Steroids having pro-oestrogenic activity

摘要

The invention comprises steroids having at the A and B rings the partial structure wherein R1 is a b -hydroxy or b -acyloxy group and R2 is a hydrogen atom or R1 and R2 together form an oxo group, and R5 and R6 together form an oxide or lactone bridge, the broken line between the 1- and 2-positions indicating a carbon-carbon bond which may be present or absent, there being no 1(2)-double bond present when there is an oxo group or an acetyl group at the 17-position. These steroids may also have at position 17 an aliphatic hydrocarbon (e.g. methylene) group. The lactones according to the invention in which R1 and R2 together form an oxo group may be prepared by oxidation of dioxides of partial formula wherein Hal is a halogen atom (the preparation of the latter being described in Specification 1,110,792), or by oxidation of hemiacetals of partial formula wherein R is a hydrogen atom or acyl group and Hal has the above significance (the preparation of the latter being described in Specification 1,110,792) followed by elimination of the 5a -halogen atom. The 6b ,19-oxides according to the invention (wherein R1 and R2 together form an oxo group) may be prepared by oxidizing a steroid of partial structure wherein Hal has the above significance (the preparation of the latter being described in Specification 1,046,243). Other steroids of partial Formula (I) can be prepared from the aforementioned products by known methods. 17-Methylene steroids of partial Formula (I) may be obtained from the corresponding 17-keto compounds by reaction with a triaryl-methylphosphonium salt (Wittig reaction). Pharmaceutical compositions suitable for oral, parenteral, rectal or topical administration comprise one or more steroids of partial Formula (I) in conjunction with a pharmaceutical carrier or excipient. The active ingredient is stated to possess pro-estrogenic activity. Reference has been directed by the Comptroller to Specification 994,746.