OLIGONUCLEOTIDES COMPRISING HOSPHORODITHIOATE INTERNUCLEOSIDE LINKAGE

To provide oligonucleotides with improved physiochemical and pharmacological properties.SOLUTION: Provided herein is an antisense gapmer oligonucleotide of formula (IA) or (IB) comprising at least one phosphorodithioate internucleoside linkage for inhibiting target RNA in a cell, where in the formul...

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Hauptverfasser: LARS JOENSON, ERIK FUNDER, KONRAD BLEICHER, HENRIK FRYDENLUND HANSEN, TROELS KOCH, WU YONG, MARTINA BRIGITTE DUSCHMALE, ADRIAN SCHAEUBLIN, JOERG DUSCHMALE, SHU XI, JESPER WORM, LI MEILING
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creator LARS JOENSON
ERIK FUNDER
KONRAD BLEICHER
HENRIK FRYDENLUND HANSEN
TROELS KOCH
WU YONG
MARTINA BRIGITTE DUSCHMALE
ADRIAN SCHAEUBLIN
JOERG DUSCHMALE
SHU XI
JESPER WORM
LI MEILING
description To provide oligonucleotides with improved physiochemical and pharmacological properties.SOLUTION: Provided herein is an antisense gapmer oligonucleotide of formula (IA) or (IB) comprising at least one phosphorodithioate internucleoside linkage for inhibiting target RNA in a cell, where in the formula, R is hydrogen or a phosphate-protecting group, and M+ is a cation, e.g., a metal cation, e.g., an alkali metal cation, e.g., a Na+ or K+ cation; or M+ is an ammonium cation.SELECTED DRAWING: None 【課題】改良された生理化学的特性及び薬理学的特性を有するオリゴヌクレオチドを提供する。【解決手段】式(IA)または(IB)TIFF2024041886000100.tif45128の少なくとも1個のホスホロジチオアートヌクレオシド間結合を含む、細胞において標的RNAを阻害するためのアンチセンスギャップマーオリゴヌクレオチドであって、式中、Rは、水素またはリン酸保護基であり、かつ、M+は、陽イオン、例えば金属陽イオン、例えばアルカリ金属陽イオン、例えばNa+陽イオンもしくはK+陽イオンであるか、またはM+は、アンモニウム陽イオンである、前記アンチセンスギャップマーオリゴヌクレオチドを提供する。【選択図】なし
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or M+ is an ammonium cation.SELECTED DRAWING: None 【課題】改良された生理化学的特性及び薬理学的特性を有するオリゴヌクレオチドを提供する。【解決手段】式(IA)または(IB)TIFF2024041886000100.tif45128の少なくとも1個のホスホロジチオアートヌクレオシド間結合を含む、細胞において標的RNAを阻害するためのアンチセンスギャップマーオリゴヌクレオチドであって、式中、Rは、水素またはリン酸保護基であり、かつ、M+は、陽イオン、例えば金属陽イオン、例えばアルカリ金属陽イオン、例えばNa+陽イオンもしくはK+陽イオンであるか、またはM+は、アンモニウム陽イオンである、前記アンチセンスギャップマーオリゴヌクレオチドを提供する。【選択図】なし</abstract><oa>free_for_read</oa></addata></record>
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subjects BEER
BIOCHEMISTRY
CHEMISTRY
COMPOSITIONS THEREOF
CULTURE MEDIA
DERIVATIVES THEREOF
ENZYMOLOGY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
MICROBIOLOGY
MICROORGANISMS OR ENZYMES
MUTATION OR GENETIC ENGINEERING
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SPIRITS
SUGARS
VINEGAR
WINE
title OLIGONUCLEOTIDES COMPRISING HOSPHORODITHIOATE INTERNUCLEOSIDE LINKAGE
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