申请人:Asahi Kasei Kogyo Kabushiki Kaisha
公开号:US04166128A1
公开(公告)日:1979-08-28
Novel substituted phenylglycolic acid represented by the formula ##STR1## AND ITS PHARMACEUTICALLY ACCEPTABLE NON-TOXIC ESTERS AND SALTS HAVE POTENT ANALGESIC, ANTI-INFLAMMATORY AND ANTIPYRETIC ACTIVITIES, A LOW TOXICITY AND A SATISFACTORY THERAPEUTIC INDEX, AND CAN BE FAVORABLY EMPLOYED AS A MEDICINE FOR TREATMENT OF VARIOUS INFLAMMATORY DISEASES SUCH AS ARTHRITIS, COMMON COLD, RHEUMATISM AND LIKE INFLAMMATIONS AND ALSO FOR ANALGESIC AND ANTIPYRETIC PURPOSES. The substituted phenylglycolic acid is prepared by reacting a lower alkyl ester of 2-(2,6-dichloroanilino)phenylglycolic acid with a basic substance, which lower alkyl ester is also a novel compound and can be obtained starting from 1-(2,6-dichlorophenyl)indole-2,3-dione through 2-(2,6-dichloroanilino)phenylglyoxylic acid and, in turn, a lower alkyl ester of 2-(2,6-dichloroanilino)-phenylglyoxylic acid.
新型的取代苯基乙醇酸,化学式为##STR1##及其药用可接受的无毒酯和盐具有强效的镇痛、抗炎和退热活性,毒性低,治疗指数满意,可作为治疗各种炎症性疾病如关节炎、感冒、风湿病及类似炎症以及镇痛和退热用途的药物。取代苯基乙醇酸是通过将2-(2,6-二氯苯胺基)苯基乙醇酸的较低烷基酯与碱性物质反应制备的,这种较低烷基酯也是一种新型化合物,可以从1-(2,6-二氯苯基)吲哚-2,3-二酮出发,经过2-(2,6-二氯苯胺基)苯甘酸和依次是2-(2,6-二氯苯胺基)苯甘酸较低烷基酯获得。