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Last Updated: May 16, 2024

Claims for Patent: 10,519,146


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Summary for Patent: 10,519,146
Title:KRAS G12C inhibitors and methods of using the same
Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
Inventor(s): Lanman; Brian Alan (Thousand Oaks, CA), Chen; Jian (Thousand Oaks, CA), Reed; Anthony B. (Thousand Oaks, CA), Cee; Victor J. (Thousand Oaks, CA), Liu; Longbin (Thousand Oaks, CA), Kopecky; David John (Thousand Oaks, CA), Lopez; Patricia (Thousand Oaks, CA), Wurz; Ryan Paul (Thousand Oaks, CA), Nguyen; Thomas T. (Thousand Oaks, CA), Booker; Shon (Thousand Oaks, CA), Nishimura; Nobuko (Thousand Oaks, CA), Shin; Youngsook (Thousand Oaks, CA), Tamayo; Nuria A. (Thousand Oaks, CA), Allen; John Gordon (Thousand Oaks, CA), Allen; Jennifer Rebecca (Thousand Oaks, CA)
Assignee: Amgen Inc. (Thousand Oaks, CA)
Application Number:15/984,855
Patent Claims: 1. A compound having a structure selected from: ##STR00668## ##STR00669## ##STR00670## ##STR00671## or a stereoisomer thereof, an atropisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, or a pharmaceutically acceptable salt of the atropisomer thereof.

2. The compound of claim 1 having the structure ##STR00672## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

3. The compound of claim 1 having the structure ##STR00673## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

4. A compound having the structure ##STR00674## or a stereoisomer thereof, an atropisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, or a pharmaceutically acceptable salt of the atropisomer thereof.

5. The compound of claim 1 having the structure ##STR00675## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

6. The compound of claim 1 having the structure ##STR00676## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

7. The compound of claim 1 having the structure ##STR00677## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

8. The compound of claim 1 having the structure ##STR00678## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

9. The compound of claim 1 having the structure ##STR00679## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

10. The compound of claim 1 having the structure ##STR00680## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

11. The compound of claim 1 having the structure ##STR00681## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

12. The compound of claim 1 having the structure ##STR00682## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

13. The compound of claim 1 having the structure ##STR00683## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

14. The compound of claim 1 having the structure ##STR00684## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

15. The compound of claim 1 having the structure ##STR00685## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

16. The compound of claim 1 having the structure ##STR00686## or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof.

17. The pharmaceutically acceptable salt of the compound of claim 1.

18. A pharmaceutical formulation comprising the compound of claim 1, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

19. A pharmaceutical formulation comprising the compound of claim 2, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

20. A pharmaceutical formulation comprising the compound of claim 3, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

21. A pharmaceutical formulation comprising the compound of claim 4, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

22. A pharmaceutical formulation comprising the compound of claim 5, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

23. A pharmaceutical formulation comprising the compound of claim 6, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

24. A pharmaceutical formulation comprising the compound of claim 7, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

25. A pharmaceutical formulation comprising the compound of claim 8, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

26. A pharmaceutical formulation comprising the compound of claim 9, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

27. A pharmaceutical formulation comprising the compound of claim 10, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

28. A pharmaceutical formulation comprising the compound of claim 11, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

29. A pharmaceutical formulation comprising the compound of claim 12, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

30. A pharmaceutical formulation comprising the compound of claim 13, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

31. A pharmaceutical formulation comprising the compound of claim 19, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

32. A pharmaceutical formulation comprising the compound of claim 15, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

33. A pharmaceutical formulation comprising the compound of claim 16, or the stereoisomer thereof, the atropisomer thereof, the pharmaceutically acceptable salt thereof, the pharmaceutically acceptable salt of the stereoisomer thereof, or the pharmaceutically acceptable salt of the atropisomer thereof and a pharmaceutically acceptable excipient.

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