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Title:
BRIDGED ARTIFICIAL NUCLEOSIDE AND NUCLEOTIDE
Document Type and Number:
WIPO Patent Application WO/2011/052436
Kind Code:
A1
Abstract:
Provided is a novel molecule for an antisense by which the expression of a specific gene can be efficiently regulated. As formulae (I) and (II) show, the novel artificial nucleoside has an amide bond introduced into a bridged structure of 2',4'-BNA/LNA. An oligonucleotide containing this 2',4'-bridged artificial nucleotide has a binding affinity for a single-stranded RNA comparable to that of publicly known 2',4'-BNA/LNA, and a resistance to nuclease stronger than that of LNA. Since the binding affinity of the aforesaid oligonucleotide to a single-stranded RNA is much stronger than that of S-oligo, in particular, it is expected that the oligonucleotide is applicable to nucleic acid drugs.

Inventors:
OBIKA, Satoshi (1-1 Yamadaoka, Suita-sh, Osaka 71, 〒5650871, JP)
小比賀 聡 (〒71 大阪府吹田市山田丘1番1号 国立大学法人大阪大学内 Osaka, 〒5650871, JP)
HARI, Yoshiyuki (1-1 Yamadaoka, Suita-sh, Osaka 71, 〒5650871, JP)
張 功幸 (〒71 大阪府吹田市山田丘1番1号 国立大学法人大阪大学内 Osaka, 〒5650871, JP)
KODAMA, Tetsuya (1-1 Yamadaoka, Suita-sh, Osaka 71, 〒5650871, JP)
Application Number:
JP2010/068409
Publication Date:
May 05, 2011
Filing Date:
October 19, 2010
Export Citation:
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Assignee:
OSAKA UNIVERSITY (1-1 Yamadaoka, Suita-shi Osaka, 71, 〒5650871, JP)
国立大学法人大阪大学 (〒71 大阪府吹田市山田丘1番1号 Osaka, 〒5650871, JP)
OBIKA, Satoshi (1-1 Yamadaoka, Suita-sh, Osaka 71, 〒5650871, JP)
小比賀 聡 (〒71 大阪府吹田市山田丘1番1号 国立大学法人大阪大学内 Osaka, 〒5650871, JP)
HARI, Yoshiyuki (1-1 Yamadaoka, Suita-sh, Osaka 71, 〒5650871, JP)
張 功幸 (〒71 大阪府吹田市山田丘1番1号 国立大学法人大阪大学内 Osaka, 〒5650871, JP)
International Classes:
C07H19/06; A61K31/712; C07H19/16; C07H21/00
Domestic Patent References:
WO1999060855A11999-12-02
WO2005021570A12005-03-10
WO1998039352A11998-09-11
WO2005021570A12005-03-10
WO2003068795A12003-08-21
Other References:
"Nucleic Acids Symposium Series, 2009.09", vol. 53, article YAHARA, A. ET AL.: "Synthesis and properties of a novel 2',4'-BNA bearing a urea bridged structure", pages: 11 - 12, XP055077947, DOI: doi:10.1093/nass/nrp006
"Nucleic Acids Symposium Series", 2007, article NISHIDA, M. ET AL.: "Synthesis and chemical properties of a novel 2',4'-bridged nucleic acid analog with a seven-membered cyclic carbamate structure", pages: 157 - 158, XP055077949, DOI: doi:10.1093/nass/nrm079
See also references of EP 2495248A4
C. WAHLESTEDT ET AL., PROC. NATL. ACAD. SCI. USA, vol. 97, no. 10, 2000, pages 5633 - 5638
Y HARI ET AL., BIOORG. MED. CHEM., vol. 14, 2006, pages 1029 - 1038
K. MIYASHITA ET AL., CHEM. COMMUN., 2007, pages 3765 - 3767
S.MA RAHMAN ET AL., J. AM. CHEM. SOC., vol. 130, no. 14, 2008, pages 4886 - 4896
M. KUWAHARA ET AL., NUCLEIC ACIDS RES., vol. 36, no. 13, 2008, pages 4257 - 4265
OBIKA ET AL., BIOORG. MED. CHEM., vol. 9, 2001, pages 1001 - 1011
KOSHKIN, A. A. ET AL., TETRAHEDRON, vol. 54, 1998, pages 3607 - 3630
SINGH, S. K ET AL., CHEM. COMMUN., 1998, pages 455 - 456
Attorney, Agent or Firm:
SHINDO, Takuya (5th Floor, Okina Bldg. 2-9, Nishitenma 3-chome, Kita-ku, Osaka-sh, Osaka 47, 〒5300047, JP)
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