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Title:
非リン酸骨格結合を含むオリゴヌクレオチド
Document Type and Number:
Japanese Patent JP2008504840
Kind Code:
A
Abstract:
One aspect of the present invention relates to a ribonucleoside substituted with a phosphonamidite group at the 3′-position. In certain embodiments, the phosphonamidite is an alkyl phosphonamidite. Another aspect of the present invention relates to a double-stranded oligonucleotide comprising at least one non-phosphate linkage. Representative non-phosphate linkages include phosphonate, hydroxylamine, hydroxylhydrazinyl, amide, and carbamate linkages. In certain embodiments, the non-phosphate linkage is a phosphonate linkage. In certain embodiments, a non-phosphate linkage occurs in only one strand. In certain embodiments, a non-phosphate linkage occurs in both strands. In certain embodiments, a ligand is bound to one of the oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, a ligand is bound to both of the oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, the oligonucleotide strands comprise at least one modified sugar moiety. Another aspect of the present invention relates to a single-stranded oligonucleotide comprising at least one non-phosphate linkage. Representative non-phosphate linkages include phosphonate, hydroxylamine, hydroxylhydrazinyl, amide, and carbamate linkages. In certain embodiments, the non-phosphate linkage is a phosphonate linkage. In certain embodiments, a ligand is bound to the oligonucleotide strand. In certain embodiments, the oligonucleotide comprises at least one modified sugar moiety.

Inventors:
Manoharan, Macia
Rajiv, Karan Sotasil Gee
Application Number:
JP2007520376A
Publication Date:
February 21, 2008
Filing Date:
June 29, 2005
Export Citation:
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Assignee:
ALNYLAM PHARMACEUTICALS, INC.
International Classes:
C12N15/09; A61K31/7125; A61K31/713; A61K48/00; A61P1/04; A61P3/10; A61P9/00; A61P9/10; A61P11/00; A61P11/06; A61P17/00; A61P19/02; A61P25/00; A61P25/02; A61P25/16; A61P25/28; A61P27/02; A61P29/00; A61P31/04; A61P31/10; A61P31/12; A61P31/14; A61P31/16; A61P31/18; A61P31/20; A61P31/22; A61P33/04; A61P33/06; A61P33/10; A61P35/00; A61P35/04; A61P37/02; A61P37/06; C07H7/04; C07H19/04; C07H19/06; C07H19/16; C07H21/04; C12N15/11; C12N15/113
Domestic Patent References:
JPH03504015A1991-09-05
Foreign References:
US5606049A1997-02-25
US5731429A1998-03-24
US5789576A1998-08-04
Other References:
NUCLEOSIDES & NUCLEOTIDES, vol. 12, no. 10, JPN6011014730, 1993, pages 1007 - 1013, ISSN: 0001875571
NUCLEOSIDES & NUCLEOTIDES, vol. Vol. 15, No. 1-3, JPN6011014733, 1996, pages 387 - 397, ISSN: 0001875572
TETRAHEDRON LETT., vol. 43, JPN6011014735, 2002, pages 795 - 797, ISSN: 0001875573
NUCLEIC. ACIDS RES., vol. 23, no. 14, JPN6011014738, 1995, pages 2677 - 2684, ISSN: 0001875574
Attorney, Agent or Firm:
Yanagita Seiji
Go Sakuma