Patent Evaluation: Use of Piperidines in the Treatment of Breast Cancer

Summary

Novelty: Piperidine-2,6-dione derivatives proposed to be aromatase inhibitors are disclosed. These compounds may be useful for the treatment of androgen dependent disorders such as neoplasms and more specifically, prostatic cancer.

Biology: Clinical trials in ten post-menopausal patients with advanced breast cancer are reported. It was observed that pyridoglutethimide did not affect the mean Cortisol and aldosterone levels. However, there was a progressive dose-related fall in dehydroepiandrostenane sulphate (< 50% at the highest dose), testosterone and androstenedione levels.

Chemistry: Details of preparation are disclosed in UK patents 2,151,226 and 2,216,524.