Akzo Nobel N.v.

N.v. Organon

Wilhelmus Gerardus Eduardus Joseph Schoonen

Hubert Jan Jozef Loozen

Gerrit Herman Veeneman

Disclosed is a novel class of steroid compounds based on estradiol, and carrying an 11&#x3b2;-substitution. Said substitution is a hydrocarbon group which may be linear or branched, provided that it comprises, as the longest chain on carbon atom no. 11 of the steroid skeleton, one single linear chain having a length of from 5 to 9 carbon atoms, wherein said chain may be saturated or unsaturated. The resulting compounds have a desirable mixed agonist/antagonist profile for estrogen receptor &#x3b1; and estrogen receptor &#x3b2;.

Estrogenic estra-1,3,5(10)-trienes with differential effects on the alpha and beta estrogen receptors, having a linear hydrocarbon chain of from 5-9 carbon atoms in position 11

Disclosed are novel, selective estrogens type having a steroid skeleton with a non-aromatic A-ring and a free or capped hydroxyl group at carbon atom No. 3. The estrogens satisfy general formula (I), in which R is H, (C -C )alkyl or (C -C )acyl; R is H, &agr;-(C -C )alkyl, &agr;-(C -C )alkenyl or &agr;-(C -C )alkynyl; R is H or (C -C )alkyl, (C -C )alkenyl or (C -C )alkynyl, each at location 15 or 16 of the steroid skeleton; R is H or (C -C )alkyl, (C -C )alkenyl or (C -C )alkynyl, each optionally substituted with halogen; preferred is ethynyl; R is H, (C -C )alkyl or (C -C )acyl; R is (C -C )alkyl, (C -C )alkenyl, (C -C )alkynyl or (C -C )alkylidene, each optionally substituted.

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Parklaan, Netherlands

Wilhelmus Gerardus Eduardus Joseph Schoonen