Abstract: The invention provides a production method of a glycoside compound or a salt thereof, which includes subjecting a thioether compound and an alcohol compound to a coupling reaction in the presence of a halogenating agent, a desiccant and a Lewis acid, and then distillation in the presence of at least one kind of additive selected from a sulfur-containing antioxidant and a maleimide group-containing compound to give a thioether compound and a step of subjecting a glycoside compound and a thioether compound to a coupling reaction in the presence of a halogenating agent, a desiccant and a Lewis acid to give a glycoside compound. By this method, a phosphoramidite preferable for the production (synthesis) of a nucleic acid can be produced more efficiently at a high purity.

Abstract: The present invention provides a composition containing a nucleic acid molecule and a buffer, and having the features of (a) being in the form of a solution at ambient temperature; and (b) a content of the nucleic acid molecule after storage at 25° C., relative humidity 60% for 4 weeks, of not less than 80% relative to the content at the time of start of the storage.

Abstract: The invention provides a single-stranded nucleic acid molecule of (A) or (B) containing a TGF-?1 gene expression inhibitory sequence. The single-stranded nucleic acid molecule (A) consists of region (Xc), linker region (Lx) and region (X) from the 5?-side to the 3?-side, wherein linker region (Lx) has a non-nucleotide structure containing at least one of a pyrrolidine skeleton and a piperidine skeleton, and at least one of region (X) and region (Xc) contains the expression inhibitory sequence.

Abstract: The invention provides a single-stranded nucleic acid capable of inhibiting expression of a target gene having a delivery function. The nucleic acid contains, from the 5?-side to the 3?-side, a 5?-side region (Xc), a linker region (Lx), an inner region (Z), a linker region (Ly) and a 3?-side region (Yc) in this order, wherein the inner region (Z) is constituted by linkage of the inner 5?-side region (X) and the inner 3?-side region (Y), the 5?-side region (Xc) is complementary to the inner 5?-side region (X), the 3?-side region (Yc) is complementary to the inner 3?-side region (Y), at least one of the inner region (Z), the 5?-side region (Xc) and the 3?-side region (Yc) comprises an expression inhibitory sequence that inhibits expression of a target gene, and at least one of the 5?-terminus, the 3?-terminus, the linker region (Lx) and the linker region (Ly) is bound to a bio-related substance.

Abstract: The invention provides a single-stranded nucleic acid capable of inhibiting expression of a target gene having a delivery function. The nucleic acid contains, from the 5?-side to the 3?-side, a 5?-side region (Xc), a linker region (Lx), an inner region (Z), a linker region (Ly) and a 3?-side region (Yc) in this order, wherein the inner region (Z) is constituted by linkage of the inner 5?-side region (X) and the inner 3?-side region (Y), the 5?-side region (Xc) is complementary to the inner 5?-side region (X), the 3?-side region (Yc) is complementary to the inner 3?-side region (Y), at least one of the inner region (Z), the 5?-side region (Xc) and the 3?-side region (Yc) comprises an expression inhibitory sequence that inhibits expression of a target gene, and at least one of the 5?-terminus, the 3?-terminus, the linker region (Lx) and the linker region (Ly) is bound to a bio-related substance.

Abstract: The invention provides a microRNA inhibitor that has two or more sequences complementary to the sequence of microRNA to be the target of inhibition, which two or more complementary sequences are linked via one or more linker residues.

Abstract: The invention provides a single-stranded nucleic acid molecule containing an expression inhibitory sequence that inhibits expression of a target gene, region (X), linker region (Lx), and region (Xc), wherein the linker region (Lx) is linked between the region (Xc) and the region (Xc), the region (Xc) is complementary to the region (X), at least one of the region (X) and the region (Xc) contains the expression inhibitory sequence, and the linker region (Lx) contains an atomic group derived from an amino acid. The single-stranded nucleic acid molecule can inhibit expression of the target gene.

Abstract: The invention provides an artificial match-type miRNA utilizing miRNA. A In particular, the invention provides a single strand nucleic acid containing an X region and a Y region, wherein the 3?-terminal of the X region and the 5?-terminal of the Y region are linked via a linker region of a non-nucleotide structure, the X region contains a guide strand sequence of a mature miRNA, and the Y region contains a sequence completely complementary to the X region is an artificial match-type miRNA. The artificial match-type miRNA can suppress expression of the target gene.

Abstract: The invention provides a glucoside compound, which is capable of providing a phosphoramidite, which can be produced at low cost and can produce a nucleic acid in high yield and with high purity. The glycoside compound has the formula wherein B, R1, and R2 are as described herein, R3 is —OCH2(OCH2)n—O-L1-[D1], in which L1 is an ethylene group, wherein hydrogen atoms besides a hydrogen atom bonded to the ?-position relative to [D1] are optionally substituted by a straight chain or branched alkyl group, n is a positive integer, and [D1] is an electron-withdrawing group.

