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DOUBLE-STRANDED NUCLEIC ACID MOLECULE, AND USE THEREOF meetings

Foreign code F180009449
File No. (S2017-0077-N0)
Posted date Jul 24, 2018
Country WIPO
International application number 2017JP039364
International publication number WO 2018079841
Date of international filing Oct 31, 2017
Date of international publication May 3, 2018
Priority data
  • P2016-213131 (Oct 31, 2016) JP
Title DOUBLE-STRANDED NUCLEIC ACID MOLECULE, AND USE THEREOF meetings
Abstract [Problem] To provide a double-stranded nucleic acid molecule exhibiting excellent antitumor activity. [Solution] A double-stranded nucleic acid molecule containing a first polynucleotide chain which includes a base sequence represented by chemical formula (1) (SEQ ID NO: 1), and a second polynucleotide chain which includes a complementary base sequence to the first polynucleotide chain.
Scope of claims [claim1]
1. The following chemical formula (1) (SEQ ID NO:1) 1 containing the nucleotide sequence represented by the first polynucleotide strand, and the second polynucleotide strand complementary nucleotide sequence in the 1 and 2 comprising a first polynucleotide strands, the double-stranded nucleic acid molecule of:
however, in a chemical formula (1), (T/U) is represents T U or; N A are respectively and independently, C, g, T, represents U or deficiency; k is 1 or a 0; L is, in the following chemical formula (2a) -(2 g) :
represented by the chemical formula (2a) in, or N Z represents CH is, represented by any one of a substituted or unsubstituted cyclic compound-containing group or, or, 2 wherein the one or more of the cyclic compound-containing group is respectively connected to each other through other than a phosphodiester bond 2 represents a divalent group composed; M is, represents a hydrogen atom or a hydroxyl protecting group; at this time, the first polynucleotide strand 1 nucleotides is, independently, 2 '- O- methyl, 2' - methoxyethoxy, 2 '- fluoro, 2' - allyl, 2 '- -2 - oxoethyl O-2 (methylamino), 4' - thio, 4 '- (CH2)2-O-2'-crosslinking, 2' - locked nucleic acid or 2' -O- (N - methylcarbamate) is selected from the group consisting of a substituted modified sugar moiety may be a base, a first polynucleotide strand is other than a phosphodiester bond 1, independently from each other, of the following chemical formula (3) :
in chemical (3) formulae, X1O independently, represent S or Se, X2OH or independently O-, SHor S-, SeHor Se-, and alkyl groups of 1-4 carbon atoms or a morpholino group (however, X1X O and where2O is-are excluded), represented by the modified linkages phosphorus atoms may be substituted.
[claim2]
2. Wherein the first 2 and second 1 polynucleotide strand is the number of nucleotides of a polynucleotide strand, each independently of the nucleotide at the 23-30, the double-stranded nucleic acid molecule according to claim 1.
[claim3]
3. Wherein the nucleotide sequence shown in SEQ ID NO:1 (T/U) is, in U, double stranded nucleic acid molecule according to claim 1 or 2.
[claim4]
4. Wherein the nucleotide sequence shown in SEQ ID NO:1 NN is, or is a TT GG, double stranded nucleic acid molecule of any one of claims 1-3.
[claim5]
5. Wherein the first chain in the 2, of the following chemical formula (5) (SEQ ID NO:2) comprising the nucleotide sequence shown in, any one of claims 1-4 double stranded nucleic acid molecule of:however, represented by the chemical formula (5) (sequence number 2) in, N'independently A, C, g, T, U or deficiency represents; k, L and M is as defined above and; at this time, the first 2 to a polynucleotide strand nucleotides is, independently, 2 '- O- methyl, 2' - methoxyethoxy, 2 '- fluoro, 2' - allyl, 2 '- O-2 (methylamino) -2 - oxoethyl, 4' - thio, 4 '- (CH2)2-O-2'-crosslinking, 2' - locked nucleic acid or 2' -O- (N - methylcarbamate) is selected from the group consisting of a substituted modified sugar moiety may be a base, a first polynucleotide strand is other than a phosphodiester bond 2, are each independently, wherein the modification of the phosphorus atoms represented by (3) a chemical formula may be replaced with.
[claim6]
6. Wherein the nucleotide sequence shown in SEQ ID NO:2 NN is, GG in, a double-stranded nucleic acid molecule according to claim 5.
[claim7]
7. Wherein the double stranded nucleic acid molecule of any one of claims 1-6 to containing the base sequence encoding, vectors.
[claim8]
8. Double stranded nucleic acid molecule of any one of claims 1-6, or according to claim 7 vector as an active ingredient, an anti-tumor agent.
[claim9]
9. The cationic polyamino acids of a hydrophilic polymer chain segment and a block copolymer having a segment, of any one of claims 1-6 comprises double stranded nucleic acid molecule, wherein the cationic poly amino acid segment of positive charges and negative charges of the double stranded nucleic acid molecules are offset and electrically neutral, said double-stranded nucleic acid molecule is a hydrophilic polymer chain segment covered with pharmaceutical composition structure type unit, an anti-tumor agent.
[claim10]
10. Bladder cancer, colon cancer, breast cancer, leukemia, ovarian cancer, prostate cancer, hepatocellular cancer (Hepatocarcinoma), lung cancer, stomach cancer, esophageal cancer, pancreatic cancer, glioblastoma, pharynges cancer, nasopharynx cancer, oral cancer, pituitary tumor and can be a tumor selected from the group consisting of prevention and/or treatment, the anti-tumor agent according to claim 8 or 9.
[claim11]
11. Double stranded nucleic acid molecule of any one of claims 1-6, according to claim 7 vector, or any one of claims 8-10 the anti-tumor agent in a subject comprising administering to the, prevention and/or treatment of the tumor.
[claim12]
12. Wherein the tumor, bladder cancer, colon cancer, breast cancer, leukemia, ovarian cancer, prostate cancer, hepatocellular cancer (Hepatocarcinoma), lung cancer, stomach cancer, esophageal cancer, pancreatic cancer, glioblastoma, pharynges cancer, nasopharynx cancer, oral cancer, and is selected from the group consisting of tumor adenohypophysis, method according to claim 11.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • GIFU UNIVERSITY
  • Inventor
  • AKAO YUKIHIRO
IPC(International Patent Classification)
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