Abstract: Provided is a novel nucleic acid molecule that can inhibit the expression of a gene and can be produces easily and efficiently. 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, 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. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.

Abstract: The object of the present invention is to provide a novel and useful galactose derivative, which is a component of a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the drug carrier and a medicine. The present invention relates to a galactose derivative represented by the following general formula (I) a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, an oligo nucleic acid). wherein, R1 represents hydrogen, an alkyl having 1 to 10 carbons which may be substituted or 1-(D)-deoxylactito-1-yl; R2 represents a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms.

Abstract: The present invention relates to a novel and useful galactose derivative constituting a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the carrier and a medicine. The present invention also relates to a galactose derivative made up of galactose, a suitable spacer and a certain lipid, a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, or an oligo nucleic acid).

Abstract: The object of the present invention is to provide a novel and useful galactose derivative, which is a component of a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the drug carrier and a medicine. The present invention relates to a galactose derivative represented by the following general formula (I) a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, an oligo nucleic acid). wherein, R1 represents hydrogen, an alkyl having 1 to 10 carbons which may be substituted or 1-(D)-deoxylactito-1-yl; R2 represents a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms.

Abstract: An object of the present invention is to provide a useful and novel phosphoramidite compound for the synthesis of oligo-RNA. A phosphoramidite compound represented by general formula (1), wherein: BX represents a nucleobase optionally having a protecting group; and R1 is a substituent represented by general formula (2), wherein: R11, R12 and R13 are the same or different and each represents hydrogen or alkoxy; R2a and R2b are the same or different and each represents alkyl, or R2a and R2b taken together with the adjacent nitrogen atom may form a 5- to 6-membered saturated amino cyclic group, the amino cyclic group optionally having an oxygen or sulfur atom as a ring-composing member in addition to the adjacent nitrogen atom; and WG1 and WG2 are the same or different and each represents an electron-withdrawing group.

Abstract: The present invention relates to a novel and useful galactose derivative constituting a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the carrier and a medicine. The present invention also relates to a galactose derivative made up of galactose, a suitable spacer and a certain lipid, a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, or an oligo nucleic acid).

Abstract: A novel phosphotriesterified ribonucleic acid compound which is important for liquid-phase synthesis of oligo-RNA is provided. Examples of the ribonucleic acid compound of the invention may include ribonucleic acid compounds represented by the following general formula: (wherein B represents adenine, guanine, cytosine or uracil or a modified form thereof; R21 represents aryl which may be substituted or a monocyclic or bicyclic heterocyclic group which may be substituted; R20 represents H or alkyl which may be substituted; and R1 represents a protecting group which can be removed at 90% or more at a temperature in the range from 0° C. to 60° C. under acidic conditions at a pH value from 2 to 4 within 24 hours).

Abstract: The present invention provides a chain-shortened polynucleotide wherein the proportion of a 2?-5? phosphodiester bond is up to 3% based on the whole phosphodiester bonds or a salt thereof and a pharmaceutical composition containing the same, and a method for producing the same.

Abstract: The present invention to novel nociceptin receptor agonists which are peptide derivatives represented by the following general formula (1): (in which A is alkylene, —CH2)nCO— or a group expressed by the following formula (2) or (3): wherein n represents an integer of 1 to 8; X and Y are same or different and each represents —CONH— or —CH2NH—; R1, R2 and R3 are same or different and each represents alkyl, aryl or heteroaryl; Z represents —CON(R4)R5 or —CH2N(R4)R5; R4 and R5 are same or different and each represents hydrogen, alkyl, aryl or heteroaryl) or a pharmaceutically acceptable salt thereof. A pharmaceutical composition according to the present invention is useful as a nociceptin receptor agonist.

Abstract: The present invention provides a chain-shortened polynucleotide wherein the proportion of a 2′-5′ phosphodiester bond is up to 3% based on the whole phosphodiester bonds or a salt thereof and a pharmaceutical composition containing the same, and a method for producing the same.

Abstract: The present invention provides a chain-shortened polynucleotide wherein the proportion of a 2′-5′ phosphodiester bond is up to 3% based on the whole phosphodiester bonds or a salt thereof and a pharmaceutical composition containing the same, and a method for producing the same.

