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. A formulation comprising a spray-dried amorphous co-solution of a compound of formula 5-1
and an excipient or other carrier.
2. The formulation of claim 1 , wherein the excipient or other carrier is mannitol, polyvinyl pyrrolidone and/or hydroxypropylmethylcellulose.
3. A method for treating a condition selected from prostate cancer, breast cancer, endometriosis, uterine leiomyoma (fibroids), ovarian cancer, prostatic hyperplasia, assisted reproductive therapy, and precocious puberty in a subject in need thereof comprising administering to the subject a pharmaceutically effective amount of the formulation of claim 1 .
4. The method of claim 3 , wherein the condition is endometriosis.
5. The method of claim 3 , wherein the condition is uterine leiomyoma (fibroids).
6. A formulation comprising an amorphous co-solution of a compound of formula 5-1
and an excipient or other carrier.
7. The formulation of claim 6 , wherein the excipient or other carrier is a polymer.
8. The formulation of claim 6 , wherein the excipient or other carrier is selected from mannitol, polyvinyl pyrrolidone and hydroxypropylmethylcellulose.
9. A method for treating a condition selected from prostate cancer, breast cancer, endometriosis, uterine leiomyoma (fibroids), ovarian cancer, prostatic hyperplasia, assisted reproductive therapy, and precocious puberty in a subject in need thereof comprising administering to the subject a pharmaceutically effective amount of the formulation of claim 6 .
10. The method of claim 9 , wherein the condition is endometriosis.
11. The method of claim 9 , wherein the condition is uterine leiomyoma (fibroids).