IP Library Granted Patent US 8,778,893
Granted Patent B2
US 8,778,893 · App. 13/500,365 · Granted Jul 15, 2014

(R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol metabolites

Inventors: Jiachang Gong (Belle Mead, NJ); Lisa J. Christopher (East Windsor, NJ); Vinod Kumar Arora (Cheshire, CT)
Assignee: Bristol-Myers Squibb Company
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Quick Facts
Patent No.
US 8,778,893
App. No.
13/500,365
Granted
Jul 15, 2014
Kind
B2
Abstract

The present invention is directed to metabolites of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol, the compound of formula (I), pharmaceutical compositions thereof, and to methods of using the metabolites and the pharmaceutical compositions in the treatment of cancer.

Claims (22)

1. A substantially pure compound which is a metabolite of the compound of formula (I)

or a pharmaceutically acceptable salt form thereof, which metabolite is

1)

or a pharmaceutically acceptable salt form thereof, or which metabolite is

2)

or a pharmaceutically acceptable salt form thereof, or which metabolite is

3)

or a pharmaceutically acceptable salt form thereof.

2. A pharmaceutical composition, comprising a pharmaceutically acceptable vehicle or diluent and one or more compounds of claim 1 .

3. A method of treating cancer, comprising the step of administering to a subject in need thereof an effective amount of the compound of claim 1 , wherein the cancer is selected from breast cancer, colorectal cancer, hepatocellular carcinoma, non-small cell lung cancer and prostate cancer.

4. The compound according to claim 1 which is

or a pharmaceutically acceptable salt form thereof.

5. The compound according to claim 1 which is

or a pharmaceutically acceptable salt form thereof.

6. The compound according to claim 1 which is

or a pharmaceutically acceptable salt form thereof.

7. A pharmaceutical composition, comprising a pharmaceutically acceptable vehicle or diluent and the compound of claim 4 .

8. A method of treating cancer, comprising the step of administering to a subject in need thereof an effective amount of the compound of claim 4 , wherein the cancer is selected from breast cancer, colorectal cancer, hepatocellular carcinoma, non-small cell lung cancer and prostate cancer.

9. A pharmaceutical composition, comprising a pharmaceutically acceptable vehicle or diluent and the compound of claim 5 .

10. A method of treating cancer, comprising the step of administering to a subject in need thereof an effective amount of the compound of claim 5 , wherein the cancer is selected from breast cancer, colorectal cancer, hepatocellular carcinoma, non-small cell lung cancer and prostate cancer.

11. A pharmaceutical composition, comprising a pharmaceutically acceptable vehicle or diluent and the compound of claim 6 .

12. A method of treating cancer, comprising the step of administering to a subject in need thereof an effective amount of the compound of claim 6 , wherein the cancer is selected from breast cancer, colorectal cancer, hepatocellular carcinoma, non-small cell lung cancer and prostate cancer.

Continuity (2)
Provisional Application 61248581 · Oct 5, 2009
Related Publication 20120196814A1 · Aug 2, 2012