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Last Updated: October 16, 2019

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Claims for Patent: 8,258,118

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Summary for Patent: 8,258,118
Title:4-pyridinone compounds and their use for cancer
Abstract: Disclosed are compounds of Formula (I): ##STR00001## and salts thereof. Also, disclosed are methods of using the compounds in the treatment of proliferative diseases, such as cancer, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a pharmaceutically acceptable salt.
Inventor(s): Borzilleri; Robert M. (New Hope, PA), Cai; Zhen-Wei (Belle Mead, NJ)
Assignee: Bristol-Myers Squibb Company (Princeton, NJ)
Application Number:13/349,173
Patent Claims:1. A method for treating cancer in a patient in need of such treatment, comprising administering to said patient a therapeutically effective amount of a compound having the following Formula (I): ##STR00043## wherein: G is H, --CHX--OP(.dbd.O)(OH).sub.2, or --CHX--OC(.dbd.O)Z; X is H or alkyl optionally substituted with one or more of OH, halogen, cyano, and/or --NR.sup.1R.sup.2; Z is alkyl, cycloalkyl, aryl, or heterocyclo optionally substituted with one or more of alkyl, OH, halogen, cyano, and/or --NR.sup.3R.sup.4; and R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently H and/or alkyl; or a pharmaceutically salt thereof.

2. The method according to claim 1 wherein said cancer is bladder cancer, breast cancer, colorectal cancer, gastric cancer, head and neck cancer, kidney cancer, liver cancer, lung cancer, ovarian cancer, pancreas/gall bladder cancer, prostate cancer, thyroid cancer, osteosarcoma, rhabdomyosarcoma, melanoma, glioblastomas/astrocytomas, MFH/fibrosarcoma, or mesothelioma.

3. The method according to claim 1 wherein said compound is: ##STR00044## or a pharmaceutically salt thereof.

4. The method according to claim 1 wherein said patient is human.

5. The method according to claim 1, further comprising administering an additional anticancer agent.

6. The method according to claim 5 wherein said additional anticancer agent is gefitinib, erlotinib, or cetuximab.

7. The method according to claim 1 wherein said cancer is dependent upon Met activation, wherein the Met activation is regulated by gene amplification, and activated Met mutation, and/or HGF stimulation.

8. The method according to claim 3 wherein said compound is: ##STR00045## or a pharmaceutically acceptable salt thereof.

9. The method according to claim 8 wherein said compound is: ##STR00046##

10. The method according to claim 8 wherein said compound or pharmaceutically acceptable salt thereof is a bis-trisamine salt.

11. The method according to claim 3 wherein said compound is: ##STR00047##

12. The method according to claim 2 wherein said cancer is bladder cancer, breast cancer, colorectal cancer, gastric cancer, head and neck cancer, kidney cancer, liver cancer, lung cancer, melanoma, ovarian cancer, pancreas/gall bladder cancer, prostate cancer, or thyroid cancer.

13. The method according to claim 12 wherein said cancer is bladder cancer, gastric cancer, head and neck cancer, or lung cancer.

14. The method according to claim 12 wherein said cancer is prostate cancer.

15. The method according to claim 12 wherein said cancer is breast cancer.

16. The method according to claim 12 wherein said cancer is kidney cancer.

17. The method according to claim 12 wherein said cancer is melanoma.

18. The method according to claim 12 wherein said cancer is colorectal cancer.

19. The method according to claim 12 wherein said cancer is gastric cancer.

20. The method according to claim 12 wherein said cancer is ovarian cancer.

Details for Patent 8,258,118

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Imclone ERBITUX cetuximab VIAL; INTRAVENOUS 125084 001 2004-06-18   Request a Trial Bristol-Myers Squibb Company (Princeton, NJ) 2028-01-23 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

International Patent Family for US Patent 8,258,118

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