Title:
MODIFIED OLIGONUCLEOTIDES
Document Type and Number:
WIPO Patent Application WO/2006/025154
Kind Code:
A1
Abstract:
The invention aims at providing oligonucleotides modified at the 3' end which are excellent in penetration through cell membrane, resistance to nuclease, and the ability to form double strands and whose production was difficult in the prior art. The aim is attained by a modified oligonucleotide wherein the 5',3'-phosphoric diester linkage between the first and second nucleosides from the 3' end is replaced by a linkage represented by the general formula (I-1): -X1-C(=Y1)-Z1- (I) [wherein X1 is O, NH, or S; Y1 is O or S; and Z1 is O, NH, or S]. Such modified oligonucleotides can be produced through solid phase synthesis by using unit compounds for solid phase synthesis as represented by the general formula (X-1) as the starting raw material: (X-1) wherein R2, W11, W21, B1, B2, A, X2, X1, Y1, Z1 and M are each as defined in the description.
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Inventors:
KITADE YUKIO
UENO YOSHIHITO
WATAYA YUSUKE
UENO YOSHIHITO
WATAYA YUSUKE
Application Number:
PCT/JP2005/012579
Publication Date:
March 09, 2006
Filing Date:
July 07, 2005
Export Citation:
Assignee:
UNIV GIFU (JP)
UNIV OKAYAMA NAT UNIV CORP (JP)
KITADE YUKIO
UENO YOSHIHITO
WATAYA YUSUKE
UNIV OKAYAMA NAT UNIV CORP (JP)
KITADE YUKIO
UENO YOSHIHITO
WATAYA YUSUKE
International Classes:
C07H19/073; A61K31/7125; A61K31/713; A61K48/00; A61P43/00; C07H19/173; C07H21/00; C12N15/00; (IPC1-7): C07H19/073; A61K31/7125; A61K31/713; A61K48/00; A61P43/00; C07H19/173; C07H21/00; C12N15/00
Domestic Patent References:
| WO2003070918A2 | 2003-08-28 |
Foreign References:
| JPH09503494A | 1997-04-08 | |||
| JPS62502338A | 1987-09-10 | |||
| JP2004519458A | 2004-07-02 | |||
| JPH1072486A | 1998-03-17 | |||
| JPH0368594A | 1991-03-25 |
Other References:
STIRCHAK P. ET AL.: "Uncharged stereoregular nucleic acid analogs. 1.Synthesis of a cytosine-containing oligomer with carbamate interbucleoside linkages.", JOURNAL OF ORGANIC CHEMISTRY, vol. 52, no. 19, 1987, pages 4202 - 4206, XP002070311
WALDNER A. ET AL.: "Synthesis of oligodeoxyribonucleotides containing dimers with carbamate moieties as replacement of the natural phosphodiester linkage.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS., vol. 4, no. 3, 1994, pages 405 - 408, XP002991792
WALDNER A. ET AL.: "Synthesis of oligodeoxyribonucleotides containing dimers with carbamate moieties as replacement of the natural phosphodiester linkage.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS., vol. 4, no. 3, 1994, pages 405 - 408, XP002991792
Attorney, Agent or Firm:
IKEUCHI SATO & PARTNER PATENT ATTORNEYS (OAP TOWER, 8-30, Tenmabashi 1-chome,, Kita-ku, Osaka-sh, Osaka, JP)
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