17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone derivative, use thereof, and medicament containing the derivative
View Patent ↗The invention relates to 17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone derivatives with the chemical formula I, where R 4 , R 6a , R 6b , R 7 , R 15 , R 16a , R 16b , R 18 and Z have the meanings stated in claim 1 , and their solvates, hydrates, stereoisomers and salts. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.
1. A 17-Hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone selected from
17β-Hydroxy-7α-vinyl-19-nor-17α-pregna-4,20(Z)-dien-3-one-21-carboxylic acid γ-lactone;
6,6-(1,2-Ethanediyl)-17β-hydroxy-19-nor-17α-pregna-4,20(Z)-dien-3-one-21-carboxylic acid γ-lactone;
16,16-(1,2-Ethanediyl)-17β-hydroxy-19-nor-17α-pregna-4,20(Z)-dien-3-one-21-carboxylic acid γ-lactone;
17β-Hydroxy-7α-vinyl-18-methyl-19-nor-17α-pregna-4,20(Z)-dien-3-one-21-carboxylic acid γ-lactone;
6,6-(1,2-Ethanediyl)-17β-hydroxy-18-methyl-19-nor-17α-pregna-4,20(Z)-dien-3-one-21-carboxylic acid γ-lactone;
4-Chloro-17β-hydroxy-18-methyl-19-nor-17α-pregna-4,20(Z)-dien-3-one-21-carboxylic acid γ-lactone and
4-Chloro-17β-hydroxy-19-nor-17α-pregna-4,20(Z)-dien-3-one-21-carboxylic acid γ-lactone.
2. A method for oral contraception comprising administering to subject in need thereof an effective amount of the 17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone compound as claimed in claim 1 .
3. A medicinal product containing at least one 17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone compound as claimed in claim 1 and at least one suitable pharmaceutically harmless carrier substance.
4. The medicinal product as claimed in claim 3 , additionally containing at least one estrogen.
5. The medicinal product as claimed in claim 4 , characterized in ha the estrogen is ethinylestradiol.
6. The medicinal product as claimed in claim 4 , characterized in that the estrogen is estradiol valerate.
7. The medicinal product as claimed in claim 4 , characterized in that the estrogen is a natural estrogen.
8. The medicinal product as claimed in claim 7 , characterized in that the natural estrogen is estradiol.
9. The medicinal product as claimed in claim 7 , characterized in that the natural estrogen is a conjugated estrogen.
10. A medicinal product for intrauterine use, comprising the 17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone compound as claimed in claim 1 and at least one additive.
11. An intrauterine system (IUS), comprising the 17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone compound as claimed in claim 1 and at least one additive.