IP Library Granted Patent US 12,440,491
Granted Patent B2
US 12,440,491 · App. 18/213,464 · Granted Oct 14, 2025

KRAS G12C inhibitors and methods of using the same

Inventors: John Gordon Allen (Newbury Park, CA); Jennifer Rebecca Allen (Newbury Park, CA); Ana Elena Minatti (Santa Monica, CA); Qiufen Xue (Thousand Oaks, CA); Ryan Paul Wurz (Newbury Park, CA); Christopher M. Tegley (Daly City, CA); Alexander J. Pickrell (Westlake Village, CA); Thomas T. Nguyen (Newbury Park, CA); Vu Van Ma (Oak Park, CA); Patricia Lopez (Woodland Hills, CA); Longbin Liu (Thousand Oaks, CA); David John Kopecky (Washington, DC); Michael J. Frohn (Thousand Oaks, CA); Ning Chen (Thousand Oaks, CA); Jian Jeffrey Chen (San Diego, CA); Aaron C. Siegmund (Ventura, CA); Albert Amegadzie (Westlake Village, CA); Nuria A. Tamayo (Newbury Park, CA); Shon Booker (Sherman Oaks, CA); Clifford Goodman (Calabasas, CA); Mary Walton (Camarillo, CA); Nobuko Nishimura (West Hills, CA); Youngsook Shin (Seoul, KR); Jonathan D. Low (Northridge, CA); Victor J. Cee (Thousand Oaks, CA); Anthony B. Reed (Newbury Park, CA); Hui-Ling Wang (Thousand Oaks, CA); Brian Alan Lanman (Woodland Hills, CA)
Assignee: Amgen Inc.
A61K31/517A61K31/4985A61K39/39558A61P35/00C07D403/04C07D471/04
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Quick Facts
Patent No.
US 12,440,491
App. No.
18/213,464
Granted
Oct 14, 2025
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 (17)

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

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

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

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

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

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

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

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

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

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

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

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.

