17-side chain alkynyl-and 20-oxopregna-derivatives of vitamin D, methods for their production and pharmaceutical compositions thereof

摘要

1-Hydroxy pregnacalciferol derivatives of formula (I) and their corresponding 5,6-trans isomers wherein R¹ is hydroxyl or lower alkoxy and R² is optionally hydroxylated or lower alkoxylated lower alkynyl or R¹ is C(R^A) (R^B)CH₃ where R^A is optionally hydroxylated or lower alkoxylated lower alkynyl and R^B is hydroxyl or lower alkoxy or R^A and R^B together represent oxo and R² is hydrogen, hydroxyl or lower alkoxy, and R³ and R⁴ represent hydrogen atoms, exhibit anti-progesterone activity and may be useful as antineoplastic, antifertility, antiproliferative, immunosuppressive and/or antiinflammatory agents.