Abstract: The present invention herein provides a simple, efficient and industrially useful method for purifying an aminoacetylpyrrolidinecarbonitrile derivative which is useful as a DPP-IV inhibitor. The method comprises the steps of acting an acid such as maleic acid on an aminoacetylpyrrolidinecarbonitrile derivative represented by the following Formula 1 to form a salt, isolating the salt and then regenerating the foregoing derivative from the salt: (In the formula, A represents CH2, CHF or CF2; R represents a C1 to C6 alkyl group which may have a substitutent, a C3 to C8 cycloalkyl group which may have a substitutent, an arylmethyl group which may have a substitutent, an arylethyl group which may have a substitutent, an aromatic hydrocarbon ring which may have a substitutent, an aromatic hetero ring which may have a substitutent, or an aliphatic hetero ring which may have a substitutent; and n represents 1 or 2).

Abstract: Novel intermediates for the production of aminoacetyl pyrrolidine carbonitrile derivatives ensure the safe and efficient production of the compounds. Specifically, the present invention provides a sulfonyloxyacetyl pyrrolidine derivative, represented by the following formula: (Chemical Formula 1) (wherein R1 is a substituted or unsubstituted C1-C6 alkyl group, a substituted or unsubstituted C3-C6 cycloalkyl group, a substituted or unsubstituted arylmethyl group, a substituted or unsubstituted aromatic hydrocarbon, a substituted or unsubstituted aromatic heterocyclic ring or a substituted or unsubstituted aliphatic heterocyclic ring; R2 is CONH2 or CN; and X is CH2, CHF or CF2.

Abstract: Novel intermediates for the production of aminoacetyl pyrrolidine carbonitrile derivatives ensure the safe and efficient production of the compounds. Specifically, the present invention provides a sulfonyloxyacetyl pyrrolidine derivative, represented by the following formula: (Chemical Formula 1) (wherein R1 is a substituted or unsubstituted C1-C6 alkyl group, a substituted or unsubstituted C3-C6 cycloalkyl group, a substituted or unsubstituted arylmethyl group, a substituted or unsubstituted aromatic hydrocarbon, a substituted or unsubstituted aromatic heterocyclic ring or a substituted or unsubstituted aliphatic heterocyclic ring; R2 is CONH2 or CN; and X is CH2, CHF or CF2.

Abstract: The invention provides 4-substituted aryl-5-hydroxyisoquinolinone derivatives and their pharmacologically acceptable addition salts with excellent inhibitory effect on poly (ADP-ribose) synthetase. 4-Substituted aryl-5-hydroxyisoquinolinone derivatives, represented by a general formula (1) and their pharmacologically acceptable addition salts.

Abstract: The invention provides 4-substituted aryl-5-hydroxyisoquinolinone derivatives and their pharmacologically acceptable addition salts with excellent inhibitory effect on poly (ADP-ribose) synthetase. 4-Substituted aryl-5-hydroxyisoquinolinone derivatives, represented by a general formula (1) and their pharmacologically acceptable addition salts.

Abstract: The invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor having 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives and addition salts thereof as effective ingredients, and processes for the preparation of both. The compounds are 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives represented by the formula (1) where A denotes a single bond or methylene (CH2), Y denotes a nitrogen atom or ═CH—, V denotes a single bond or methylene (CH2), T denotes a hydroxyl group, amino group, lower alkoxycarbonyl group, carboxyl group, aldehyde group or the like, Q denotes a halogen atom, lower alkyl group or lower alkoxy group, and R1 denotes a hydroxyl group, lower alkoxy group or the like, and addition salts thereof.

Abstract: The present invention provides 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid compounds and their addition salts, and processes for preparing them, which have antagonism against excitatory amino acid receptors, in particular, an AMPA receptor. The 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid compounds and their addition salts of the present invention are represented by formula (1) wherein Q, R, R1 and R2 are as described in the specification.