2. The method of claim 1 , wherein the cancer is non-small cell lung cancer.

3. The method of claim 1 , wherein the cancer is colorectal cancer.

4. The method of claim 1 , wherein the cancer is pancreatic cancer.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 17, 2023
From: ALLEN, JOHN GORDON; ALLEN, JENNIFER REBECCA; MINATTI, ANA ELENA; XUE, QIUFEN; WURZ, RYAN PAUL; TEGLEY, CHRISTOPHER M.; NGUYEN, THOMAS T.; MA, VU VAN; LOPEZ, PATRICIA; LIU, LONGBIN; KOPECKY, DAVID JOHN; FROHN, MICHAEL J.; CHEN, NING; CHEN, JIAN JEFFREY; SIEGMUND, AARON C.; AMEGADZIE, ALBERT; TAMAYO, NURIA A.; BOOKER, SHON; GOODMAN, CLIFFORD; WALTON, MARY; NISHIMURA, NOBUKO; SHIN, YOUNGSOOK; LOW, JONATHAN D.; CEE, VICTOR J.; REED, ANTHONY B.; WANG, HUI-LING; LANMAN, BRIAN ALAN; PICKRELL, ALEXANDER J.
To: AMGEN INC.
Reel/Frame 065257/0784 →
Continuity (4)
Continuation 17363878 · Jun 30, 2021
Continuation 16402538 · May 3, 2019
Provisional Application 62667282 · May 4, 2018
Related Publication 20240050430A1 · Feb 15, 2024
References Cited (400)
US 4232027A · Turk et al. · 1980 [cited by applicant]
US 5100883A · Schiehser · 1992 [cited by applicant]
US 5118677A · Caufield · 1992 [cited by applicant]
US 5118678A · Kao et al. · 1992 [cited by applicant]
US 5120842A · Failli et al. · 1992 [cited by applicant]
US 5151413A · Caufield et al. · 1992 [cited by applicant]
US 5256790A · Nelson · 1993 [cited by applicant]
US 5258389A · Goulet et al. · 1993 [cited by applicant]
US 5521184A · Zimmerman · 1996 [cited by applicant]
US 5650415A · Tang et al. · 1997 [cited by applicant]
US 5656643A · Spada et al. · 1997 [cited by applicant]
US 5712291A · D'Amato · 1998 [cited by applicant]
US 5728813A · Lyman et al. · 1998 [cited by applicant]
US 5747498A · Schnur et al. · 1998 [cited by applicant]
US 5770599A · Gibson · 1998 [cited by applicant]
US 5789427A · Chen et al. · 1998 [cited by applicant]
US 5792783A · Tang et al. · 1998 [cited by applicant]
US 5861510A · Piscopio et al. · 1999 [cited by applicant]
US 5863949A · Robinson et al. · 1999 [cited by applicant]
US 5892112A · Levy et al. · 1999 [cited by applicant]
US 5969110A · Beckmann et al. · 1999 [cited by applicant]
US 5981245A · Fox et al. · 1999 [cited by applicant]
US 5990141A · Hirth et al. · 1999 [cited by applicant]
US 6057124A · Bartley et al. · 2000 [cited by applicant]
US 6111090A · Gorman et al. · 2000 [cited by applicant]
US 6232447B1 · Cerretti · 2001 [cited by applicant]
US 6235764B1 · Larson et al. · 2001 [cited by applicant]
US 6258812B1 · Bold et al. · 2001 [cited by applicant]
US 6413932B1 · Cerretti et al. · 2002 [cited by applicant]
US 6515004B1 · Misra et al. · 2003 [cited by applicant]
US 6596852B2 · Cerretti et al. · 2003 [cited by applicant]
US 6630500B2 · Gingrich et al. · 2003 [cited by applicant]
US 6656963B2 · Firestone et al. · 2003 [cited by applicant]
US 6713485B2 · Carter et al. · 2004 [cited by applicant]
US 6727225B2 · Wiley · 2004 [cited by applicant]
US 7025962B1 · Gorman et al. · 2006 [cited by applicant]
US 7354944B2 · Zeng et al. · 2008 [cited by applicant]
US 7361760B2 · Sircar et al. · 2008 [cited by applicant]
US 7514566B2 · Zeng et al. · 2009 [cited by applicant]
US 7618632B2 · Collins et al. · 2009 [cited by applicant]
US 7700636B2 · Monenschein et al. · 2010 [cited by applicant]
US 7812135B2 · Smith et al. · 2010 [cited by applicant]
US 7897619B2 · Zeng et al. · 2011 [cited by applicant]
US 7919504B2 · Zeng et al. · 2011 [cited by applicant]
US 7919514B2 · Monenschein et al. · 2011 [cited by applicant]
US 8388967B2 · Smith et al. · 2013 [cited by applicant]
US 8586023B2 · Shiku et al. · 2013 [cited by applicant]
US 8591886B2 · Ponath et al. · 2013 [cited by applicant]
US 10519146B2 · Lanman · 2019 [cited by examiner]
US 10532042B2 · Lanman et al. · 2020 [cited by applicant]
US 10640504B2 · Lanman · 2020 [cited by examiner]
US 10689377B2 · Blake · 2020 [cited by examiner]
