| 摘要 |
<p>Sulphonamides of formula (I) are their salts when R2 = H, are new: R1 = H, Cl or Br. R2 = H or 1-4c alkyl. R3 =H, 1-4C alkyl, 3-5C alkenyl or alkynyl (the unsaturation is not alpha to the N atom), 5-6C cycloalkyl or 2-4C hydroxyalkyl with the OH separated from the N by >=2C. R4 = any R3 gp. other than H; or is additionally phenyl or phenyl (1-4C)alkyl (opt. ring substd. by 1 or 2 F, Cl, Br or by one 1-4C alkyl or alkoxy), or pyridyl or pyrimidinyl (opt. substd. by 1 or 2 methyl), when R3 = H or 1-4C alkyl. also R3 and R4 can together complete pyrrolidino, piperidino or morpholino. (I) are prepd. e.g. from R3R4NH and corresp. sulphonyl chloride. (I) are useful in prevention or treatment of allegic asthma or asthma induced by exertions, and for prophylaxis of other allergies. The daily dose is 0.5-300 mg/kg in usual oral, rectal or parenteral forms. A typical cpd., methyl 2-chloro-5-dimethylsulphamoylbenzene-1,3-dioxamate, was prepd. from Me2NH and 4-chloro-3,5-bis(methoxyoxalylamino)benzenesulphonyl chloride.</p> |
