IP Library Granted Patent US 8,741,911
Granted Patent B2
US 8,741,911 · App. 13/785,575 · Granted Jun 3, 2014

Raf inhibitor compounds

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Quick Facts
Patent No.
US 8,741,911
App. No.
13/785,575
Granted
Jun 3, 2014
Kind
B2
Abstract

The present invention provides a pyrido[2,3-d]pyrimidine compound, or a pharmaceutically acceptable salt thereof, that inhibits Raf and, therefore, may be useful in treating cancer.

Claims (22)

1. A compound which is 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-phenyl)urea, or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 which is 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea.

3. The compound according to claim 2 wherein the compound is in a crystalline form characterized by a X-ray powder diffraction pattern having characteristic peaks, in 2θ±0.2, occurring at 16.0 and one or more of 6.9, 7.0, 18.2, and 23.2.

4. A pharmaceutical composition comprising a compound which is 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-phenyl) urea, or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically acceptable carrier.

5. A pharmaceutical composition comprising a compound which is 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-phenyl)urea, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient.

6. The pharmaceutical composition according to claim 5 comprising the compound which is 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-phenyl)urea.

7. The pharmaceutical composition according to claim 6 wherein the compound is in a crystalline form characterized by a X-ray powder diffraction pattern having characteristic peaks, in 2θ±0.2, occurring at 16.0 and one or more of 6.9, 7.0, 18.2, and 23.2.

8. A pharmaceutical composition comprising a compound which is 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea, or a pharmaceutically acceptable salt thereof, and polyvinyl pyrrolidone vinyl acetate (PVP-VA).

9. The pharmaceutical composition according to claim 8 comprising the compound which is 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-phenyl)urea.

10. The pharmaceutical composition according to claim 9 wherein the compound is in a crystalline form characterized by a X-ray powder diffraction pattern having characteristic peaks, in 2θ±0.2, occurring at 16.0 and one or more of 6.9, 7.0, 18.2, and 23.2.

11. The pharmaceutical composition according to claim 8 wherein the PVP-VA is Kollidon® VA 64.

12. The pharmaceutical composition according to claim 9 wherein the PVP-VA is Kollidon® VA 64.

13. The pharmaceutical composition according to claim 10 wherein the PVP-VA is Kollidon® VA 64.

14. A method of treating cancer, comprising administering to a patient in need thereof, an effective amount of a compound which is 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-phenyl)urea, or a pharmaceutically acceptable salt thereof, wherein the cancer is selected from the group consisting of thyroid cancer, ovarian cancer, melanoma, acute myelogenous leukemia (AML), and colorectal cancer.

15. The method according to claim 14 comprising the compound which is 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)-phenyl)urea.

16. The method according to claim 15 wherein the compound is in a crystalline form characterized by a X-ray powder diffraction pattern having characteristic peaks, in 2θ±0.2, occurring at 16.0 and one or more of 6.9, 7.0, 18.2, and 23.2.

17. The method according to claim 14 , wherein the cancer is melanoma.

18. The method according to claim 15 , wherein the cancer is melanoma.

19. The method according to claim 16 , wherein the cancer is melanoma.

20. The method according to claim 14 , wherein the cancer is colorectal cancer.

21. The method according to claim 15 , wherein the cancer is colorectal cancer.

22. The method according to claim 16 , wherein the cancer is colorectal cancer.

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded Dec 24, 2015
From: BRIGHTSTAR ASSOCIATES, LLC
To: DECIPHERA PHARMACEUTICALS, LLC
Reel/Frame 037359/0831 →
SECURITY INTEREST Recorded Aug 10, 2015
From: DECIPHERA PHARMACEUTICALS, LLC
To: BRIGHTSTAR ASSOCIATES LLC
Reel/Frame 036288/0037 →
SECURITY INTEREST Recorded Aug 10, 2015
From: DECIPHERA PHARMACEUTICALS, LLC
To: BRIGHTSTAR ASSOCIATES LLC
Reel/Frame 036315/0091 →
SECURITY INTEREST Recorded Aug 10, 2015
From: DECIPHERA PHARMACEUTICALS, LLC
To: BRIGHTSTAR ASSOCIATES LLC
Reel/Frame 036315/0188 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 6, 2013
From: ALLGEIER, MATTHEW CARL; PATEL, PHENIL J.; WOLFANGEL, CRAIG D.; FLYNN, DANIEL L.; KAUFMAN, MICHAEL D.
To: ELI LILLY AND COMPANY; DECIPHERA PHARMACEUTICALS, LLC
Reel/Frame 029939/0324 →