US 10988485B2 · Minatti et al. · 2021 [cited by applicant]
US 11045484B2 · Wurz et al. · 2021 [cited by applicant]
US 11053226B2 · Shin et al. · 2021 [cited by applicant]
US 11090304B2 · Allen · 2021 [cited by examiner]
US 11096939B2 · Booker et al. · 2021 [cited by applicant]
US 11236091B2 · Chaves et al. · 2022 [cited by applicant]
US 11285135B2 · Lanman et al. · 2022 [cited by applicant]
US 11285156B2 · Allen et al. · 2022 [cited by applicant]
US 11299491B2 · Parsons et al. · 2022 [cited by applicant]
US 11306087B2 · Lanman · 2022 [cited by examiner]
US 11426404B2 · Henary et al. · 2022 [cited by applicant]
US 11439645B2 · Lipford et al. · 2022 [cited by applicant]
US 11766434B2 · Carswell · 2023 [cited by examiner]
US 11766436B2 · Allen · 2023 [cited by examiner]
US 11827635B2 · Chaves et al. · 2023 [cited by applicant]
US 11905281B2 · Lanman et al. · 2024 [cited by applicant]
US 11918584B2 · Lipford et al. · 2024 [cited by applicant]
US 11993597B2 · Lanman · 2024 [cited by examiner]
US 12083121B2 · Allen et al. · 2024 [cited by applicant]
US 12280056B2 · Lipford et al. · 2025 [cited by applicant]
US 20020042368A1 · Fanslow, III et al. · 2002 [cited by applicant]
US 20030105091A1 · Riedl et al. · 2003 [cited by applicant]
US 20030162712A1 · Cerretti et al. · 2003 [cited by applicant]
US 20090012085A1 · Baum et al. · 2009 [cited by applicant]
US 20090023761A1 · Chen et al. · 2009 [cited by applicant]
US 20090030002A1 · Chen et al. · 2009 [cited by applicant]
US 20090054405A1 · Booker et al. · 2009 [cited by applicant]
US 20090137581A1 · Chen et al. · 2009 [cited by applicant]
US 20090163489A1 · Booker et al. · 2009 [cited by applicant]
US 20090270445A1 · Zeng et al. · 2009 [cited by applicant]
US 20100273764A1 · Andrews et al. · 2010 [cited by applicant]
US 20100331293A1 · Chushing et al. · 2010 [cited by applicant]
US 20100331306A1 · Bui et al. · 2010 [cited by applicant]
US 20110092504A1 · Bo et al. · 2011 [cited by applicant]
US 20110097305A1 · Connors et al. · 2011 [cited by applicant]
US 20140288045A1 · Ren et al. · 2014 [cited by applicant]
US 20150239900A1 · Li et al. · 2015 [cited by applicant]
US 20160159738A1 · Ren et al. · 2016 [cited by applicant]
US 20160166571A1 · Janes et al. · 2016 [cited by applicant]
US 20160297774A1 · Li et al. · 2016 [cited by applicant]
US 20180015087A1 · Liu et al. · 2018 [cited by applicant]
US 20180072723A1 · Blake et al. · 2018 [cited by applicant]
US 20180177767A1 · Lanman et al. · 2018 [cited by applicant]
US 20180334454A1 · Lanman et al. · 2018 [cited by applicant]
US 20190077801A1 · Lanman et al. · 2019 [cited by applicant]
US 20190336514A1 · Wurz et al. · 2019 [cited by applicant]
US 20190345169A1 · Minatti et al. · 2019 [cited by applicant]
US 20190374542A1 · Allen et al. · 2019 [cited by applicant]
US 20190375749A1 · Chen et al. · 2019 [cited by applicant]
US 20200030324A1 · Booker et al. · 2020 [cited by applicant]
US 20200055845A1 · Lanman et al. · 2020 [cited by applicant]
US 20200069657A1 · Lanman et al. · 2020 [cited by applicant]
US 20200165231A1 · Shin et al. · 2020 [cited by applicant]
US 20200207766A1 · Lanman et al. · 2020 [cited by applicant]
US 20200216446A1 · Parsons et al. · 2020 [cited by applicant]
US 20200222407A1 · Lipford et al. · 2020 [cited by applicant]
US 20200360374A1 · Henary et al. · 2020 [cited by applicant]
US 20200369662A1 · Chaves et al. · 2020 [cited by applicant]
US 20210009577A1 · Lanman et al. · 2021 [cited by applicant]
US 20220002298A1 · Chen et al. · 2022 [cited by applicant]
US 20220106313A1 · Chaves et al. · 2022 [cited by applicant]
US 20220168280A1 · Lanman et al. · 2022 [cited by applicant]
US 20220175782A1 · Allen et al. · 2022 [cited by applicant]
US 20220213101A1 · Lanman et al. · 2022 [cited by applicant]
US 20220220112A1 · Parsons et al. · 2022 [cited by applicant]
US 20220235045A1 · Chaves et al. · 2022 [cited by applicant]
