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公开(公告)号：US11591594B2
公开(公告)日：2023-02-28
申请号：US16812233
申请日：2020-03-06
IPC分类号： C12N15/11 , C07H21/00 , C07H1/00 , C12N15/113
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/I18267. 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.
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公开(公告)号：US20220112493A1
公开(公告)日：2022-04-14
申请号：US17405706
申请日：2021-08-18
IPC分类号： C12N15/113
摘要： The invention relates to a single-stranded antisense gapmer oligonucleotide comprising at least one dinucleoside of formula (I) wherein (A1), (A2) and A are as defined in the description and in the claims. The oligonucleotide according to the invention can be used as a medicament.
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公开(公告)号：US20210378652A1
公开(公告)日：2021-12-09
申请号：US17303890
申请日：2021-06-09
发明人： Richard E. OLSON , Brian R. ANDERSON , Peter HAGEDORN , Marianne Lerbech JENSEN , Ivar M. MCDONALD , Stephen E. MERCER
摘要： The present disclosure relates to antisense oligonucleotides, which target CAMK2D mRNA in a cell, leading to reduced expression of CAMK2D protein. Reduction of CAMK2D protein expression is beneficial for the treatment of certain medical disorders, e.g., cardiovascular-related diseases or disorders.
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公开(公告)号：US20210309690A1
公开(公告)日：2021-10-07
申请号：US16320918
申请日：2017-07-25
IPC分类号： C07H21/00
摘要： The invention relates to a process for the manufacture of an oligonucleotide comprising at least one non-chiral phosphorothioate intemucleoside linkage of formula (I) wherein R1 is as defined in the description and in the claims.
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公开(公告)号：US20210270845A1
公开(公告)日：2021-09-02
申请号：US17183273
申请日：2021-02-23
发明人： Jesper Worm , Lukasz Kielpinski
IPC分类号： G01N33/68 , C12N15/113
摘要： The invention relates to the field of secondary markers for microRNA activity, and in particular the invention relates to the identification of Serpine1 as a mRNA which is repressed by microRNA-134 in neuronal cells, and the use of Serpine1 mRNA or protein as a biomarker for microRNA-134 modulation, such as a biomarker for antisense oligonucleotide inhibitors of microRNA-134.
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公开(公告)号：US20210095277A1
公开(公告)日：2021-04-01
申请号：US15733392
申请日：2019-01-16
IPC分类号： C12N15/113
摘要： The present invention relates to antisense LNA oligonucleotides (oligomers) complementary to SREBF1 pre-mRNA intron and exon sequences, which are capable of inhibiting the expression of SREBP1 protein. Inhibition of SREBF1 expression is beneficial for a range of medical disorders including cardiovascular disease, type 2 diabetes, fatty liver, metabolic diseases, and cancer.
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公开(公告)号：US20210040137A1
公开(公告)日：2021-02-11
申请号：US16805618
申请日：2020-02-28
摘要： The present invention relates to the field of oligonucleotide conjugates and to methods of synthesis thereof. In the present method a low-water content solvent environment allows a more efficient conjugation, reducing the amount of conjugate moiety needed and increasing the conjugation reaction speed.
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公开(公告)号：US20200339982A1
公开(公告)日：2020-10-29
申请号：US15733307
申请日：2018-12-21
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 medicament.
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公开(公告)号：US20200318109A1
公开(公告)日：2020-10-08
申请号：US16812233
申请日：2020-03-06
IPC分类号： C12N15/11 , C07H21/00 , C07H1/00 , C12N15/113
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/I 18267. 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.
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公开(公告)号：US20200216845A1
公开(公告)日：2020-07-09
申请号：US16477656
申请日：2018-01-10
IPC分类号： C12N15/113
摘要： The present invention relates to antisense oligonucleotides that are capable of modulating expression of RelA in a target cell. The oligonucleotides are complementary to mammalian RELA pre-m RNA intron sequence. The present invention further relates to conjugates of the oligonucleotide and pharmaceutical compositions and methods for treatment of cancer, inflammation or autoimmune diseases using the oligonucleotide.
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