Abstract: The invention provides a microRNA inhibitor that has two or more sequences complementary to the sequence of microRNA to be the target of inhibition, which two or more complementary sequences are linked via one or more linker residues.

Abstract: The invention provides a glucoside compound, which is capable of providing a phosphoramidite, which can be produced at low cost and can produce a nucleic acid in high yield and with high purity. The glycoside compound has the formula wherein B, R1, R2, and R3 are as described herein.

Abstract: Provided is a novel nucleic acid molecule that is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes, in sequence from the 5? side to the 3? side: a 5? side region (Xc); an inner region (Z); and a 3? side region (Yc). The inner region (Z) is composed of an inner 5? side region (X) and an inner 3? side region (Y) that are linked to each other. The 5? side region (Xc) is complementary to the inner 5? side region (X). The 3? side region (Yc) is complementary to the inner 3? side region (Y). At least one of the inner region (Z), the 5? side region (Xc), and the 3? side region (Yc) includes the expression inhibitory sequence.

Abstract: The present invention provides a process for preparing an isotope-containing phosphate compound easily. The process for preparing an isotope-containing phosphate compound according to the present invention includes the step of: oxidizing a trivalent phosphorus compound with an oxidizing agent containing an isotope to synthesize a pentavalent phosphate compound to which the isotope has been introduced. The present invention preferably is applied to the synthesis of nucleic acids such as DNA and RNA, for example. The isotope preferably is a stable isotope. The oxidizing agent preferably is H218O, 3H-1,2-benzodithiol 3-one 1,1-dioxide having 34S, or a diisopropylethylamine-borane complex having 10B, for example.

Abstract: Provided is a novel nucleic acid molecule that can be produced easily and efficiently and can inhibit the expression of a gene. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes: a region (X); a linker region (Lx); and a region (Xc). The linker region (Lx) is linked between the regions (Xc) and (Xc). The region (Xc) is complementary to the region (X). At least one of the regions (X) and (Xc) includes the expression inhibitory sequence. The linker region (Lx) has a non-nucleotide structure including at least one of a pyrrolidine skeleton and a piperidine skeleton. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.

Abstract: Provided is a novel nucleic acid molecule that can be produced easily and efficiently and can inhibit the expression of a gene. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes: a region (X); a linker region (Lx); and a region (Xc). The linker region (Lx) is linked between the regions (Xc) and (Xc). The region (Xc) is complementary to the region (X). At least one of the regions (X) and (Xc) includes the expression inhibitory sequence. The linker region (Lx) has a non-nucleotide structure including at least one of a pyrrolidine skeleton and a piperidine skeleton. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.

Abstract: Provided is a novel nucleic acid molecule that is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes, in sequence from the 5? side to the 3? side: a 5? side region (Xc); an inner region (Z); and a 3? side region (Yc). The inner region (Z) is composed of an inner 5? side region (X) and an inner 3? side region (Y) that are linked to each other. The 5? side region (Xc) is complementary to the inner 5? side region (X). The 3? side region (Yc) is complementary to the inner 3? side region (Y). At least one of the inner region (Z), the 5? side region (Xc), and the 3? side region (Yc) includes the expression inhibitory sequence.

Abstract: The invention provides a glucoside compound, which is capable of providing a phosphoramidite, which can be produced at low cost and can produce a nucleic acid in high yield and with high purity. The glycoside compound has the formula wherein B, R1, R2, and R3 are as described herein.

Abstract: Provided is a novel nucleic acid molecule that is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes, in sequence from the 5? side to the 3? side: a 5? side region (Xc); an inner region (Z); and a 3? side region (Yc). The inner region (Z) is composed of an inner 5? side region (X) and an inner 3? side region (Y) that are linked to each other. The 5? side region (Xc) is complementary to the inner 5? side region (X). The 3? side region (Yc) is complementary to the inner 3? side region (Y). At least one of the inner region (Z), the 5? side region (Xc), and the 3? side region (Yc) includes the expression inhibitory sequence.

Abstract: Provided is a novel nucleic acid molecule that can be produced easily and efficiently and can inhibit the expression of a gene. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes: a region (X); a linker region (Lx); and a region (Xc). The linker region (Lx) is linked between the regions (Xc) and (Xc). The region (Xc) is complementary to the region (X). At least one of the regions (X) and (Xc) includes the expression inhibitory sequence. The linker region (Lx) has a non-nucleotide structure including at least one of a pyrrolidine skeleton and a piperidine skeleton. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.

Abstract: Provided is a novel nucleic acid molecule that can be produced easily and efficiently and can inhibit the expression of a gene. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes: a region (X); a linker region (Lx); and a region (Xc). The linker region (Lx) is linked between the regions (Xc) and (Xc). The region (Xc) is complementary to the region (X). At least one of the regions (X) and (Xc) includes the expression inhibitory sequence. The linker region (Lx) has a non-nucleotide structure including at least one of a pyrrolidine skeleton and a piperidine skeleton. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.