US 20220378787A1 · Henary et al. · 2022 [cited by applicant]
US 20220395504A1 · Allen et al. · 2022 [cited by applicant]
US 20230028414A1 · Henary et al. · 2023 [cited by applicant]
US 20230121955A1 · Lipford et al. · 2023 [cited by applicant]
US 20230248729A1 · Henary et al. · 2023 [cited by applicant]
US 20240067647A1 · Chaves et al. · 2024 [cited by applicant]
US 20240082251A1 · Henary et al. · 2024 [cited by applicant]
US 20240091230A1 · Ang et al. · 2024 [cited by applicant]
US 20240173328A1 · Lipford et al. · 2024 [cited by applicant]
US 20240174660A1 · Lanman et al. · 2024 [cited by applicant]
US 20240190862A1 · Wang et al. · 2024 [cited by applicant]
US 20240287068A1 · Lanman et al. · 2024 [cited by applicant]
US 20240408089A1 · Henary et al. · 2024 [cited by applicant]
US 20250057817A1 · Lanman et al. · 2025 [cited by applicant]
DE 19629652A1 · 1998 [cited by applicant]
EP 0090505A2 · 1983 [cited by applicant]
EP 404355A1 · 1990 [cited by applicant]
EP 511792A2 · 1992 [cited by applicant]
EP 0520722A1 · 1992 [cited by applicant]
EP 0566226A1 · 1993 [cited by applicant]
EP 0606046A1 · 1994 [cited by applicant]
EP 0682027A1 · 1995 [cited by applicant]
EP 0407122A1 · 1996 [cited by applicant]
EP 0770622A2 · 1997 [cited by applicant]
EP 0780386A1 · 1997 [cited by applicant]
EP 0787772A2 · 1997 [cited by applicant]
EP 0818442A2 · 1998 [cited by applicant]
EP 0837063A1 · 1998 [cited by applicant]
EP 0931788A2 · 1999 [cited by applicant]
EP 0970070B1 · 2000 [cited by applicant]
EP 1004578A2 · 2000 [cited by applicant]
EP 1181017B1 · 2002 [cited by applicant]
EP 1786785B9 · 2007 [cited by applicant]
EP 1866339B1 · 2007 [cited by applicant]
EP 1947183A1 · 2008 [cited by applicant]
EP 3401314A1 · 2019 [cited by applicant]
EP 3055290B1 · 2019 [cited by applicant]
JP 02233610A · 1990 [cited by applicant]
JP 2019031476A · 2019 [cited by applicant]
WO 1990005719A1 · 1990 [cited by applicant]
WO 1992005179A1 · 1992 [cited by applicant]
WO 1992020642A1 · 1992 [cited by applicant]
WO 1993011130A1 · 1993 [cited by applicant]
WO 1994002136A1 · 1994 [cited by applicant]
WO 1994002485A1 · 1994 [cited by applicant]
WO 1994009010A1 · 1994 [cited by applicant]
WO 1995009847A1 · 1995 [cited by applicant]
WO 1995014023A1 · 1995 [cited by applicant]
WO 1995016691A1 · 1995 [cited by applicant]
WO 1995019774A1 · 1995 [cited by applicant]
WO 1995019970A1 · 1995 [cited by applicant]
WO 1996027583A1 · 1996 [cited by applicant]
WO 1996030347A1 · 1996 [cited by applicant]
WO 1996031510A1 · 1996 [cited by applicant]
WO 1996033172A1 · 1996 [cited by applicant]
WO 1996033980A1 · 1996 [cited by applicant]
WO 1996041807A1 · 1996 [cited by applicant]
WO 1997002266A1 · 1997 [cited by applicant]
WO 1997013771A1 · 1997 [cited by applicant]
WO 1997019065A1 · 1997 [cited by applicant]
WO 1997027199A1 · 1997 [cited by applicant]
WO 1997030034A1 · 1997 [cited by applicant]
WO 1997030044A1 · 1997 [cited by applicant]
WO 1997032880A1 · 1997 [cited by applicant]
WO 1997032881A1 · 1997 [cited by applicant]
WO 1997034895A1 · 1997 [cited by applicant]
WO 1997038983A1 · 1997 [cited by applicant]
WO 1997038994A1 · 1997 [cited by applicant]
WO 1997049688A1 · 1997 [cited by applicant]
WO 1998002434A1 · 1998 [cited by applicant]
WO 1998002437A1 · 1998 [cited by applicant]
WO 1998002438A1 · 1998 [cited by applicant]
WO 1998002441A2 · 1998 [cited by applicant]
WO 1998003516A1 · 1998 [cited by applicant]
WO 1998007697A1 · 1998 [cited by applicant]
WO 1998007726A1 · 1998 [cited by applicant]
WO 1998014449A1 · 1998 [cited by applicant]
WO 1998014450A1 · 1998 [cited by applicant]
WO 1998014451A1 · 1998 [cited by applicant]
WO 1998017662A1 · 1998 [cited by applicant]
WO 1998030566A1 · 1998 [cited by applicant]
WO 1998033768A1 · 1998 [cited by applicant]
WO 1998033798A2 · 1998 [cited by applicant]
WO 1998034915A1 · 1998 [cited by applicant]
