Mesoprogestins (progesterone receptor modulators) as a...

A - Human Necessities – 61 – K

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A61K 31/567 (2006.01) A61P 5/34 (2006.01)

Patent

CA 2383659

The present invention refers to the use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as component for the combined use together with an estrogen for the man-ufacture of a medicament for HRT as well as in respective HRT-methods and methods of treating hormone deficiency and hormone irregularity symptoms. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the proges-terone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. J867, J912, J956 and J1042 are the mesoprogestins preferred according to the invention.

La présente invention concerne l'utilisation de mésoprogestines comme composants pharmaceutiques pour la fabrication d'un médicament de traitement hormonal substitutif et comme composant prévu pour être associé avec un oestrogène dans la fabrication d'un médicament de traitement hormonal substitutif. La présente invention concerne également des procédés de traitement hormonal substitutif et de traitement de carence hormonale et de symptômes d'irrégularités hormonales. Les mésoprogestines sont définies comme des composés exerçant une activité agoniste et antagoniste au niveau du récepteur de progestérone in vivo. Elles stabilisent la fonction du récepteur de progestérone à un niveau intermédiaire des activités agonistes et antagonistes. Des états fonctionnels correspondants ne peuvent pas être obtenus avec des progestines ou des antiprogestines. Selon l'invention, les mésoprogestines préférées sont les J867, J912, J956 et J1042.

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