Processes for the preparation of uracil derivatives
US-10494347-B2 · Dec 3, 2019 · US
US11459305B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11459305-B2 |
| Application number | US-202016739263-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jan 10, 2020 |
| Priority date | Nov 7, 2007 |
| Publication date | Oct 4, 2022 |
| Grant date | Oct 4, 2022 |
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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.
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What is claimed is: 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).
resulting in pure drug agglomerate optionally containing up to 5% of excipient · CPC title
with organic macromolecular compounds · CPC title
Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives · CPC title
with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil · CPC title
as doubly bound oxygen atoms or as unsubstituted hydroxy radicals · CPC title
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