IP Library › Granted Patent US 12,459,895
Granted Patent B2
US 12,459,895 · App. 18/507,616 · Granted Nov 4, 2025

MEK inhibitors and uses thereof

Inventors: Alfredo C. Castro (Somerville, MA); Michael J. Burke (Melrose, MA); Thomas A. Wynn (Lexington, MA); Sabine K. Ruppel (Cambridge, MA); Sergio L. Santillana Soto (Lexington, MA); Eric Haines (Andover, MA); Lan Xu (Wellesley, MA); Oksana Zavidij (Westminster, MA)
Assignee: Ikena Oncology, Inc.
C07D213/64A61P35/00
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,459,895
App. No.
18/507,616
Granted
Nov 4, 2025
Kind
B2
Abstract

The present disclosure provides MEK inhibitors, compositions thereof, and methods of using the same.

Claims (30)

1 . A method of treating cancer in a subject, comprising administering to the subject a therapeutically effective amount of a compound selected from:

or a pharmaceutically acceptable salt thereof.

2 . The method of claim 1 , wherein the cancer is a K-Ras mutant cancer, a mutant B-Raf cancer, an N-Ras mutant cancer, a C-Raf mutant cancer, or an NF1 and/or NF2 mutant cancer, or any combination thereof.

3 . The method according to claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

4 . The method according to claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

5 . The method according to claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

6 . The method according to claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

7 . The method according to claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

8 . The method according to claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

9 . The method according to claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

10 . The method according to claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

11 . The method according to claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

12 . The method of claim 2 , wherein the K-Ras mutant cancer is a cancer having a mutant or variant K-Ras G12, K-Ras G13, K-Ras Q61, or K-Ras A146, or any combination thereof.

13 . The method of claim 2 , wherein the mutant B-Raf cancer is a cancer having a mutant or variant B-Raf V600, B-Raf K601, B-Raf P367, B-Raf G464, B-Raf L485, B-Raf E586, B-Raf T588, B-Raf T599, B-Raf L597, B-Raf G469, B-Raf G496, B-Raf D287, B-Raf V459, B-Raf G466, B-Raf S467, B-Raf N581, B-Raf D594, B-Raf F595, or B-Raf G596, or any combination thereof.

14 . The method of claim 2 , wherein the N-Ras mutant cancer is a cancer having a mutant or variant N-Ras G12, or N-Ras Q61, or any combination thereof.

15 . The method of claim 2 , wherein the C-Raf mutant cancer is a cancer having a mutant or variant C-Raf S427, or C-Raf 1448, or any combination thereof.

16 . The method of claim 2 , wherein the K-Ras mutant cancer is K-Ras mutant non-small cell lung cancer (NSCLC), K-Ras mutant pancreatic cancer, K-Ras mutant colorectal cancer, K-Ras mutant uterine carcinoma, K-Ras mutant endometrial carcinoma, K-Ras mutant bladder cancer, K-Ras mutant head and neck cancer, K-Ras mutant thyroid cancer, or K-Ras mutant low-grade serous ovarian cancer.

17 . The method of claim 2 , wherein the N-Ras mutant cancer is N-Ras mutant melanoma, N-Ras mutant multiple myeloma, N-Ras mutant acute myeloid leukemia (AML), or N-Ras mutant Bladder cancer.

18 . The method of claim 2 , wherein the B-Raf mutant cancer is B-Raf mutant non-small cell lung cancer (NSCLC).

19 . The method of claim 2 , wherein the C-Raf mutant cancer is C-Raf mutant bladder cancer.

20 . The method of claim 2 , wherein the NF1 and/or NF2 mutant cancer is NF1 mutant glioma, NF1 mutant non-small cell lung cancer (NSCLC), or NF2 mutant neurofibroma.

