07H19/20 , C07H21/04 , C07H1/00
摘要： The present invention relates to a compound of formula (II) or (IIb) Wherein X, Y, Rx, Ry, R5 and Nu are as defined in the description and in the claims. The compound of formula (II) can be used in the manufacture of oligonucleotides.
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公开(公告)号：US10955407B2
公开(公告)日：2021-03-23
申请号：US16068963
申请日：2016-10-19
摘要： The invention relates to methods for predicting the in vivo toxicity of oligonucleotides, such as antisense oligonucleotides using in vitro cell based assays based on gymnotically administering oligonucleotides to primary mammalian hepatocytes and subsequently measuring the levels of toxicity biomarkers such as the release of LDH into the cell culture media and/or intracellular ATP.
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公开(公告)号：US20210071181A1
公开(公告)日：2021-03-11
申请号：US17061534
申请日：2020-10-01
发明人： Joacim ELMEN , Phil KEARNEY , Sakari KAUPPINEN
IPC分类号： C12N15/113
摘要： The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 17 nucleobases which are complementary to human microRNAs. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the mIRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC.
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公开(公告)号：US09566293B2
公开(公告)日：2017-02-14
申请号：US14886860
申请日：2015-10-19
发明人： Gregroy Hardee , Ellen Marie Straarup , Marie Wickstrom Lindholm , Henrik Orum , Henrik Frydenlund Hansen
IPC分类号： C07H21/02 , C07H21/04 , A61K31/712 , C12N15/113 , A61K9/00
CPC分类号： A61K31/712 , A61K9/0053 , C12N15/113 , C12N15/1136 , C12N2310/11 , C12N2310/113 , C12N2310/315 , C12N2310/3231 , C12N2310/3341 , C12N2320/30
摘要： The invention provides for LNA oligomers, for the treatment of a metabolic or liver disorder, wherein the LNA oligomer is administered orally in a unit dose of less than 50 mgs/kg, wherein the LNA oligomer is administered in the presence of a penetration (permeation) enhancer.
摘要翻译： 本发明提供用于治疗代谢或肝病症的LNA寡聚体，其中所述LNA低聚物以小于50mg / kg的单位剂量口服给药，其中所述LNA低聚物在渗透（渗透 ）增强剂。
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