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
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	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
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Beschreibung
Zusammenfassung:	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