Abstract: [Problem] To provide a novel compound that exhibits an agonistic effect on dopamine D2 receptors. [Solution] The present invention provides a compound represented by the general formula (I): in which R1 is C1-6 alkyl or the like; R2 is hydrogen or the like; R3 and R4 are each hydrogen, C1-6 alkyl, R10R11N—C1-6 alkyl, aralkyl, or the like; R5 and R6 are hydrogen or the like; and R7 is hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine D2 receptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.

Abstract: A process for producing carrier polymer particles comprising covering the surface of organic polymer particles having a particle diameter of 0.1 to 20 micrometers with a saccharide by chemically bonding the organic polymers and the saccharide.

Abstract: [Problem] To provide a novel compound that exhibits an agonistic effect on dopamine D2 receptors. [Solution] The present invention provides a compound represented by the general formula (I): in which R1 is C1-6 alkyl or the like; R2 is hydrogen or the like; R3 and R4 are each hydrogen, C1-6 alkyl, R10R11N—C1-6 alkyl, aralkyl, or the like; R5 and R6 are hydrogen or the like; and R7 is hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine D2 receptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.

Abstract: The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 is cyano or the like; R2 and R3 are hydrogen or the like; R4 is C1-6 alkyl or the like; R5 is C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, cycloalkyl-C1-6 alkyl, aralkyl or the like; R6 and R7 are each hydrogen, C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, C1-6 alkoxy-C1-6 alkyl, R12R13N—C1-6 alkyl or the like, which exhibit potent dopamine D2 receptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Abstract: The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 is cyano or the like; R2 and R3 are hydrogen or the like; R4 is C1-6 alkyl or the like; R5 is C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, cycloalkyl-C1-6 alkyl, aralkyl or the like; R6 and R7 are each hydrogen, C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, C1-6 alkoxy-C1-6 alkyl, R12R13N—C1-6 alkyl or the like, which exhibit potent dopamine D2 receptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Abstract: The organic polymer particles comprise a carboxyl group and 2,3-dihydroxypropyl group, and the magnetic particles for diagnostics comprise fine magnetic material particles and a polymer part containing a hydrophilic polymer part and a crosslinked polymer part, a dry coating film obtained from a water dispersion thereof having a contact angle with water of 5° to 60°. The process for producing the carboxyl group-containing particles comprises a step of producing an ester bond by reacting a hydroxyl group in organic polymer particles having the hydroxyl group with a carboxylic anhydride. The organic polymer particles comprise a hydroxyl group originating from a 2,3-dihydroxypropyl group and a polyoxyethylene group.

Abstract: Carrier polymer particles comprising organic polymer particles having a particle diameter of 0.1 to 20 micrometers and a saccharide with which the surface of the organic polymer particles is covered, the organic polymer particles and the saccharide being chemically bonded.

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 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: Carrier polymer particles comprising organic polymer particles having a particle diameter of 0.1 to 20 micrometers and a saccharide with which the surface of the organic polymer particles is covered, the organic polymer particles and the saccharide being chemically bonded.

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

Abstract: Crystals of a salt of 4?-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3?,5?-dimethylbiphenyl-4-carboxylic acid. The ? type, ? type and ? type crystals produced by treating hydrochloride of 4?-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3?,5?-dimethylbiphenyl-4-carboxylic acid with specified solvents, which can be discriminated by the characteristic diffraction peaks of powder X-ray diffractometry and the like.

Abstract: The present invention provides a novel crystal polymorph of ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride which can be determined by characteristic diffraction peaks of the powder X-ray diffraction or the like, and obtained from ethyl (?)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]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 an industrial method for preparing aminoalcohol derivatives (I) having a biphenyl group, biphenyloxyacetaldehyde derivatives which are used therefore, preparing methods thereof, and intermediates used for the preparing method. The present invention also provides a preparing method including processes for preparing a 3-substituted biphenylcarboxylic acid derivative represented by the following general formula: by allowing a 3-fluorobiphenylcarboxylic acid derivative prepared from a 3-fluorobiphenylcarbonitrile derivative which can be prepared by allowing a 4-halophenol derivative to react with a 2-fluorobenzonitrile derivative which is substituted by a leaving group at 4-position to react with an organometallic reagent.

Abstract: Carrier polymer particles comprising organic polymer particles having a particle diameter of 0.1 to 20 micrometers and a saccharide with which the surface of the organic polymer particles is covered, the organic polymer particles and the saccharide being chemically bonded.

Abstract: Crystals of a salt of 4?-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3?, 5?-dimethylbiphenyl-4-carboxylic acid. The ? type, ? type and ? type crystals produced by treating hydrochloride of 4?-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl-amino]ethoxy}-3-isopropyl-3?,5?-dimethylbiphenyl-4-carboxylic acid with specified solvents, which can be discriminated by the characteristic diffraction peaks of powder X-ray diffractometry and the like.

Abstract: The organic polymer particles comprise a carboxyl group and 2,3-dihydroxypropyl group, and the magnetic particles for diagnostics comprise fine magnetic material particles and a polymer part containing a hydrophilic polymer part and a crosslinked polymer part, a dry coating film obtained from a water dispersion thereof having a contact angle with water of 5° to 60°. The process for producing the carboxyl group-containing particles comprises a step of producing an ester bond by reacting a hydroxyl group in organic polymer particles having the hydroxyl group with a carboxylic anhydride. The organic polymer particles comprise a hydroxyl group originating from a 2,3-dihydroxypropyl group and a polyoxyethylene group.

Abstract: The present invention provides ethyl (?)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxy]acetate hydrochloride, crystalline forms thereof and pharmaceutical compositions containing them, which have excellent ?3-adrenoceptor stimulating effects, therapeutic effects on pollakiuria or urinary incontinence and storage stabilities and are useful as a medicament.

Abstract: The present invention provides ethyl (−)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxy]acetate hydrochloride, crystalline forms thereof and pharmaceutical compositions containing them, which have excellent &bgr;3-adrenoceptor stimulating effects, therapeutic effects on pollakiuria or urinary incontinence and storage stabilities and are useful as a medicament.