11Beta-long-chain-substituted 19-nor-17alpha-pregna-1,3,5(10)-trien-17beta-ols with a 21,16alpha-lactone ring
AssigneeSchering Corporation
InventorsGerd Mueller, Jens Hoffmann, Karl-Heinrich Fritzemeier, Alexander Hillisch
Life of this patent
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Abstract
This invention relates to new 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring with a long-chain substituent in 11β-position of general formula II 1 in which R11 means a straight-chain alkyl radical with 6 to 17 carbon atoms, and R3 and R13 have the meanings that are explained in more detail in the description. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.
Claims9
19-Nor-17α-pregna-1,3,5(10)-trienes with a 21,16α-lactone ring of general formula (II)
- 15
- in which
- R3 means a hydrogen atom, a C1-4-alkyl, C2-6-acyl or tri(C1-4-alkyl)silyl group or a group R18SO2—,
- whereby
- R18 means a group R19R20N—,
- in which
- R19 and R20, independently of one another, are a hydrogen atom, a C1-5-alkyl radical, a group C(O)R21 and
- in which
- R21 means a straight-chain or branched hydrocarbon radical with up to 6 carbon atoms, a C3-7-cycloalkyl radical, an aryl radical, an aralkyl radical or an alkylaryl radical,
- and
- R11 means a straight-chain alkyl radical with 6 to 17 carbon atoms, and
- R13 means a methyl or ethyl group.
Dependencies are inferred from the claim text.