Patent Evaluation: Camphor derivatives as oxytocin antagonists

Novelty: Novel piperazinyl(su1phon)amide derivatives of camphor are claimed as oxytocin antagonists. They are potentially useful for preventing preterm labour and for stopping labour prior to caesarian delivery.Biology: A radioligand binding assay using a crude membrane preparation of uteri from DES-treated rats is described. The specified compound gave an IC50 value of 5.4nM.Chemistry: Over one hundred compounds are exemplified. Two compounds are specifically claimed including 1 -((7,7-dimethyl-2-endo-(2S-(dimethylamino)-4-(methylsulphonyl)butyr-ido)-bicyclo [2.2.1] heptan- 1 - yl)-methanesulphony1)-4-(2-methyl-pheny1)piperazine.