INDOLE-2-CARBOXYLIC ACID DERIVATIVE

摘要

PROBLEM TO BE SOLVED: To obtain the subject new compound that has little harmful side effect and high in-vivo activity, and is useful an excellent selective antagonist for glycine binding site of N-methyl-D-aspartic acid receptor. SOLUTION: This new compound is an indole-2-carboxylic acid derivative of formula I (X<1> , X<2> are independently H, an alkyl, halogen, cyano, etc.; R<1> is H, a carboxyl-protective group; R<2> is H or an alkyl; A is an acidic residue or group capable of being converted into an acid residue in vivo; E is a basic residue or group capable of being converted into a base residue in vivo; J is dimethylene or vinylene; Y is a single bond, alkylene etc.; Z is a single bond, or alkylnen) or its pharmacologically permissible salt, e.g. a compound of formula II. The compound of formula I is obtained, for example, by condensing a compound of formula III with a compound of formula IV [E<0> is a group of NHL<1> (L<1> is an amino acid, etc.); A<0> is a protected carboxyl[ followed by deprotection.