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NUCLEOSIDE DERIVATIVE AND USE THEREOF meetings

Foreign code F170009069
File No. (S2015-2046-N0)
Posted date May 29, 2017
Country WIPO
International application number 2016JP077006
International publication number WO 2017047594
Date of international filing Sep 13, 2016
Date of international publication Mar 23, 2017
Priority data
  • P2015-180893 (Sep 14, 2015) JP
Title NUCLEOSIDE DERIVATIVE AND USE THEREOF meetings
Abstract Provided is a nucleoside derivative represented by formula (1). (In formula (1), Y represents an unfused aromatic or heterocyclic hydrocarbon group or a fused polycyclic based hydrocarbon group, W1 represents a hydrogen atom, a hydroxyl group-protecting group, or a phosphate ester group, W2 represents a hydrogen atom, a hydroxyl group-protecting group, or a phosphate ester group, and R1, R2, and R3 each independently represent a hydrogen atom or a linear saturated hydrocarbon group having 1-4 carbon atoms.)
Outline of related art and contending technology BACKGROUND ART
Is a nucleic acid drug, RNA and DNA is a component of the combination of 4 kinds of bases chemically synthesized pharmaceuticals, acts directly on the disease-causing gene is believed to inhibit expression thereof. Is a nucleic acid drug, using antisense DNA antisense pharmaceutical, pharmaceutical siRNA using RNA, pharmaceutical miRNA and the like. For example, the antisense method, antisense DNA complementary single-stranded mRNA corresponding by binding to a method for inhibiting the expression of protein, its mechanism of action of the pre-mRNA splicing inhibition or mRNA due to steric hindrance such as inhibition of ribosome binding to the, degradation of mRNA by RNase H is two.
DNA/RNA double-stranded RNA is RNase H chain only specifically hydrolyze enzyme, is RNase H antisense DNA/RNA if a substrate of the double-stranded, antisense DNA expression of the protein is a catalytic amount can be suppressed. Is in an antisense approach in order to establish, synthesized oligonucleotides and the target mRNA to form a stable double-stranded, that are present in vivo nuclease resistance to necessary when pressure or the like.
In addition, also in the nucleic acid drug such as siRNA or miRNA, synthesized RNA and the target mRNA to form a stable double-stranded, that is resistant to the nucleases present in the organism and the like can be similarly required.
Up oligonucleosides derivatives, benzene - synthesis of artificial nucleic acid phosphate backbone have been reported (patent document 1). In addition, sugar portion from the backbone methylene glycol nucleic acid (GNA) will also have been reported (non-patent document 1).
Scope of claims (In Japanese)[請求項1]
以下の式(1)で表されるヌクレオシド誘導体。
[化1]
(式(1)中、Yは縮合していない芳香族系若しくは複素環式炭化水素基又は縮合多環系炭化水素基を表し、W1は、水素原子、水酸基保護基、リン酸エステル基を表し、W2は、水素原子、水酸基保護又はリン酸エステル基を表し、R1、R2及びR3は、それぞれ独立に、水素原子、炭素数1~4の直鎖状の飽和炭化水素基を表す。)
[請求項2]
前記Yは、縮合多環系炭化水素基である、請求項1に記載のヌクレオシド誘導体。
[請求項3]
前記Yは、ピリミジン骨格又はプリン骨格を含む塩基を表す、請求項1又は2に記載のヌクレオシド誘導体。
[請求項4]
以下の式(2)で表されるヌクレオシド誘導体単位を備える、オリゴヌクレオチド誘導体。
[化2]
(式(2)中、Yは縮合していない芳香族系炭化水素基若しくは複素環式炭化水素基又は縮合多環系炭化水素基を表し、R1、R2及びR3は、それぞれ独立に、水素原子、炭素数1~4の直鎖状の飽和炭化水素基を表す。)
[請求項5]
前記ヌクレオシド誘導体単位を2個以上連続して備える、請求項4に記載のオリゴヌクレオチド誘導体。
[請求項6]
前記ヌクレオシド誘導体単位を5’末端及び/又は3’末端に2個以上連続して備える、請求項5に記載のオリゴヌクレオチド誘導体。
[請求項7]
前記オリゴヌクレオチ誘導体は、オリゴデオキシリボヌクレオチドである、請求項4~6ののいずれかに記載のオリゴヌクレオチド誘導体。
[請求項8]
請求項4~7ののいずれかに記載のオリゴヌクレオチド誘導体を含む遺伝子発現抑制剤。
[請求項9]
前記オリゴヌクレオチド誘導体は、オリゴデオキシリボヌクレオチドである、請求項8に記載の遺伝子発現抑制剤。
[請求項10]
前記オリゴヌクレオチド誘導体は、オリゴリボヌクレオチドである、請求項8に記載の遺伝子発現抑制剤。
[請求項11]
請求項4~7のいずれかに記載のオリゴヌクレオチド誘導体を含む、アプタマー。
[請求項12]
請求項4~7のいずれかに記載のオリゴヌクレオチド誘導体を含む、CpGオリゴヌクレオチド。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • GIFU UNIVERSITY
  • Inventor
  • UENO Yoshihito
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KW KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
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