IP Library › Granted Patent US 12,582,660
Granted Patent B2
US 12,582,660 · App. 17/053,057 · Granted Mar 24, 2026

Inhibitors of the RAS oncoprotein, methods of making and methods of use thereof

Inventors: Geoffrey J. Clark (Pewee Valley, KY); John O. Trent (Louisville, KY); Joseph A. Burlison (Louisville, KY)
Assignee: University of Louisville Research Foundation, Inc.
A61K31/55A61K31/357A61K31/40C07K16/2818
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Quick Facts
Patent No.
US 12,582,660
App. No.
17/053,057
Granted
Mar 24, 2026
Kind
B2
Abstract

A compound for use in treating a disease associated with activating mutations in RAS, or for use in treating a disease treatable by a reduction in RAS activity, is selected from a compound of Formula (I), salts and esters thereof. The compounds are particularly useful in treating cancer.

Claims (20)

1 . A compound selected from the group consisting of

2 . The compound of claim 1 selected from the group consisting of

3 . The compound of claim 1 , selected from the group consisting of

4 . The compound of claim 1 , selected from the group consisting of

5 . A composition comprising the compound of claim 1 .

6 . A pharmaceutical composition comprising the compound of claim 1 .

7 . A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.

8 . A method of treating a disease associated with activating mutations in RAS, or treating a disease treatable by a reduction in RAS activity, comprising administering to a patient a compound selected from the group consisting of

9 . The method of claim 8 , wherein the patient is in need of treatment.

10 . The method of claim 8 , wherein the patient is human.

11 . The method of claim 8 , wherein in the disease is a tumor or cancer.

12 . The method of claim 8 , wherein in the disease is a tumor or cancer and the tumor or cancer is pancreatic ductal adenocarcinoma, colorectal adenocarcinoma, multiple myeloma, lung adenocarcinoma, skin cutaneous melanoma, uterine corpus endometrioidcarcinoma, uterine carcinosarcoma, thyroid carcinoma, acute myeloid leukemia, bladder urothelial carcinoma, gastric adenocarcinoma, cervical adenocarcinoma, head and neck squamous cell carcinoma, melanoma, lymphoma, plasmocytoma, sarcoma, glioma, thymoma, leukemia, breast cancer, prostate cancer, colon cancer, liver cancer, esophageal cancer, brain cancer, lung cancer, pancreatic cancer, ovary cancer, endometrial cancer, bladder cancer, kidney cancer, cervical cancer, hepatoma, ovary cancer, cervix cancer, skin cancer, colorectal cancer, thyroid cancer, seminoma, melanoma, myeloid cancers, lymphoid disorders, MPNST, medulloblastoma, AML, or metastatic cancers.

13 . The method of claim 8 , wherein in the disease is a tumor or cancer and the tumor or cancer is pancreatic ductal adenocarcinoma, colorectal adenocarcinoma, multiple myeloma, lung adenocarcinoma, skin cutaneous melanoma, uterine corpus endometrioidcarcinoma, uterine carcinosarcoma, thyroid carcinoma, acute myeloid leukemia, bladder urothelial carcinoma, gastric adenocarcinoma, cervical adenocarcinoma, head and neck squamous cell carcinoma, lung cancer, MPNST, medulloblastoma, AML, or pancreatic cancer.

14 . The method of claim 8 , wherein in the disease is a tumor or cancer and the tumor or cancer is pancreatic ductal adenocarcinoma, colorectal adenocarcinoma, multiple myeloma, lung adenocarcinoma, skin cutaneous melanoma, uterine corpus endometrioidcarcinoma, lung cancer, MPNST, medulloblastoma, AML, or pancreatic cancer.

15 . The method of claim 8 , wherein in the disease is a tumor or cancer and the tumor or cancer is ovarian cancer, melanoma, kidney cancer, MPNST, medulloblastoma, AML, lung cancer, or pancreatic cancer.

16 . The method of claim 8 , further comprising administering at least one member selected from the group consisting of pembrolizumab, nivolumab, AS1411, and AS1411 conjugated to gold nanoparticles.

17 . The method of claim 8 , wherein the administering is intravenous, intradermal, subcutaneous, oral, inhalation, transdermal, transmucosal, or rectal administration.

18 . The method of claim 8 , wherein the administering is oral administration.

19 . The method of claim 8 , wherein the compound is the compound from claim 1 .

20 . The method of claim 8 , wherein the compound is the compound from claim 3 .

Assignments (4)
CONFIRMATORY LICENSE Recorded Apr 16, 2026
From: UNIVERSITY OF LOUISVILLE
To: NATIONAL INSTITUTES OF HEALTH
Reel/Frame 075408/0765 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 20, 2026
From: CLARK, GEOFFREY J.; TRENT, JOHN O.; BURLISON, JOSEPH A.
To: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
Reel/Frame 073518/0069 →
CONFIRMATORY LICENSE Recorded Oct 26, 2023
From: UNIVERSITY OF LOUISVILLE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 065365/0328 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 1, 2022
From: CLARK, GEOFFREY J.; TRENT, JOHN O.; BURLISON, JOSEPH A.
To: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
Reel/Frame 060074/0143 →
Continuity (2)
Provisional Application 62669926 · May 10, 2018
Related Publication 20210137939A1 · May 13, 2021
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