Aromatic amidocarboxylic acids and pharmaceutical compositions thereof

Abstract

Abstract New aromatic amidocarboxylic acid derivatives of the general formula: ##STR1## wherein R 1 and R 2 each represent a hydrogen atom or an alkyl gp with 1-4 carbon atoms; R 3 and R 4 each represent a hydrogen atom or may be combined together to form an additional chemical bond; X represents a hydroxyl group, a halogen atom, a straight or branched chain saturated or unsaturated alkyl group with 1-4 carbon atoms, a straight or branched chain saturated or unsaturated alkoxy group with 1-4 carbon atoms, an acyloxy group with 1-4 carbon atoms, or a cycloalkyl group with up to 6 carbon atoms; n is zero or an integer of 1-3 with the proviso that when n is 2 or 3, X's may be the same or different and that when two X's are commonly the alkyl or alkoxy group, both X's may be combined together to form a ring; and Y represents a straight or branched chain alkylene group or a straight or branched chain oxyalkylene group connected to the benzene nucleus through an oxygen atom, as well as physiologically acceptable salts thereof. The new compounds possess a strong antiallergic effect and are thus useful for the treatment of asthma, hay fever, urticaria and atopic dermatitis. The above-mentioned aromatic amidocarboxylic acid and a salt thereof are prepared, for example, by reacting a reactive functional derivative of the general formula: ##STR2## wherein R 1 , R 2 , R 3 , R 4 , X and n have the same meanings as given above, with an aminophenylalkylcarboxylic acid derivative or an aminophenoxyalkylcarboxylic acid dervative of the general formula: ##STR3## wherein Y has the same meaning as given above, and if desired, converting the resulting amidocarboxylic acid into a corresponding salt thereof or vice versa.

Inventors

• 👤 Kozaburo Harita
• 👤 Yukiyoshi Ajisawa
• 👤 Kinji Iizuka
• 👤 Michio Toda
• 👤 Yukihiko Kinoshita
• 👤 Tetsuhide Kamijo
• 👤 Michihiro Kobayashi

Bibliographic Details