WO 1998034918A1 · 1998 [cited by applicant]
WO 1999007675A1 · 1999 [cited by applicant]
WO 1999007701A1 · 1999 [cited by applicant]
WO 1999020758A1 · 1999 [cited by applicant]
WO 1999029667A1 · 1999 [cited by applicant]
WO 1999035132A1 · 1999 [cited by applicant]
WO 1999035146A1 · 1999 [cited by applicant]
WO 1999040196A1 · 1999 [cited by applicant]
WO 1999045009A1 · 1999 [cited by applicant]
WO 1999052889A1 · 1999 [cited by applicant]
WO 1999052910A1 · 1999 [cited by applicant]
WO 1999061422A1 · 1999 [cited by applicant]
WO 2000002871A1 · 2000 [cited by applicant]
WO 2000012089A1 · 2000 [cited by applicant]
WO 2000059509A1 · 2000 [cited by applicant]
WO 2001003720A2 · 2001 [cited by applicant]
WO 2001014387A1 · 2001 [cited by applicant]
WO 2001032651A1 · 2001 [cited by applicant]
WO 2001037820A2 · 2001 [cited by applicant]
WO 2002055501A2 · 2002 [cited by applicant]
WO 2002059110A1 · 2002 [cited by applicant]
WO 2002066470A1 · 2002 [cited by applicant]
WO 2002068406A2 · 2002 [cited by applicant]
WO 2004005279A2 · 2004 [cited by applicant]
WO 2004007458A1 · 2004 [cited by applicant]
WO 2004007481A2 · 2004 [cited by applicant]
WO 2004009784A2 · 2004 [cited by applicant]
WO 2004063195A1 · 2004 [cited by applicant]
WO 2005005434A1 · 2005 [cited by applicant]
WO 2005007190A1 · 2005 [cited by applicant]
WO 2005011700A1 · 2005 [cited by applicant]
WO 2005016252A2 · 2005 [cited by applicant]
WO 2005021546A1 · 2005 [cited by applicant]
WO 2005055808A2 · 2005 [cited by applicant]
WO 2005115451A2 · 2005 [cited by applicant]
WO 2006044453A1 · 2006 [cited by applicant]
WO 2006083289A2 · 2006 [cited by applicant]
WO 2006121168A1 · 2006 [cited by applicant]
WO 2006122806A2 · 2006 [cited by applicant]
WO 2007133822A1 · 2007 [cited by applicant]
WO 2008070740A1 · 2008 [cited by applicant]
WO 2008118454A2 · 2008 [cited by applicant]
WO 2008118455A1 · 2008 [cited by applicant]
WO 2008118468A1 · 2008 [cited by applicant]
WO 2008153947A2 · 2008 [cited by applicant]
WO 2009036082A2 · 2009 [cited by applicant]
WO 2009055730A1 · 2009 [cited by applicant]
WO 2009085185A1 · 2009 [cited by applicant]
WO 2010003118A1 · 2010 [cited by applicant]
WO 2010083246A1 · 2010 [cited by applicant]
WO 2010096314A1 · 2010 [cited by applicant]
WO 2010108074A2 · 2010 [cited by applicant]
WO 2010126895A1 · 2010 [cited by applicant]
WO 2010132598A1 · 2010 [cited by applicant]
WO 2010151735A2 · 2010 [cited by applicant]
WO 2010151737A2 · 2010 [cited by applicant]
WO 2010151740A2 · 2010 [cited by applicant]
WO 2010151791A1 · 2010 [cited by applicant]
WO 2011028683A1 · 2011 [cited by applicant]
WO 2011031842A1 · 2011 [cited by applicant]
WO 2011051726A2 · 2011 [cited by applicant]
WO 2011090754A1 · 2011 [cited by applicant]
WO 2012142498A2 · 2012 [cited by applicant]
WO 2013039954A1 · 2013 [cited by applicant]
WO 2013155223A1 · 2013 [cited by applicant]
WO 2014023385A1 · 2014 [cited by applicant]
WO 2014143659A1 · 2014 [cited by applicant]
WO 2014152588A1 · 2014 [cited by applicant]
WO 2015001076A1 · 2015 [cited by applicant]
WO 2015054572A1 · 2015 [cited by applicant]
WO 2015075483A1 · 2015 [cited by applicant]
WO 2015109285A1 · 2015 [cited by applicant]
WO 2016035008A1 · 2016 [cited by applicant]
WO 2016044772A1 · 2016 [cited by applicant]
WO 2016049524A1 · 2016 [cited by applicant]
WO 2016049565A1 · 2016 [cited by applicant]
WO 2016049568A1 · 2016 [cited by applicant]
WO 2016164675A1 · 2016 [cited by applicant]
WO 2016168540A1 · 2016 [cited by applicant]
WO 2017015562A1 · 2017 [cited by applicant]
WO 2017058728A1 · 2017 [cited by applicant]
WO 2017058768A1 · 2017 [cited by applicant]
WO 2017058792A1 · 2017 [cited by applicant]
WO 2017058805A1 · 2017 [cited by applicant]
WO 2017058807A1 · 2017 [cited by applicant]
WO 2017058902A1 · 2017 [cited by applicant]
WO 2017058915A1 · 2017 [cited by applicant]
WO 2017087528A1 · 2017 [cited by applicant]
