申请人:Kissei Yakuhin Kogyo Kabushiki Kaisha
公开号:US03940422A1
公开(公告)日:1976-02-24
Novel aromatic carboxylic amides of the general formula: ##EQU1## wherein each of R.sub.1 and R.sub.2 is a hydrogen atom or an alkyl group having 1-4 carbon atoms, R.sub.3 and R.sub.4 are hydrogen atoms or together form another chemical bond, each X is a hydroxyl group, a halogen atom, an alkyl group having 1-4 carbon atoms and an alkoxy group containing 1-4 carbon atoms, and n is an integer of 1-3, with the proviso that when two Xs are alkyl or alkoxy groups, they may be connected together to form a ring, as well as pharmaceutically acceptable salts thereof. These compounds possess a strong antiallergenic action and are thus useful for treatment of asthma, hay fever, anticaria and atopic dermatitis. The above aromatic carboxylic amides can be prepared by reacting a reactive functional derivative of the general formula: ##EQU2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and n have the same meanings given above, with an aminobenzoic acid of the formula: And, if desired, converting the resulting amide into the corresponding salts.
通用公式为:##EQU1##,其中R.sub.1和R.sub.2中的每一个都是氢原子或具有1-4个碳原子的烷基基团,R.sub.3和R.sub.4是氢原子或共同形成另一个化学键,每个X是羟基、卤素原子、具有1-4个碳原子的烷基基团和含有1-4个碳原子的烷氧基,n是1-3的整数,但两个X是烷基或烷氧基时,它们可以连接在一起形成一个环,以及其药学上可接受的盐。这些化合物具有强大的抗过敏作用,因此对治疗哮喘、花粉症、荨麻疹和特应性皮炎有用。上述芳香族羧酰胺可通过将通用公式的反应性功能衍生物:##EQU2##,其中R.sub.1、R.sub.2、R.sub.3、R.sub.4、X和n具有上述相同的含义,与具有以下结构的氨基苯甲酸反应来制备。如果需要,将所得酰胺转化为相应的盐。