Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to 5-membered heterocyclic derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.

Abstract: A compound (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic ring which may have a substituent, a 6-membered aromatic heterocyclic ring which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Abstract: A compound represented by the general formula (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y represents a C1-6 alkylene group or the like; RN represents a hydrogen atom or a C1-6 alkyl group; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic group which may have a substituent, a 6-membered aromatic heterocyclic group which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Abstract: The present invention provides a solid oral dosage form pharmaceutical for the treatment of dysuria, which comprises, as an active ingredient, an indoline compound having an ?1-adrenoceptor blocking activity and represented by the formula: prodrug, pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof, wherein said pharmaceutical is prepared to have 85% dissolution time of not more than 60 minutes in a dissolution test according to method 2 (paddle method) of Japanese pharmacopoeia in a condition using water.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R1 represents halogen, a hydroxy group or the like; R2 represents halogen, a hydroxy group, alkyl, alkoxy, alkyl substituted by fluorine, alkoxy substituted by fluorine or the like; m represents a number from 0 to 2; n represents a number from 0 to 3; and R3 represents hydrogen, fluorine or the like.

Abstract: Patients having symptoms associated with benign prostatic hyperplasia can be treated with a once daily composition containing silodosin or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides fused heterocyclic derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 to R4 represent H, OH, an amino group, etc.; R5 and R6 represent H, OH, a halogen atom, an option ally substituted alkyl group, etc.; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; the following ring (R1) represents a group represented by the following ring (R2); G represents a group represented by the following general formula (G-1) or (G-2) (E1 represents H, F or OH; and E represents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

Abstract: The present invention provides pharmaceutical compositions useful for relieving pain caused by ureteral calculi, facilitating exclusion of ureteral calculi or the like. That is, the present invention provides a pharmaceutical composition for the treatment of ureteral lithiasis, which comprises as an active ingredient an indoline derivative represented by the following general formula (I) or a salt thereof. In the formula, R represents saturated or unsaturated aliphatic acyl which may have a substituent; hydroxyalkyl; aliphatic acyloxyalkyl; lower alkyl which has as a substituent lower alkoxy, carboxy, lower alkoxycarbonyl, aryl-substituted lower alkoxycarbonyl, carbamoyl, mono or di (lower alkyl)-substituted carbamoyl or cyano; optionally substituted aromatic acyl; furoyl or pyridylcarbonyl; R1 represents cyano or carbamoyl; and R2 represents lower alkyl which may have as a substituent halogen, cyano or aryl.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like. A glucopyranosyloxypyrazole derivative can be easily and efficiently prepared by allowing a benzylpyrazole derivative represented by the general formula: wherein R1, R2, R3, R4 and R5 may be the same or different, for example each of them is a hydrogen atom, a halogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, R6 is an alkyl group, for example R7 is a hydrogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, to react with a compound represented by the general formula: wherein as an example, PG1 is a pivaloyl group or the like, as an example, X1 is a bromine atom or the like, therefore the present invention is extremely useful as a method for preparing pharmaceutical compounds.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), X1 and X2 represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: The present invention provides ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride ¼ hydrate or a crystal thereof which can be determined by characteristic diffraction peaks of the powder X-ray diffraction, thermogravimetry-differential thermal analysis or the like, and obtained by manufacturing ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methyl-ethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.

Abstract: The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like. A glucopyranosyloxypyrazole derivative can be easily and efficiently prepared by allowing a benzylpyrazole derivative represented by the general formula: wherein R1, R2, R3, R4 and R5 may be the same or different, for example each of them is a hydrogen atom, a halogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, R6 is an alkyl group, for example R7 is a hydrogen atom or an alkyl, alkoxy, arylmethyloxy group or the like, to react with a compound represented by the general formula: wherein as an example, PG1 is a pivaloyl group or the like, as an example, X1 is a bromine atom or the like, therefore the present invention is extremely useful as a method for preparing pharmaceutical compounds.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), T represents trifluoromethyl, nitro or cyano; ring Q represents heteroaryl; X1 and X2 independently represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.

Abstract: The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 represent H, an optionally substituted alkyl group, an alkenyl group, etc.; R2 represent H, a halogen atom or an alkyl group; R3 and R4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.

Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereo

Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Abstract: The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.