A one-pot process for the preparation of nateglinide which process comprises reacting an alkyl ester of D-phenylalanine of formula (II): where R represents C1-4alkyl typically methyl either as the free base or in salt form (typically the hydrochloride) with trans-4-isopropylcyclohexanecarboxylic acid of formula (III): where X represents hydroxy or halo typically chloro to obtain a C1-4 alkyl ester of nateglinide of formula (IV) preferably the methyl ester of nateglinide: followed by hydrolysis t...

The present invention provides a pharmaceutical composition comprising a compound represented by the formula (I):wherein each symbol is as defined in the description or a salt thereof in combination with a dipeptidyl peptidase IV inhibitor an insulin preparation a PPAR function modulator an ±-glucosidase inhibitor a biguanide a sulfonylurea mitiglinide or calcium salt hydrate thereof or nateglinide.

New nateglinide crystals i. e. nateglinide A-type crystals (main peaks in powder X-ray diffraction: 4.4 DEG 5.2 DEG 15.7 DEG 18.5 DEG (2&thetas;)) M-type crystals (main peaks in powder X-ray diffraction: 6.0 DEG 14.2 DEG 15.2 DEG 18.8 DEG (2&thetas;)) and P-type crystals (main peaks in powder X-ray diffraction: 4.8 DEG 5.3 DEG 14.3 DEG 15.2 DEG (2&thetas;)) can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which...

Abstract - 603255 Disclosed is the compound 2-(3-(cyclopropylmethyl)-2-oxo-imidazolidin-1-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide or a pharmaceutically acceptable salt thereof. Further disclosed is a pharmaceutical composition comprising a therapeutically effective amount of the compound 2-(3-(cyclopropylmethyl)-2-oxoimidazolidin-1-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide or a pharmaceutically acceptable salt thereof optionally in combination with a therapeutic...

The present invention provides a small-sized preparation that is easy to take containing 26% or more of nateglinide and 28% or more of at least one disintegrant selected from the group consisting of carmellose or salts thereof sodium carboxymethyl starch croscarmellose sodium crospovidone partly pregelatinized starch and low-substituted hydroxypropyl cellulose based on the total mass of the preparation. The preparation of the present invention has high contents of nateglinide which can be absorb...

There is provided a nateglinide-containing hydrophilic pharmaceutical preparation comprising nateglinide B-type crystals as an effective ingredient the contact angle of the surface of said preparation to water becoming 111 degree or less by incorporating in said preparation at least one hydrophilic substance selected from the groups consisting of hydrophilic polymers surfactants sugars sugar alcohols and salts. This preparation is one having sufficient immediate-release and high dissolution prop...

One-pot process for the preparation of nateglinide which process comprises reacting an alkyl ester of D-phenylalanine of formula (II) where R represents C1-4alkyl typically methyl either as the free base or in salt form (typically the hydrochloride) with trans-4-isopropylcyclohexanecarboxylic acid of formula (III) where X represents hydroxy or halo typically chloro to obtain a C1-4 alkyl ester of nateglinide of formula (IV) preferably the methyl ester of nateglinide followed by hydrolysis to yie...