Abstract: An object of the present invention is to provide a sustained-release injectable preparation which is in a medication administration form that can provide the effect of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for a prolonged period of time, the preparation releasing a therapeutically effective amount of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for at least one week. The present invention provides an injectable preparation containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, which releases the active ingredient in such a manner that its blood concentration is maintained for at least one week.

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: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases.

Abstract: An object of the present invention is to provide a sustained-release injectable preparation which is in a medication administration form that can provide the effect of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for a prolonged period of time, the preparation releasing a therapeutically effective amount of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for at least one week. The present invention provides an injectable preparation containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, which releases the active ingredient in such a manner that its blood concentration is maintained for at least one week.

Abstract: Disclosed is a phosphorylation inhibitor of SMAD2/3 protein or a therapeutic agent for fibrosis which contains as an active ingredient, a nucleic acid that suppresses NEK6 (NIMA-related serine/threonine kinase 6) gene expression.

Abstract: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases.

Abstract: Disclosed is a phosphorylation inhibitor of SMAD2/3 protein or a therapeutic agent for fibrosis which contains as an active ingredient, a nucleic acid that suppresses NEK6 (NIMA-related serine/threonine kinase 6) gene expression.

Abstract: The present invention provides a composition containing a single-stranded nucleic acid molecule consisting of a nucleotide sequence shown by 5?-AGCAGAGUACACACAGCAUAUACC-P-GGUAUAUGCUGUGUGUACUCUGCUUC-P-G-3? (SEQ ID NO: 1) (in the sequence, P is a proline derivative linker represented by (I) in the DESCRIPTION) and a buffer, and having the following features: (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: An object of the present invention is to provide a sustained-release injectable preparation which is in a medication administration form that can provide the effect of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for a prolonged period of time, the preparation releasing a therapeutically effective amount of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for at least one week. The present invention provides an injectable preparation containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, which releases the active ingredient in such a manner that its blood concentration is maintained for at least one week.

Abstract: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases. The present invention provides a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl) butoxy]-1H-quinolin-2-one or of a salt thereof, and a process for producing the same.

Abstract: An object of the present invention is to provide a sustained-release injectable preparation which is in a medication administration form that can provide the effect of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for a prolonged period of time, the preparation releasing a therapeutically effective amount of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for at least one week. The present invention provides an injectable preparation containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, which releases the active ingredient in such a manner that its blood concentration is maintained for at least one week.

Abstract: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases. The present invention provides a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof, and a process for producing the same.

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 present invention provides a single-stranded nucleic acid molecule inhibiting expression of a prorenin gene or a prorenin receptor gene, comprising only region (X), linker region (Lx) and region (Xc), wherein the aforementioned linker region (Lx) has a non-nucleotide structure comprising at least one of a pyrrolidine skeleton and a piperidine skeleton, and at least one of the aforementioned region (X) and the aforementioned region (Xc) comprises an expression inhibitory sequence comprising a nucleotide sequence consisting of at least 18 continuous nucleotides in any of an expression inhibitory sequence of a prorenin gene shown in SEQ ID NO: 1 to 5 and an expression inhibitory sequence of prorenin receptor gene shown in SEQ ID NO: 6 to 11.

Abstract: The present invention provides a composition containing a single-stranded nucleic acid molecule consisting of a nucleotide sequence shown by 5?-AGCAGAGUACACACAGCAUAUACC-P-GGUAUAUGCUGUGUGUACUCUGCUUC-P-G-3? (SEQ ID NO: 1) (in the sequence, P is a proline derivative linker represented by (I) in the DESCRIPTION) and a buffer, and having the following features: (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 present invention provides a single stranded nucleic acid molecule represented by the following formula (I): (I) (SEQ?ID?NO:?1) 5?-uagcaccauuugaaaucaguguucc-P- ggaacacugauuucaaauggugcuauu-3? wherein —P— shows a proline derivative linker represented by the following formula (Ia): an agent for treating corneal diseases such as ocular surface disorders and the like, comprising the single stranded nucleic acid molecule as an active ingredient.

Abstract: An object of the present invention is to provide a sustained-release injectable preparation which is in a medication administration form that can provide the effect of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for a prolonged period of time, the preparation releasing a therapeutically effective amount of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for at least one week. The present invention provides an injectable preparation containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, which releases the active ingredient in such a manner that its blood concentration is maintained for at least one week.

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: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases. The present invention provides a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof, and a process for producing the same.