Patent ID: 6677344
Filing Date: 2004-01-13
Classification: A61K,A61P,C07D

Abstract:
A method for the treatment of a disease involving an increase of eosinophils comprising administering to a patient in need of such treatment a chymase inhibitor in an amount effective for treatment of said disease,wherein the chymase inhibitor is a quinazoline derivative having the following formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents an aryl group;R1 represents a hydroxyl group, an amino group, a C1 to C4 lower alkylamino group which may optionally be substituted with a carboxylic acid group, a C7 to C10 lower aralkylamino group which may optionally be substituted with a carboxylic acid group, an amino group acylated with a C1 to C4 lower aliphatic acid which may optionally be substituted with a carboxylic acid group, an amino group acylated with an aromatic ring carboxylic acid which may optionally be substituted with a carboxylic acid group, an amino group acylated with a heteroaromatic ring carboxylic acid which may optionally be substituted with a carboxylic acid group, wherein the heteroaromatic ring is selected from pyridine and pyrrole, an amino group sulfonylated with a C1 to C4 lower alkanesulfonic acid which may optionally be substituted with a carboxylic acid group, an amino group sulfonylated with an aromatic ring sulfonic acid which may optionally be substituted with a carboxylic acid group, an amino group sulfonylated with a heteroaromatic ring sulfonic acid which may optionally be substituted with a carboxylic acid group, wherein the heteroaromatic ring is selected from pyridine and pyrrole, a C1 to C4 lower alkyl group substituted with a carboxylic acid group, or a C2 to C4 lower alkylene group which may optionally be substituted with a carboxylic acid group; R2 and R3 may be the same or different and represent a hydrogen atom, an unsubstituted or substituted C1 to C4 lower alkyl group, a halogen atom, a hydroxyl group, a C1 to C4 lower alkoxyl group, an amino group, a C1 to C4 lower alkylamino group which may optionally be substituted with a carboxylic acid group, a halogen atom, or a C1 to C4 lower alkoxyl group, a C7 to C10 aralkylamino group which may optionally be substituted with a carboxylic acid group, a halogen atom, or a C1 to C4 lower alkoxyl group, an amino group acylated with a C1 to C4 lower aliphatic acid which may optionally be substituted with a carboxylic acid group, an amino group acylated with an aromatic ring carboxylic acid which may optionally be substituted with a carboxylic acid group, an amino group acylated with a heteroaromatic ring carboxylic acid which may optionally be substituted with a carboxylic acid group, wherein the heteroaromatic ring is selected form pyridine and pyrrole, an amino group sulfonylated with a C1 to C4 lower alkanesulfonic acid which may optionally be substituted with a carboxylic acid group, an amino group sulfonylated with an aromatic ring sulfonic acid which may optionally be substituted with a carboxylic acid group, an amino group sulfonylated with a heteroaromatic ring sulfonic acid which may optionally be substituted with a carboxylic acid group, wherein the heteroaromatic ring is selected from pyridine and pyrrole, or a carboxylic acid group or when the ring A is a benzene ring, R1 and R2 may form, together with the substituting benzene ring, a fused heterocyclic ring selected from the group consisting of a tetrahydroquinoline ring and a benzoxazine ring, which may optionally be substituted with a carboxylic acid and in which the carbon atom in the ring may form a carbonyl group and R3 is the same as defined above; and X represents a hydrogen atom, a C1 to C4 lower alkyl group, a C1 to C4 lower alkoxy group, a halogen atom, a hydroxyl group, an amino group, or a nitro group.