16-hydroxyestratrienes as selective estrogens

Details 16-hydroxyestratrienes as selective estrogens 16-hydroxyestratrienes as selective estrogens

C - Chemistry, Metallurgy

07

J

C07J 53/00 (2006.01) A61K 31/565 (2006.01) C07J 1/00 (2006.01) C07J 15/00 (2006.01) C07J 31/00 (2006.01) C07J 33/00 (2006.01) C07J 41/00 (2006.01)

Patent

CA 2359660

The invention relates to novel compounds as pharmaceutical agents which have in vitro a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparations of the rat uterus and which preferably have in vivo a preferential effect on bones as compared to the uterus and/or a marked effect with regard to the stimulation of the expression of the 5HT2a receptor and transporter. The invention also relates to the production and to the use in therapy of these compounds and to pharmaceutical administration forms containing said novel compounds. The novel compounds are 16.alpha. and 16.beta. hydroxy-estra,1,3,5(10)-estratriene which carry additional substituents at the steroid backbone and one or more additional double bonds on the B, C and/or D rings.

Cette invention concerne de nouveaux composés utilisés comme agents pharmaceutiques, présentant, in vitro, vis à vis de préparations de récepteurs des oestrogènes de la prostate de rats, une affinité supérieure à celle vis à vis de préparations de récepteurs des oestrogènes de l'utérus de rats, et ayant de préférence, in vivo, une action plus marquée sur les os que sur l'utérus et/ou une action caractéristique en ce qui concerne la stimulation de l'expression du récepteur et du transporteur 5HT2a. Cette invention concerne également la production desdits composés, leur utilisation thérapeutique et les formes pharmaceutiques qui contiennent les nouveaux composés. Ces nouveaux composés sont le 16.alpha.-hydroxy-estra,1,3,5(10)-estratriène et le 16.beta.-hydroxy-estra,1,3,5(10)-estratriène, lesquels peuvent comporter dans leur structure stéroïde d'autres substituants ainsi que présenter une ou plusieurs double(s) liaison(s) supplémentaire(s) dans les cycles B, C et/ou D.

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