Sulfamate derivatives of 1,3,5(10)-estratriene derivatives, methods for their production and pharmaceuticals containing these compounds
AssigneeJenapharm GmbH & Co. KG
InventorsSigfrid Schwarz, Walter Elger, Gudrun Reddersen, Birgitt Schneider, Ina Thieme, Margit Richter
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Abstract
The invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compound and pharmaceutical preparations containing this compound are described. The compounds according to the invention have an estrogenic effect.
Claims3
Sulfamate derivatives of the general formula I ##STR5## wherein R.sup.1 is a --CO--R.sup.3, --CO--OR.sup.4, --CO--NR.sup.5 R.sup.6, --SO.sub.2 --R.sup.4 or --SO.sub.2 --NU.sup.5 R.sup.6 group,
- in which
- R.sup.3 is a hydrogen atom or is as defined in R.sup.4,
- R.sup.4 represents a C.sub.1 -C.sub.5 alkyl residue, a C.sub.2 -C.sub.5 alkenyl residue, a C.sub.3 -C.sub.6 cycloalkyl residue or an aryl residue containing up to 9 carbon atoms,
- R.sup.5 and R.sup.6 are independent of each other and represent a hydrogen atom, a C.sub.1 -C.sub.5 alkyl residue, an aryl residue containing up to 9 carbon atoms, or, together with the N atom, represent a polymethylene imino residue containing 3 to 6 carbon atoms, or a morpholino residue,
- R.sup.2 is a hydrogen atom or a physiologically tolerable metal, or is as defined in R.sup.4,
- R.sup.7 and R.sup.8 are independent of each other and represent a hydrogen atom, a hydroxy group or a C.sub.1 -C.sub.5 alkoxy residue,
- R.sup.9 and R.sup.10 each represent a hydrogen atom, or together represent a methylene group,
- R.sup.11, R.sup.12 and R.sup.13 are independent of each other and represent a hydrogen atom or a hydroxy group that may optionally be esterified with physiologically tolerable inorganic or organic acids,
- or R.sup.12 or R.sup.13 is an alkinyl residue containing up to 5 carbon atoms,
- rings B and C may optionally contain one or two double bonds,
- and R.sup.8, R.sup.11 and R.sup.12 are independently placed either at the .alpha.- or .beta.-position.
Dependencies are inferred from the claim text.