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Title:
PHOSPHATE SITE MODIFICATION OF NUCLEIC ACID CONTAINING NITROGEN-CONTAINING NON-AROMATIC HETEROCYCLE
Document Type and Number:
WIPO Patent Application WO/2015/125845
Kind Code:
A1
Abstract:
 Provided are: a oligonucleotide having at least one bond represented by formula (I): (in the formula, Q is S or O, X1 does not exist, or is a substituted or unsubstituted alkylene in which O may be interposed, X2 is a substituted or unsubstituted monocyclic or duocyclic nitrogen-containing non-aromatic heterocyclic group) or a pharmaceutically acceptable salt thereof, and a novel amidite which can be used as a material for synthesizing said oligonucleotide. The oligonucleotide is a novel phosphate site modification which can be used as a nucleic acid pharmaceutical.

Inventors:
KUGIMIYA AKIRA (JP)
KURODA NORIKAZU (JP)
NAKAMURA JUN (JP)
Application Number:
PCT/JP2015/054539
Publication Date:
August 27, 2015
Filing Date:
February 19, 2015
Export Citation:
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Assignee:
SHIONOGI & CO (JP)
International Classes:
C07H21/00; C07F9/24; C07H19/10; C07H19/173; A61K31/7125; A61K48/00
Domestic Patent References:
WO2014012081A22014-01-16
WO2013012758A12013-01-24
Foreign References:
JPH06500556A1994-01-20
JPH05310779A1993-11-22
Other References:
WADA,T. ET AL.: "Chemical synthesis and properties of stereoregulated phosphorothioate RNAs", NUCLEIC ACIDS SYMPOSIUM SERIES, vol. 51, no. 1, 2007, pages 119 - 120, XP055222198, ISSN: 0261-3166
ASSELINE,U. ET AL.: "Oligonucleotides covalently linked to intercalating agents. Influence of positively charged substituents on binding to complementary sequences", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 260, no. 15, 1985, pages 8936 - 8941, XP055222199
DE ,J.E. ET AL.: "Mapping of ligand binding sites on macromolecules by means of spin-labeled ligands and 2D difference spectroscopy", JOURNAL OF MAGNETIC RESONANCE(1969-1992, vol. 80, no. 2, 1988, pages 197 - 213, XP023959486, ISSN: 0022-2364
Attorney, Agent or Firm:
TAKAYAMA, Hirotsugu et al. (JP)
Hiromitsu Takayama (JP)
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