Selective progesterone receptor modulators (SPRM) and stabilized estrogen level in patient
AssigneeBayer Pharma Aktiengesellschaft
InventorsMarcus-Hillert Schultze-Mosgau, Xinying Chang, Christian Seitz, Carsten Möller
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Abstract
The present invention is related to Selective Progesterone Receptor Modulators (SPRM) as described and defined herein, and covers the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of sexual hormone dependent diseases and gynaecological diseases in particular Endometriosis or Uterine Fibroids (UF), as a sole agent or in combination with other active ingredients wherein circulating endogenous estradiol concentration of treated women is maintained to a level in a range of 40 pg/mL to 85 pg/mL.
Claims20
A method comprising administering (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one (Compound 1) of formula (I)
- or a tautomer, or a pharmaceutically acceptable salt thereof, or a mixture of the foregoing, to a woman at a daily dosage of 1 mg to 5 mg for twelve (12) weeks to twenty-four (24) weeks for the treatment of one or more disorders associated with decreased estrogen selected from the group consisting of vulvar and vaginal atrophy, vaginal dryness, pruritus, dyspareunia, vasomotor instability manifested as hot flushes, and loss of bone mineral density,
- wherein the disorders associated with decreased estrogen are observed during administration of an SPRM other than Compound 1 but are reduced with administration of Compound 1 compared with administration of the SPRM other than Compound 1.
A method comprising administering (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one (Compound 1) of formula (I)
- or a tautomer, or a pharmaceutically acceptable salt thereof, or a mixture of the foregoing, to a woman having endometriosis or uterine fibroids, at a daily dosage of 1 mg to 5 mg for twelve (12) weeks to twenty-four (24) weeks, wherein the woman is at risk of developing one or more disorders associated with decreased estrogen selected from the group consisting of vulvar and vaginal atrophy, vaginal dryness, pruritus, dyspareunia, vasomotor instability manifested as hot flushes, and loss of bone mineral density, and
- wherein Compound 1 regulates the concentration of circulating endogenous estradiol in the woman to a level within the range of 40 pg/mL to 85 pg/mL during treatment with Compound 1, and wherein the one or more disorders is reduced.
A method comprising administering (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one (Compound 1) of formula (I)
- or a tautomer, or a pharmaceutically acceptable salt thereof, or a mixture of the foregoing, to a woman at a daily dosage of 1 mg to 5 mg for twelve (12) to twenty-four (24) weeks for the treatment of at least one disorder associated with decreased estrogen selected from the group consisting of vulvar and vaginal atrophy, vaginal dryness, pruritus, dyspareunia, vasomotor instability manifested as hot flushes, and loss of bone mineral density,
- wherein the woman was previously treated for Endometriosis or Uterine Fibroids (UF) with ulipristal acetate (UPA), or a Gonadotrophin-Releasing Hormone (GnRH) analogue selected from the group consisting of leuprolide and elagolix, and exhibited a decreased circulating endogenous estradiol concentration in blood plasma during treatment with the ulipristal acetate (UPA), leuprolide or elagolix, and wherein the woman experienced at least one disorder associated with decreased estrogen upon treatment with the ulipristal acetate (UPA), leuprolide or elagolix.
Dependencies are inferred from the claim text.