US 12,440,491 B2
KRAS G12C inhibitors and methods of using the same
John Gordon Allen, Newbury Park, CA (US); Jennifer Rebecca Allen, Newbury Park, CA (US); Ana Elena Minatti, Santa Monica, CA (US); Qiufen Xue, Thousand Oaks, CA (US); Ryan Paul Wurz, Newbury Park, CA (US); Christopher M. Tegley, Daly City, CA (US); Alexander J. Pickrell, Westlake Village, CA (US); Thomas T. Nguyen, Newbury Park, CA (US); Vu Van Ma, Oak Park, CA (US); Patricia Lopez, Woodland Hills, CA (US); Longbin Liu, Thousand Oaks, CA (US); David John Kopecky, Washington, DC (US); Michael J. Frohn, Thousand Oaks, CA (US); Ning Chen, Thousand Oaks, CA (US); Jian Jeffrey Chen, San Diego, CA (US); Aaron C. Siegmund, Ventura, CA (US); Albert Amegadzie, Westlake Village, CA (US); Nuria A. Tamayo, Newbury Park, CA (US); Shon Booker, Sherman Oaks, CA (US); Clifford Goodman, Calabasas, CA (US); Mary Walton, Camarillo, CA (US); Nobuko Nishimura, West Hills, CA (US); Youngsook Shin, Seoul (KR); Jonathan D. Low, Northridge, CA (US); Victor J. Cee, Thousand Oaks, CA (US); Anthony B. Reed, Newbury Park, CA (US); Hui-Ling Wang, Thousand Oaks, CA (US); and Brian Alan Lanman, Woodland Hills, CA (US)
Assigned to Amgen Inc., Thousand Oaks, CA (US)
Filed by Amgen Inc., Thousand Oaks, CA (US)
Filed on Jun. 23, 2023, as Appl. No. 18/213,464.
Application 18/213,464 is a continuation of application No. 17/363,878, filed on Jun. 30, 2021, granted, now 11,766,436.
Application 17/363,878 is a continuation of application No. 16/402,538, filed on May 3, 2019, granted, now 11,090,304, issued on Aug. 17, 2021.
Claims priority of provisional application 62/667,282, filed on May 4, 2018.
Prior Publication US 2024/0050430 A1, Feb. 15, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/517 (2006.01); A61K 31/4985 (2006.01); A61K 39/395 (2006.01); A61P 35/00 (2006.01); C07D 403/04 (2006.01); C07D 471/04 (2006.01)
CPC A61K 31/517 (2013.01) [A61K 31/4985 (2013.01); A61K 39/39558 (2013.01); A61P 35/00 (2018.01); C07D 403/04 (2013.01); C07D 471/04 (2013.01)] 4 Claims
 
1. A method of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound, wherein the compound is

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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; or

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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; or

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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; or

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or a stereoisomer thereof, an atropisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, a pharmaceutically acceptable salt of the atropisomer thereof; or

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or a stereoisomer thereof, an atropisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, a pharmaceutically acceptable salt of the atropisomer thereof; or

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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; or

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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; or

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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; or

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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, or

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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, or

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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;
wherein the cancer is mediated by a KRAS G12C mutation; and
wherein the cancer is non-small cell lung cancer, small intestine cancer, appendix cancer, colorectal cancer, endometrial cancer, pancreatic cancer, skin cancer, gastric cancer, nasal cavity cancer, bile duct cancer, or brain cancer.