4 results about "Carbocyclic nucleoside" patented technology

The present invention belongs to the technical field of medicine and provides a carbocyclic nucleoside-containing siRNA conjugate, and a pharmaceutical composition and a use thereof. The sense strand and / or antisense strand of the siRNA conjugate comprises at least one carbocyclic nucleoside represented by structural formula (I) below. The sense strand comprises at least 16 consecutive nucleotides of the nucleotide sequence 5'-GUCAUCCACAAUGAGAGUACA-3', and the antisense strand comprises at least 18 consecutive nucleotides of the nucleotide sequence 5'-UGUACUCUCAUUGUGGAUGACGA-3'. The carbocyclic nucleoside-containing siRNA conjugate provided by the present invention can be used for treating, preventing, and / or alleviating AGT-related diseases, such as hypertension.

The application discloses a rhodium-catalyzed desymmetrization hydroformylation method for constructing polychiral center carbon ring nucleosides. The method for constructing polychiral center carbon ring nucleosides comprises the following steps: under the condition of an inert atmosphere, an acetylacetone dicarbonyl rhodium metal precursor and a chiral ligand are added into an organic solvent to prepare a catalyst solution, the catalyst solution is mixed with a substrate, and a reaction is carried out under the condition of a hydrogen atmosphere and a carbon monoxide atmosphere; after the reaction is completed, filtration and purification are carried out, and polychiral center cycloalkyl aldehyde is obtained; and the aldehyde group is converted to obtain the polychiral center carbon ring nucleosides. The method for constructing polychiral center carbon ring nucleosides has the advantages of high selectivity, wide substrate compatibility, high reaction efficiency, easy conversion of products, and the like. The whole reaction process can obtain polychiral center cycloalkyl aldehyde in one step with extremely high enantioselectivity and diastereoselectivity, the aldehyde group is converted, polychiral center carbon rings can be obtained with high yield, high dr value and high ee value, and the method is simple and easy to operate.

In the present application, as one embodiment of the invention, an oligonucleotide or a salt thereof is disclosed, characterized in that, in the sequence of the oligonucleotide, at least one carbocyclic nucleoside derivative residue of a divalent group represented by the following formula (B) (in the formula, each symbol is consistent with the description record.) is contained, the oligonucleotide or the salt thereof shows excellent effects on a target RNA or the like while maintaining high safety.