Steroidal quinols and their use for estrogen replacement...

A - Human Necessities – 61 – K

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A61K 31/565 (2006.01) A61K 31/566 (2006.01) A61K 31/567 (2006.01) A61P 5/30 (2006.01)

Patent

CA 2539661

The present invention relates to novel estrogen-related steroidal quinols and their use as drugs for estrogen replacement therapy. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution into tissues, bone, in the cardiovascular system, and in the CNS (central nervous system) with only a slight estrogenic action or no estrogenic action in the uterus. The compounds are suitable for the production of pharmaceutical agents for use in numerous indications (for example, estrogen replacement therapy, prevention and treatment of osteoporosis).

La présente invention concerne des quinoles stéroïdes liées à l'oestrogène et l'utilisation de celle-ci comme médicament de thérapie de remplacement d'oestrogène. Ces quinoles présentent des propriétés physico-chimiques améliorées, une biodisponibilité améliorée et une meilleure répartition dans les tissus, les os, dans le système cardio-vasculaire et dans le système nerveux central (SNC) avec uniquement une légère action oestrogénique ou non oestrogénique dans l'utérus. Ces composés conviennent pour la production d'agents pharmaceutiques destinés à de nombreuses indications (par exemple thérapie de remplacement d'oestrogène, prévention et traitement de l'ostéoporose).

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