PROCESSES FOR THE PREPARATION OF URACIL DERIVATIVES
The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
1 .- 11 . (canceled)
12 . Amorphous 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid sodium salt (compound 5-1) having an impurity profile comprising one or more of the following substances:
heptane,
methyl isobutyl ketone,
isopropyl acetate, and
methyl ethyl ketone.
13 . A pharmaceutical composition comprising amorphous 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid sodium salt (compound 5-1) having an impurity profile of claim 12 , and a pharmaceutically acceptable carrier and/or diluent.
14 . 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid sodium salt (compound 5-1) having an impurity profile comprising one or more of the following substances:
heptane,
methyl isobutyl ketone,
isopropyl acetate, and
methyl ethyl ketone.
15 . A pharmaceutical composition comprising 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid sodium salt (compound 5-1) having an impurity profile of claim 14 and a pharmaceutically acceptable carrier and/or diluent.
16 . A method for treating a condition selected from endometriosis and uterine fibroids in a subject in need thereof, comprising administering to the subject a pharmaceutical composition of claim 13 .
17 . A method for treating a condition selected from endometriosis and uterine fibroids in a subject in need thereof, comprising administering to the subject a pharmaceutical composition of claim 15 .