Assignments (2)
CHANGE OF NAME Recorded Dec 23, 2025
From: IKENA ONCOLOGY, INC.
To: IMAGENEBIO, INC.
Reel/Frame 073522/0031 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 3, 2024
From: CASTRO, ALFREDO C.; BURKE, MICHAEL J.; WYNN, THOMAS A.; RUPPEL, SABINE K.; SANTILLANA SOTO, SERGIO L.; HAINES, ERIC; XU, LAN; ZAVIDIJ, OKSANA
To: IKENA ONCOLOGY, INC.
Reel/Frame 066006/0471 →
Continuity (6)
Division 18323700 · May 25, 2023
Provisional Application 63488807 · Mar 7, 2023
Provisional Application 63479131 · Jan 9, 2023
Provisional Application 63375875 · Sep 16, 2022
Provisional Application 63345698 · May 25, 2022
Related Publication 20240190822A1 · Jun 13, 2024
References Cited (110)
US 8889638B2 · Cohen et al. · 2014 [cited by applicant]
US 20080263785A1 · David et al. · 2008 [cited by applicant]
US 20120238599A1 · Lee et al. · 2012 [cited by applicant]
CN 107200716A · 2017 [cited by applicant]
CN 113979995A · 2022 [cited by applicant]
EP 1243581A1 · 2002 [cited by applicant]
EP 1304101A1 · 2003 [cited by applicant]
EP 1982982A1 · 2008 [cited by applicant]
EP 3061747A1 · 2016 [cited by applicant]
EP 3275866A1 · 2018 [cited by applicant]
EP 3643308A1 · 2020 [cited by applicant]
HU 0101304A2 · 2002 [cited by applicant]
JP S60214358A · 1985 [cited by applicant]
JP 2001140075A · 2001 [cited by applicant]
JP 2003005355A · 2003 [cited by applicant]
JP 2003063139A · 2003 [cited by applicant]
JP 2004339159A · 2004 [cited by applicant]
JP 4359237B2 · 2009 [cited by applicant]
JP 2019064403A · 2019 [cited by applicant]
JP 2019064404A · 2019 [cited by applicant]
JP 2019065135A · 2019 [cited by applicant]
JP 2019065136A · 2019 [cited by applicant]
JP 2019065137A · 2019 [cited by applicant]
JP 2019065138A · 2019 [cited by applicant]
JP 2021181432A · 2021 [cited by applicant]
WO WO199844925A1 · 1998 [cited by applicant]
WO WO2001025208A1 · 2001 [cited by applicant]
WO WO2001096308A1 · 2001 [cited by applicant]
WO WO2002024650A2 · 2002 [cited by applicant]
WO WO2002053543A1 · 2002 [cited by applicant]
WO WO2003031449A2 · 2003 [cited by applicant]
WO WO2003043992A1 · 2003 [cited by applicant]
WO WO2003047577A2 · 2003 [cited by applicant]
WO WO2003070277A1 · 2003 [cited by applicant]
WO WO2003099858A1 · 2003 [cited by applicant]
WO WO2005051300A2 · 2005 [cited by applicant]
WO WO2005051301A2 · 2005 [cited by applicant]
WO WO2005051302A2 · 2005 [cited by applicant]
WO WO2005051906A2 · 2005 [cited by applicant]
WO WO2005054198A2 · 2005 [cited by applicant]
WO WO2005085207A2 · 2005 [cited by applicant]
WO WO2005118571A1 · 2005 [cited by applicant]
WO WO2005121142A1 · 2005 [cited by applicant]
WO WO2006002983A1 · 2006 [cited by applicant]
WO WO2006039721A2 · 2006 [cited by applicant]
WO WO2006107859A2 · 2006 [cited by applicant]
WO WO2006107860A2 · 2006 [cited by applicant]
WO WO2006109876A1 · 2006 [cited by applicant]
WO WO2007024021A1 · 2007 [cited by applicant]
WO WO2007044084A2 · 2007 [cited by applicant]
WO WO2007109585A2 · 2007 [cited by applicant]
WO WO2007132179A2 · 2007 [cited by applicant]
WO WO2008005457A2 · 2008 [cited by applicant]
WO WO2008012555A2 · 2008 [cited by applicant]
WO WO2008103277A2 · 2008 [cited by applicant]
WO WO2008128056A1 · 2008 [cited by applicant]
WO WO2008154221A2 · 2008 [cited by applicant]
