CARBOHYDRATE CONJUGATES AS DELIVERY AGENTS FOR OLIGONUCLEOTIDES

Title:

CARBOHYDRATE CONJUGATES AS DELIVERY AGENTS FOR OLIGONUCLEOTIDES

Document Type and Number:

Japanese Patent JP2016034974

Kind Code:

A

Abstract:

PROBLEM TO BE SOLVED: To provide new receptor specific ligand conjugated iRNA agents and methods for their preparation that address shortcomings of in vivo delivery of oligonucleotide therapeutics.SOLUTION: The present invention provides iRNA agents comprising at least one subunit of the formula (I). In the formula, A and B are each independently O, N(R) or S; X and Y are each independently for each occurrence H, OH, a hydroxy protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, -P(Z')(Z'')O-nucleoside, -P(Z')(Z'')O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, -P(Z')(Z'')O-Linker-OP(Z''')(Z'''')O-oligonucleotide, a nucleotide, an oligonucleotide, -P(Z')(Z'')-formula(I), -P(Z')(Z'')- or -Linker-R; R is Lor -Linker-L, or has the structure including a plurality of -Linker-Las branched chains shown in the chemical formula 7 herein, where Lis independently for each occurrence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, or polysaccharide; Ris independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and Z', Z'', Z''' and Z'''' are each independently for each occurrence O or S.SELECTED DRAWING: None

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Inventors:

MUTHIAH MANOHARAN
KALLANTHOTTATHIL G RAJEEV
NARAYANANNAIR K JAYAPRAKASH
MARTIN MAIER

Application Number:

JP2015224825A

Publication Date:

March 17, 2016

Filing Date:

November 17, 2015

Export Citation:

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Assignee:

ALNYLAM PHARMACEUTICALS INC

International Classes:

A61K31/713; A61K47/48; A61P3/00; A61P25/00; A61P27/02; A61P29/00; A61P31/00; A61P35/00; A61P43/00; C12N15/113; C12Q1/02; C12Q1/68

Domestic Patent References:

JP2007527891A

2007-10-04

Foreign References:

WO2006020768A2	2006-02-23
WO2006078278A2	2006-07-27
WO2005116226A2	2005-12-08

Other References:

NATURE BIOTECHNOLOGY,2007VOL.25,NO.10,P.1149-1157, JPN6013038197, ISSN: 0003481609
JOURNAL OF MEDICINAL CHEMISTRY,2004,VOL.47,NO.23,P.5798-5808, JPN6013038199, ISSN: 0003481610
JOURNAL OF MEDICINAL CHEMISTRY,1999,VOL.42,NO.4,P.609-618, JPN6013038200, ISSN: 0003481611
BIOCONJUGATE CHEM.,2003,VOL.14,NO.1,P.239-246, JPN6013038202, ISSN: 0003481612

Attorney, Agent or Firm:

Yanagita Seiji
Go Sakuma

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