Preparation of and formulation comprising a MEK inhibitor

US9598376B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9598376-B2
Application numberUS-201615053441-A
CountryUS
Kind codeB2
Filing dateFeb 25, 2016
Priority dateOct 19, 2012
Publication dateMar 21, 2017
Grant dateMar 21, 2017

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  1. Title

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  2. Abstract

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  3. Assignees and inventors

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  4. Key dates

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  5. First independent claim

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  6. CPC / IPC classifications

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  7. Citations and related patents

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Abstract

Official abstract text for this publication.

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.

First claim

Opening claim text (preview).

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.

Assignees

Inventors

Classifications

  • 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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What does patent US9598376B2 cover?
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 co…
Who is the assignee on this patent?
Novartis Ag, Array Biopharma Inc
What technology area does this patent fall under?
Primary CPC classification A61K31/4184. Mapped technology areas include Human Necessities.
When was this patent published?
Publication date Tue Mar 21 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 4 related publications on this page (citations in our corpus or others sharing the same primary CPC).