WO 2017100546A1 · 2017 [cited by applicant]
WO 2017172979A1 · 2017 [cited by applicant]
WO 2017201161A1 · 2017 [cited by applicant]
WO 2018064510A1 · 2018 [cited by applicant]
WO 2018068017A1 · 2018 [cited by applicant]
WO 2018119183A2 · 2018 [cited by applicant]
WO 2018119183A3 · 2018 [cited by applicant]
WO 2018140598A1 · 2018 [cited by applicant]
WO 2018217651A1 · 2018 [cited by applicant]
WO 2018218069A1 · 2018 [cited by applicant]
WO 2019051291A1 · 2019 [cited by applicant]
WO 2019213516A1 · 2019 [cited by applicant]
WO 2019213526A1 · 2019 [cited by applicant]
WO 2019217691A1 · 2019 [cited by applicant]
WO 2019232419A1 · 2019 [cited by applicant]
WO 2019241157A1 · 2019 [cited by applicant]
WO 2019243533A1 · 2019 [cited by applicant]
WO 2019243535A1 · 2019 [cited by applicant]
WO 2020050890A2 · 2020 [cited by applicant]
WO 2020102730A1 · 2020 [cited by applicant]
WO 2020106640A1 · 2020 [cited by applicant]
WO 2020156285A1 · 2020 [cited by applicant]
WO 2020232130A1 · 2020 [cited by applicant]
WO 2020236947A1 · 2020 [cited by applicant]
WO 2020236948A1 · 2020 [cited by applicant]
WO 2002006213A2 · 2022 [cited by applicant]
“A Phase 1, Study Evaluating the Safety, Tolerability, PK, and Efficacy of AMG 510 in Subjects With Solid Tumors With a S Mutation.” NCT03600883, comparison of version submitted Jul. 17, 2018 and Apr. 3, 2019 (update po… [cited by applicant]
“Acute Leukemia,” [cited by applicant]
“KRASG12C Inhibitor,” Mirati Therapeutics, retrieved on Nov. 27, 2018, from https://www.mirati.com/mrtx849/, 5 pages. [cited by applicant]
Ahmadian, et al., “Guanosine triphosphatase stimulation of oncogenic Ras mutants,” [cited by applicant]
Airoldi, et al., “Glucose-Derived Ras Pathway Inhibitors: Evidence of Ras-Ligand Binding and Ras-GEF (Cdc25) Interaction Inhibition,” [cited by applicant]
AMG-510; CS-0081316; Source: AbaChemScene (CS-0081316); Deposit Date: May 13, 2019 Available Date: May 13, 2019; SID: 384060804[CID: 137278711] (available at https://pubchem.ncbi.nlm.nih.gov/substance/384060804/). [cited by applicant]
AMG-510; HY-114277; Source: MedChemexpress Mce (HY-114277); Deposit Date: May 13, 2019 Available Date: May 13, 2019; SID: 384060569[CID: 137278711] (available at https://pubchem.ncbi.nlm.nih.gov/substance/384060569). [cited by applicant]
ATTC “Organism: [cited by applicant]
Barnett, et al., “Identification and characterization of pleckstrin-holomogy-domain-dependent and isoenzyme specific Akt inhibitors,” [cited by applicant]
Bhatia, et al., “A Review on Bioisosterism: A Rational Approach for Drug Design and Molecular Modification,” [cited by applicant]
Bull, et al., “Isoquino[2,1- [cited by applicant]
Campillo, et al., “Novel Bronchodilators: Synthesis, Transamination Reactions, and Pharmacology of a Series of Pyrazino[2,3- [cited by applicant]
Canon, et al., “The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity,” [cited by applicant]
Canon, et al., “The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity,” [cited by applicant]
Cee, et al., “Discovery of AMG 510, a first-in-humancovalent inhibitor of KRAS [cited by applicant]
Cohen, “The development and therapeutic potential of protein kinase inhibitors,” [cited by applicant]
Cowen Slide deck—Warp Drive Bio, slides 1-32, “Corporate Overview Exploiting the Molecules and Mechanisms of Nature to Create Transformative Medicines” http://www.warpdrivebio.com/news/cowen%202016.pdf (last visited Apr… [cited by applicant]
Dasmahapatra, et al., “In vitro Combination Treatment with Perifosine and UCN-01 Demonstrates Synergism Against Prostate (PC-3) and Lung (A549) Epithelial Adenocarcinoma Cell Lines,” [cited by applicant]
Database Registry [Online], Chemical Abstracts Service, Columbus, Ohio, US; Jul. 31, 2017 (Jul. 31, 2017), XP002801805, retrieved from STN Database accession No. 2105944-09-8. [cited by applicant]
