Preparation of and formulation comprising a MEK inhibitor
US-9382212-B1 · Jul 5, 2016 · US
US9598376B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9598376-B2 |
| Application number | US-201615053441-A |
| Country | US |
| Kind code | B2 |
| Filing date | Feb 25, 2016 |
| Priority date | Oct 19, 2012 |
| Publication date | Mar 21, 2017 |
| Grant date | Mar 21, 2017 |
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The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro -3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound.
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What is claimed is: 1. A method of treating a cancer is selected from melanoma, pancreatic cancer, ovarian cancer, carcinoma of the fallopian tubes, peritoneal cancer, biliary cancer, colon cancer, or rectal cancer in a patient in need thereof, comprising administering to said mammal a pharmaceutical composition comprising crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide and a pharmaceutically acceptable carrier or excipient. 2. The method according to claim 1 , wherein the cancer is melanoma. 3. The method according to claim 2 , wherein said melanoma is BRAFV600 or NRAS-mutant melanoma. 4. The method according to claim 3 , wherein the pharmaceutical composition is formulated as a tablet. 5. The method according to claim 4 , wherein the pharmaceutical composition comprises approximately 15 mg crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide. 6. The method according to claim 5 , wherein the pharmaceutical composition further comprises lactose monohydrate, microcrystalline cellulose, colloidal silicon dioxide, croscarmellose sodium, and magnesium stearate. 7. The method according to claim 6 , wherein said melanoma is NRAS-mutant melanoma. 8. The method according to claim 3 , further comprising administering an additional therapeutic agent. 9. The method according to claim 8 , wherein the additional therapeutic agent is a chemotherapeutic agent or anti-tumor agent. 10. The method according to claim 9 , wherein the pharmaceutical composition comprising crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide and the additional therapeutic agent are administered separately. 11. The method according to claim 10 , wherein said melanoma is BRAFV600 mutant melanoma. 12. The method according to claim 9 , wherein the pharmaceutical composition comprising crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide and the additional therapeutic agent are administered simultaneously. 13. The method according to claim 1 , wherein the cancer is colon cancer. 14. The method according to claim 1 , wherein the cancer is ovarian cancer.
Antineoplastic agents · CPC title
Carboxylic acids; Salts or anhydrides thereof · CPC title
Organic compounds · CPC title
by cooling of the solution · CPC title
condensed with carbocyclic rings, e.g. benzimidazoles · CPC title
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