15,16-Methylene-17-hydroxy-19-nor-21-carboxylic acid-steroid gamma-lactone derivative, use thereof and medicinal products containing the derivative

摘要

Disclosed are 15,16-methylene-17-hydroxy-19-nor-21-carboxylic acid-steroid g-lactone derivatives and their solvates, hydrates, stereoisomers and salts, as represented by the general formula (I), in which Z is selected from the group comprising oxygen, two hydrogen atoms, NOR' and NNHSO2R'; R4 is selected from the group comprising hydrogen, fluorine, chlorine or bromine; R18 is hydrogen or alkyl; and wherein the remaining substituents are as defined herein. Representative compounds as disclosed herein include 17b-hydroxy-15a,16a-methylene-19-nor-17a-pregna-4,20(Z)-dien-3-one-21-carboxylic acid g-lactone, 17b-hydroxy-7a-cyclopropyl-15b,16b-methylene-19-nor-17a-pregna-4,20(Z)-dien-3-one-21-carboxylic acid g-lactone and 17a-pregna-4,20(Z)-dien-3-one-21-carboxylic acid g-lactone. Further disclosed is a medicinal product (such as an intrauterine system (IUS)) which contains at least one 15,16-methylene-17-hydroxy-19-nor-21-carboxylic acid-steroid g-lactone derivative as defined above and at least one suitable pharmaceutically harmless additive for oral contraception or for the treatment of pre-, peri- and postmenopausal complaints.