Dermer, et al., “Another Anniversary for the War on Cancer,” [cited by applicant]
Douelle, et al., “Highly Diastereoselective Synthesis of vicinal Quaternary and Tertiary Stereocenters Using the Iodo-aldol Cyclization,” [cited by applicant]
Erkkilä, et al., “Mild Organocatalytic α-Methylenation of Aldehydes,” [cited by applicant]
Extended European Search Report for European Patent Application No. 19208193.2, dated Jun. 3, 2020, pp. 1-8. [cited by applicant]
Fakih, et al., “Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12C inhibitor, in advanced solid tumors,” [cited by applicant]
Fakih, et al., “Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12C inhibitor, in advanced solid tumors,” Presentation, ASCO, Chicago, IL, U… [cited by applicant]
Final Office Action for U.S. Appl. No. 15/984,855, mailed Mar. 28, 2019, 7 pages. [cited by applicant]
Final Office Action for U.S. Appl. No. 16/436,647, mailed Mar. 24, 2021, 7 pages. [cited by applicant]
Final Office Action for U.S. Appl. No. 16/661,907, mailed Mar. 27, 2020, 29 pages. [cited by applicant]
Freshney, et al., Culture of Animal Cells, [cited by applicant]
Gentile, et al., “Discovery and Structural Investigation of Novel Binders to the Ras Switch II Pocket,” NCI Initiative Symposium Poster (2015). [cited by applicant]
Gills and Dennis, “The development of phosphatidylinositol ether lipid analogues as inhibitors of the serine/threonine kinase, Akt,” [cited by applicant]
Goldberg, et al., “Role of PD-1 and its ligand, B7-H1, in early fate decisions of CD8 T cells,” [cited by applicant]
Goldstein, et al., “Biological efficacy of a chimeric antibody to the epidermal growth factor receptor in a human tumor xenograft model,” [cited by applicant]
Golub, et al., “Molecular Classification of Cancer: Class Discovery and Class Prediction by Gene Expression Monitoring,” [cited by applicant]
Govindan, et al., “Safety, Efficacy, and Pharmacokinetics of AMG 510, a Novel KRASG12C Inhibitor, in Patients with Non-Small Cell Lung Cancer,” Abstract and Presentation, North American Conference on Lung Cancer (NACLC)… [cited by applicant]
Govindan, et al., “Phase 1 Study of AMG 510, a Novel KRAS G12C Inhibitor, in Advanced Solid Tumors with KRAS p.G12C Mutation,” Abstract, ESMO Congress, Barcelona, Spain, Sep. 27-Oct. 1, 2019. [cited by applicant]
Govindan, et al., “Phase 1 Study of AMG 510, a Novel KRAS G12C Inhibitor, in Advanced Solid Tumors with KRAS p.G12C Mutation,” Poster, ESMO Congress, Barcelona, Spain, Sep. 27, 2019-Oct. 1, 2019. [cited by applicant]
Govindan, et al., “Phase 1 Study of Safety, Tolerability, Pharmacokinetics, and Efficacy of AMG 510, a Novel KRAS [cited by applicant]
Gura, “Cancer Models: Systems for Identifying New Drugs are Often Faulty,” [cited by applicant]
Halford, “Amgen unveils its Kras covalent inhibitor AMG 510,” [cited by applicant]
Hallin, et al., “The KRAS [cited by applicant]
Hansen, et al., “Abstract 686: Drugging an undruggable pocket: the biochemical mechanism of covalent KRAS [cited by applicant]
Hichri, et al., “A Convenient Synthesis of 1,3,2-Benzodiazaphophorine-2-Oxide,” [cited by applicant]
Hichri, et al., Caplus Abstract, 162:245378 (2015). [cited by applicant]
Hocker, et al., “Andrographolide derivatives inhibit guanine nucleotide exchange and abrogate oncogenic Ras function,” [cited by applicant]
Huang, et al., “Epidermal Growth Factor Receptor Blockade with C225 Modulates Proliferation, Apoptosis, and Radiosensitivity in Squamous Cell Carcinomas of the Head and Neck,” [cited by applicant]
International Search Report for PCT/US2017/067801, mailed Jul. 25, 2018, 6 pages. [cited by applicant]
International Search Report for PCT/US2018/033714, mailed Jul. 17, 2018, 3 pages. [cited by applicant]
International Search Report for PCT/US2018/050044, mailed Oct. 30, 2018, 7 pages. [cited by applicant]
International Search Report for PCT/US2019/030593, mailed Aug. 6, 2019, 4 pages. [cited by applicant]