WO WO2009001097A2 · 2008 [cited by applicant]
WO WO2009011410A1 · 2009 [cited by applicant]
WO WO2009011411A1 · 2009 [cited by applicant]
WO WO2009011412A2 · 2009 [cited by applicant]
WO WO2009046840A1 · 2009 [cited by applicant]
WO WO2009054543A1 · 2009 [cited by applicant]
WO WO2009054544A1 · 2009 [cited by applicant]
WO WO2009082038A2 · 2009 [cited by applicant]
WO WO2009082039A1 · 2009 [cited by applicant]
WO WO2009093264A2 · 2009 [cited by applicant]
WO WO2010072696A2 · 2010 [cited by applicant]
WO WO2011140817A1 · 2011 [cited by applicant]
WO WO2012163490A1 · 2012 [cited by applicant]
WO WO2013016668A2 · 2013 [cited by applicant]
WO WO2013070659A1 · 2013 [cited by applicant]
WO 2013136249A1 · 2013 [cited by applicant]
WO WO2014150427A2 · 2014 [cited by applicant]
WO WO2014155301A1 · 2014 [cited by applicant]
WO WO2014169843A1 · 2014 [cited by applicant]
WO WO2014177982A1 · 2014 [cited by applicant]
WO WO2014207100A1 · 2014 [cited by applicant]
WO WO2015058589A1 · 2015 [cited by applicant]
WO WO2015196072A2 · 2015 [cited by applicant]
WO WO2016009306A1 · 2016 [cited by applicant]
WO WO2016035008A1 · 2016 [cited by applicant]
WO WO2016155473A1 · 2016 [cited by applicant]
WO WO2017117687A1 · 2017 [cited by applicant]
WO WO2018013789A1 · 2018 [cited by applicant]
WO WO2018151830A1 · 2018 [cited by applicant]
WO WO2019018119A1 · 2019 [cited by applicant]
WO WO2019066069A1 · 2019 [cited by applicant]
WO WO2019066070A1 · 2019 [cited by applicant]
WO WO2020125747A1 · 2020 [cited by applicant]
WO WO2020156162A1 · 2020 [cited by applicant]
WO WO2021018112A1 · 2021 [cited by applicant]
WO WO2021047573A1 · 2021 [cited by applicant]
WO WO2021085636A1 · 2021 [cited by applicant]
WO WO2021142144A1 · 2021 [cited by applicant]
WO WO2021142345A1 · 2021 [cited by applicant]
WO WO2021234003A1 · 2021 [cited by applicant]
WO WO2022221866A1 · 2022 [cited by applicant]
WO 2023173053A1 · 2023 [cited by applicant]
WO 2023173057A1 · 2023 [cited by applicant]
WO 2023230205A1 · 2023 [cited by applicant]
Abe et al., “Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate),” ACS Med. Chem. Lett. 2011;2(4):320-324. [cited by applicant]
Ishii et al., “Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity,” Cancer Res. 2013;1(73):4050-4060. [cited by applicant]
Khan et al., “Structural basis for the action of the drug trametinib at KSR-bound MEK,” Nature. 2020;588:509-514. [cited by applicant]
PCT International Search Report and Written Opinion from PCT/US2023/023482, dated Jul. 31, 2023. [cited by applicant]
PCT International Search Report and Written Opinion from PCT/US2022/071732, dated Jul. 27, 2022. [cited by applicant]
PCT International Search Report and Written Opinion from PCT/US2023/064086, dated May 11, 2023. [cited by applicant]
PCT International Search Report and Written Opinion from PCT/US2023/064091, dated May 10, 2023. [cited by applicant]
Price, “Putative allosteric MEK1 and MEK2 inhibitors,” Expert Opin. Ther. Patents. 2008;18(6): 603-627. [cited by applicant]
Sun et al., “Discovery of 3-benzyl-1,3-benzoxazine-2,4-dione analogues as allosteric mitogen-activated kinase kinase (MEK) inhibitors and anti-enterovirus 71 (EV71) agents,” Bioorg Med Chem. 2016;24(16):3472-82. [cited by applicant]