IP Library › Granted Patent US 10,519,146
Granted Patent B2
US 10,519,146 · App. 15/984,855 · Granted Dec 31, 2019

KRAS G12C inhibitors and methods of using the same

Inventors: Brian Alan Lanman (Thousand Oaks, CA); Jian Chen (Thousand Oaks, CA); Anthony B. Reed (Thousand Oaks, CA); Victor J. Cee (Thousand Oaks, CA); Longbin Liu (Thousand Oaks, CA); David John Kopecky (Thousand Oaks, CA); Patricia Lopez (Thousand Oaks, CA); Ryan Paul Wurz (Thousand Oaks, CA); Thomas T. Nguyen (Thousand Oaks, CA); Shon Booker (Thousand Oaks, CA); Nobuko Nishimura (Thousand Oaks, CA); Youngsook Shin (Thousand Oaks, CA); Nuria A. Tamayo (Thousand Oaks, CA); John Gordon Allen (Thousand Oaks, CA); Jennifer Rebecca Allen (Thousand Oaks, CA)
Assignee: Amgen Inc.
C07D417/04A61K31/416A61K31/454A61K31/496A61K31/502A61K31/5025A61K31/517A61K31/519A61K31/55A61K31/7068A61K38/07A61P35/00C07D237/34C07D239/80C07D275/04C07D401/04C07D401/14C07D403/04C07D417/12C07D471/04C07D475/00C07D487/04C07D487/08C07D487/10C07D513/04
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Quick Facts
Patent No.
US 10,519,146
App. No.
15/984,855
Granted
Dec 31, 2019
Kind
B2
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.

Claims (49)

1. A compound having a structure selected from:

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 7, 2018
From: LANMAN, BRIAN ALAN; CHEN, JIAN; REED, ANTHONY B.; CEE, VICTOR J.; LIU, LONGBIN; KOPECKY, DAVID JOHN; LOPEZ, PATRICIA; WURZ, RYAN PAUL; NGUYEN, THOMAS T.; BOOKER, SHON; NISHIMURA, NOBUKO; SHIN, YOUNGSOOK; TAMAYO, NURIA A.; ALLEN, JOHN GORDON; ALLEN, JENNIFER REBECCA
To: AMGEN INC.
Reel/Frame 046820/0192 →
Continuity (2)
Provisional Application 62509629 · May 22, 2017
Related Publication 20180334454A1 · Nov 22, 2018
Cited By (31)
US 12,195,460 US 12,246,020 US 12,252,486 US 12,280,056 US 12,281,112 US 12,312,350 US 12,312,351 US 12,331,048 US 12,351,578 US 12,391,689 US 12,391,691 US 12,398,133 US 12,398,136 US 12,410,167 US 12,415,806 US 12,421,234 US 12,440,491 US 12,441,728 US 12,441,729 US 12,459,896 US 12,466,825 US 12,473,281 US 12,503,467 US 12,570,672 US 12,582,657 US 12,583,854 US 12,692,266 US 12,721,851 US 12,723,047 US 12,729,207 US 12,735,419