KRAS G12C inhibitors and methods of using the same

Patent metadata

Field	Value
Publication number	US-11905281-B2
Application number	US-202017031607-A
Country	US
Kind code	B2
Filing date	Sep 24, 2020
Priority date	May 22, 2017
Publication date	Feb 20, 2024
Grant date	Feb 20, 2024

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.

First claim

What is claimed is:

1. A compound, wherein the compound is selected from:

2. The compound of claim 1 , wherein the compound is

3. The compound of claim 1 , wherein the compound is

4. The compound of claim 1 , wherein the compound is

5. The compound of claim 1 , wherein the compound is

6. The compound of claim 1 , wherein the compound is

7. The compound of claim 1 , wherein the compound is

8. A process of making a compound, wherein the compound is

or a pharmaceutically acceptable salt thereof, and wherein the process comprises
(a) transforming 2,6-dichloro-5-fluoro-nicotinic acid into 2,6-dichloro-5-fluoronicotinamide;
(b) transforming 2,6-dichloro-5-fluoronicotinamide into the compound of claim 2 ;
(c) transforming the compound of claim 2 into the compound of claim 3 ;
(d) transforming the compound of claim 3 into the compound of claim 4 ;
(e) transforming the compound of claim 4 into the compound of claim 5 ;
transforming the compound of claim 5 into the compound of claim 6 ; or
(g) transforming the compound of claim 6 into the compound of claim 7 .

9. The process of claim 8 , wherein the process comprises transforming 2,6-dichloro-5-fluoro-nicotinic acid into 2,6-dichloro-5-fluoronicotinamide.

10. The process of claim 8 , wherein the process comprises transforming 2,6-dichloro-5-fluoronicotinamide into the compound of claim 3 .

11. The process of claim 8 , wherein the process comprises transforming the compound of claim 2 into the compound of claim 3 .

12. The process of claim 8 , wherein the process comprises transforming the compound of claim 3 into the compound of claim 4 .

13. The process of claim 8 , wherein the process comprises transforming the compound of claim 4 into the compound of claim 5 .

14. The process of claim 8 , wherein the process comprises transforming the compound of claim 5 into the compound of claim 6 .

15. The process of claim 8 , wherein the process comprises transforming the compound of claim 6 into the compound of claim 7 .

16. A compound, wherein the compound is

Assignees

• Amgen Inc

Inventors

• 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

Classifications

• C07D417/04 Primary

  directly linked by a ring-member-to-ring-member bond · CPC title

• A61K31/416 Primary

  condensed with carbocyclic ring systems, e.g. indazole · CPC title

• A61K31/454

  containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone · CPC title

• A61K31/496

  Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin · CPC title

• A61K31/502

  ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine · CPC title