5-{2-hydroxy-3-'1-(3-trifluoromethylphenyl)-cyclopropyl-propionylamino}-phtalide and related compounds with progesterone receptor modulating activity for use in fertility control and hormone replacement therapy

Non-steroidal progestins of formula (I) are disclosed, wherein R1 and R2 are independently of each other -H or -F, R3 is -CH3 or -CF3, and Ar is (a) or (b), or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor...

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Bibliographische Detailangaben
Hauptverfasser: FUHRMANN, ULRIKE, KLOTZBUCHER, MICHAEL, SCHMEES, NORBERT, HEGELE-HARTUNG, CHRISTA, LEHMANN, MANFRED, MUHN, PETER
Format: Patent
Sprache:eng
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Zusammenfassung:Non-steroidal progestins of formula (I) are disclosed, wherein R1 and R2 are independently of each other -H or -F, R3 is -CH3 or -CF3, and Ar is (a) or (b), or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, these progestins, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. Methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs are also described.