METHOD OF HORMONE SUPPRESSION IN HUMANS
The present invention relates to a glycine transporter-1 inhibitor having the formula (I) wherein X is 1-3 substituents selected from H, halogen, methyl, methoxy, trifluoromethyl and trifluoromethoxy and Y is 1-3 substituents selected from H, methyl and halogen or a pharmaceutically acceptable salt thereof for use in a treatment in humans to suppress the level of one or more hormone selected from luteinizing hormone, follicle-stimulating hormone, estradiol and testosterone. The present invention further relates to such a glycine transporter-1 inhibitor as part of a contraceptive regimen or as a treatment for hypersexuality.
1 - 11 . (canceled)
12 . A glycine transporter-1 inhibitor having the formula I
wherein
X is 1-3 substituents selected from H, halogen, methyl, methoxy, trifluoromethyl and trifluoromethoxy and
Y is 1-3 substituents selected from H, methyl and halogen
or a pharmaceutically acceptable salt thereof.
13 . The glycine transporter-1 inhibitor according to claim 1 which is N-methyl-N-[[(1R,2S)-1,2,3,4-tetrahydro-6-methoxy-1-phenyl-2-naphthalenyl]methyl glycine or a pharmaceutically acceptable salt thereof.
14 . A pharmaceutical composition comprising the compound according to claim 12 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
15 . A pharmaceutical composition comprising the compound according to claim 13 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
16 . A method of treatment to suppress one or more hormones selected from the group consisting of luteinizing hormone, follicle-stimulating hormone, estradiol and testosterone in a subject in need thereof, the method comprising administering to the subject an effective amount of a glycine transporter-1 inhibitor of formula I
wherein
X is 1-3 substituents selected from H, halogen, methyl, methoxy, trifluoromethyl and trifluoromethoxy and
Y is 1-3 substituents selected from H, methyl and halogen
or a pharmaceutically acceptable salt thereof.
17 . The method according to claim 16 , wherein the hormone is luteinizing hormone.
18 . The method according to claim 16 , wherein the hormone is follicle-stimulating hormone.
19 . The method according to claim 16 , wherein the hormone is estradiol.
20 . The method according to claim 16 , wherein the hormone is testosterone.
21 . The method according to claim 16 , wherein the subject is a female human.
22 . The method according to claim 16 , wherein the treatment is part of a contraceptive regimen.
23 . The method according to claim 16 , wherein the treatment is for hypersexuality.
24 . The method according to claim 16 , wherein the compound of formula I is N-methyl-N-[[(1R,2S)-1,2,3,4-tetrahydro-6-methoxy-1-phenyl-2-naphthalenyl]methyl glycine or a pharmaceutically acceptable salt thereof.