Abstract:
PROBLEM TO BE SOLVED: To establish a method for simply quantifying a dimethylaminoethyl methacrylate-containing copolymer in a preparation without being affected by a reagent used in elution pretreatment. SOLUTION: After the preparation containing the dimethylaminoethyl methacrylate-containing copolymer is dissolved in an extraction solvent containing a surfactant and an alkylamine derivative to dry an extracted component, it is dissolved in d6-acetone containing d-trifluoroacetic acid to measure 1H-NMR to thereby quantify the dimethylaminoethyl methacrylate-containing copolymer. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a light-stable imidafenacin-containing rapidly orally disintegrating tablet. SOLUTION: The rapidly orally disintegrating tablet is prepared by mixing granules produced by spraying an excipient with imidafenacin, tocopherol or a tocopherol derivative, and at least one binder selected from the group consisting of an acrylic polymeric substance, a vinyl polymeric substance, and stearyl alcohol with an excipient and a disintegrator without subjecting to coating treatment and compression-molding the resultant mixture, wherein the content of the tocopherol or tocopherol derivative contained in the granules is 0.05-10 pts.mass per pt.mass imidafenacin, and the content of the binder is 0.1-30 pts.mass per pt.mass imidafenacin. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a novel method of producing 5-methyl-2-(piperidine-4-ylamino)pyridine. SOLUTION: There is disclosed a production method shown in formula (in the formula, R represents a 1-6C straight chain or branched alkyl group, or an aryl 1-6C alkyl group). Namely the method of producing a 4-(5-methylpyridine-2-ylamino)piperidine-1-carboxylic acid derivative includes causing 2-amino-5-methylpyridine and a 4-piperidone-1-carboxylic acid derivative to react with each other in a solvent in the presence of a Lewis acid and a reducing agent. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a novel dimerized cyclo derivative having an excellent DPP-IV inhibitory activity or a pharmacologically acceptable salt thereof, and to provide a prophylactic and/or therapeutic agent for a DPP-IV-related disease which comprises the derivative or the pharmacologically acceptable salt thereof as an active ingredient. SOLUTION: There is disclosed a dimerized cyclo derivative represented by general formula (1) or a pharmacologically acceptable salt thereof (e.g., 1,2-ethanediol bis[4-[2-[(2S, 4S)-2-cyano-4-fluoropyrrolidin-1-yl]acetyl]aminobicyclo[2.2.2]octane-1-carboxylate]). COPYRIGHT: (C)2010,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a phenol derivative useful as a medicine having excellent S1P3 (sphingosine-1-phosphate-3 receptor) antagonist activity. SOLUTION: There is provided the phenol derivative represented by general formula (1) [wherein, R 1 is H or PO(OH) 2 ], its pharmacologically acceptable salt or hydrate. COPYRIGHT: (C)2010,JPO&INPIT