Abstract: The object of the invention is to provide a lipid device functionally equivalent to the so-called cationic liposome and of lesser toxicity and a lipid or the like as a component of the device.The compound of the invention includes but is not limited to 3-O-(4-dimethylaminobutanoyl)-1,2-O-dioleylglycerol, 3-O-(2-dimethylaminoethyl)carbamoyl-1,2-O-dioleylglycerol, 3-O-(2-diethylaminoethyl) carbamoyl-1,2-O-dioleylglycerol and 2-O-(2-diethylaminoethyl) carbamoyl-1,3-O-dioleoylglycerol. The device of the invention comprises such a lipid and a phospholipid.By administering a double-stranded RNA, for instance, together with the device of the invention, the double-stranded RNA can be safely delivered to the site of action.

Abstract: The invention is composed of a hederagenin derivative of the following formula or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising of this compound as an active ingredient. ##STR1## (wherein R.sup.1 represents OR.sup.11 or NR.sup.11 R.sup.12. R.sup.11 and R.sup.12 may be the same or different and each represents hydrogen, alkyl that may be substituted, cycloalkyl that may be substituted, alkenyl that may be substituted, alkinyl that may be substituted, aryl that may be substituted, or a heteroaromatic group that may be substituted,R.sup.2 and R.sup.3 may be the same or different and each represents hydrogen, alkyl that may be substituted, cycloalkyl that may be substituted, alkenyl that may be substituted, alkinyl that may be substituted, acyl that may be substituted, monoalkylcarbamoyl that may be substituted, dialkylcarbamoyl that may be substituted, or alkoxycarbonyl that may be substituted, or R.sup.2 and R.sup.3 taken together represents carbonyl.

Abstract: This invention has for its object to insure an effective utilization of single-stranded nucleic acid copolymers, particularly poly(adenylic acid-uridylic acid), and to provide a pharmaceutical composition having antitumor activity.The invention typically relates to a pharmaceutical composition comprising a lipid device such as Lipofectin (trademark), 3-O-(4-dimethylaminobutanoyl)-1,2-O-dioleylgycerol, 3-O-(2-dimethylamino-ethyl)carbamoyl-1,2-O-dioleylglycerol, 3-O-(2-diethylaminoethyl) carbamoyl-1,2-O-dioleylgycerol, or 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoylglycerol and poly(adenylic acid-uridylic acid).

Abstract: The present invention is composed of a nucleoside derivative of the following general formula ?I!: ##STR1## (wherein B represents adenin-9-ylmethyl, guanin-9-ylmethyl, hypoxanthin-9-ylmethyl, thymin-1-ylmethyl, uracil-1-ylmethyl, or cytosin-1-ylmethyl; X and Y may be the same or different and each represents hydrogen or hydroxy, exclusive of the case in which X is hydrogen and Y is hydroxy).The compound of the present invention is useful as an antiviral agent or an antimalignant-tumoral agent.

Abstract: Cyclic AMP and cyclic GMP derivatives, such as 8-bromoadenosine-3', 5'-cyclic methylphosphonate, are effective in inhibiting phosphodiesterases.

Abstract: Nucleic acid derivatives and pharmaceutical compositions containing such derivatives are produced containing one 4-thiouridylic acid for every 6 to 39 cytidylic acids present, which has a length of from 50 to 10,000 base pairs. Methods of treatment using these nucleic acid derivatives to treat viral infections is also described.

Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 and R.sup.2 are the same or different and each is hydrogen, hydroxy, halo, alkoxy of 1 to 4 carbon atoms or aralkyloxy of 1 to 4 carbon atoms and X and Y are each hydrogen or nicotinoyl are useful as anti-edema agents, anti-inflammatories, analgesics, anti-pyretics, anti-allergenics and anti-thrombosis agents.

Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 and R.sup.2 are the same or different and each is hydrogen, hydroxy, halo, alkoxy of 1 to 4 carbon atoms or aralkyloxy of 1 to 4 carbon atoms and X and Y are each hydrogen or nicotinoyl are useful as anti-edema agents, anti-inflammatories, analgesics, anti-pyretics, anti-allergenics and anti-thrombosis agents.