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Last Updated: April 24, 2024

Claims for Patent: 8,703,781


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Summary for Patent: 8,703,781
Title:Pharmaceutical combination of MEK inhibitor and B-RAF inhibitors
Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-tr- ioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2- -fluorophen-}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.
Inventor(s): Dumble; Melissa (Collegeville, PA), Kumar; Rakesh (Collegeville, PA), Laquerre; Sylvie (Collegeville, PA), Lebowitz; Peter (Collegeville, PA)
Assignee: GlaxoSmithKline LLC (Philadelphia, PA)
Application Number:13/499,779
Patent Claims: 1. A combination comprising: (i) a compound of formula (I) ##STR00026## or a pharmaceutically acceptable salt or solvate thereof; and (ii) a compound of formula (II) ##STR00027## or a pharmaceutically acceptable salt thereof.

2. A combination according to claim 1 wherein compound (I) is in the form of the dimethylsulfoxide solvate and the compound (II) is in the form of the methanesulfonate salt.

3. A combination kit comprising a combination according to claim 1 together with a pharmaceutically acceptable carrier or carriers.

4. A combination according to claim 1 for use in therapy.

5. A combination according to claim 1 for use in treating cancer.

6. A pharmaceutical composition comprising a combination according to claim 1 together with a pharmaceutically acceptable diluent or carrier.

7. A method of treating melanoma in a human in need thereof which comprises the administration of a therapeutically effective amount of (i) a compound of formula (I) ##STR00028## or a pharmaceutically acceptable salt or solvate thereof; and (ii) a compound of formula (II) ##STR00029## or a pharmaceutically acceptable salt thereof.

8. The method of claim 7, wherein compound (I) is in the form of the dimethylsulfoxide solvate.

9. The method of claim 7, wherein the melanoma is metastatic melanoma.

10. The method of claim 7, wherein compound (II) is in the form of the methanesulfonate salt.

11. The method of claim 7, wherein the melanoma is BRAF V600E mutant melanoma.

12. A method of treating metastatic melanoma having a BRAT V600E mutation in a human in need thereof which comprises the administration of a therapeutically effective amount of (i) a compound of formula (I) ##STR00030## or a pharmaceutically acceptable salt car solvate thereof; and (ii) a compound of formula (II) ##STR00031## or a pharmaceutically acceptable salt thereof.

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