International Search Report for PCT/US2019/030606, mailed Jul. 23, 2019, 5 pages. [cited by applicant]
International Search Report for PCT/US2019/031535, mailed Jul. 25, 2019, 7 pages. [cited by applicant]
International Search Report for PCT/US2019/034974, mailed Aug. 9, 2019, 5 pages. [cited by applicant]
International Search Report for PCT/US2019/036397, mailed Aug. 26, 2019, 5 pages. [cited by applicant]
International Search Report for PCT/US2019/036626, mailed Jun. 2, 2020, 5 pages. [cited by applicant]
International Search Report for PCT/US2019/061815, mailed Mar. 5, 2020, 6 pages. [cited by applicant]
International Search Report for PCT/US2019/062051, mailed Mar. 2, 2020, 3 pages. [cited by applicant]
International Search Report for PCT/US2019/62064, mailed Oct. 29, 2020, 9 pages. [cited by applicant]
International Search Report for PCT/US2020/032686, mailed Aug. 14, 2020, 4 pages. [cited by applicant]
International Search Report for PCT/US2020/033831, mailed Jul. 9, 2020, 6 pages. [cited by applicant]
International Search Report for PCT/US2020/033832, mailed Jul. 8, 2020, 4 pages. [cited by applicant]
Janes, et al., “Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor,” [cited by applicant]
Jarvis, “Notorious KRAS: Taking down cancer researchers' biggest foe,” [cited by applicant]
Jin, et al., “Inhibition of AKT survival pathway by a small molecule inhibitor in human endometrial cancer cells,” [cited by applicant]
Johnson et al., “Relationships between drug activity in NCI preclinical in vitro and in vivo models and early clinical trials,” [cited by applicant]
Lanman, et al., “Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRAS [cited by applicant]
Lanman, et al., “Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRAS [cited by applicant]
Lanman, et al., “Discovery of a Covalent Inhibitor of KRAS [cited by applicant]
Li, et al., “Targeting Protein-Protein Interaction with Covalent Small-Molecule Inhibitors,” [cited by applicant]
Lim, et al., “Therapeutic Targeting of Oncogenic K-Ras by a Covalent Catalytic Site Inhibitor,” [cited by applicant]
Lipford, et al., “Pre-Clinical Development of AMG 510: The First Inhibitor of KRAS [cited by applicant]
Liu, Y., “Session SY28—Transformative Small Molecule Therapies—Targeting KRAS mutant cancers with a covalent G12C—specific inhibitor,” Presentation on Apr. 4, 2017, AACR Annual Meeting Presentation, Apr. 1-5, 2017, Wash… [cited by applicant]
Lopez, et al.,“Optimization of quinazolinone-based covalent inhibitors of KRAS [cited by applicant]
Lu, et al., “KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry,” [cited by applicant]
Maurer, et al., “Small-molecule ligands bind to a distinct pocket in Rad and inhibit SOS-mediated nucleotide exchange activity,” [cited by applicant]
McGregor, et al., “Expanding the Scope of Electrophiles Capable of Targeting K-Ras Oncogenes,” [cited by applicant]
Meanwell, “Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design,” [cited by applicant]
Mirati Therapeutics, “Corporate Presentation Nov. 2017,” Slides 1-41 (2017). [cited by applicant]
Modjtahedi, et al., “The human EGF receptor as a target for cancer therapy: six new rat mAbs AGainst the receptor on the breast carcinoma MDA-MB 468,” [cited by applicant]
Morrissey et al., “Immunotherapy and Novel Combinations in Oncology: Current Landscape, Challenges, and Opportunities,” [cited by applicant]
National Cancer Institute identifier: NSC 154020, retrieved on Nov. 29, 2018, from https://cactus.nci.nih.gov/ncidb2.2/. [cited by applicant]
NCBI Reference Sequence, “GTPase KRas isoform a [ [cited by applicant]
Non-Final Office Action (Corrected) for U.S. Appl. No. 16/125,359, mailed Apr. 8, 2019, 13 pages. [cited by applicant]
Non-Final Office Action for U.S. Appl. No. 15/849,905, mailed Mar. 20, 2019, 18 pages. [cited by applicant]