IP Library › Granted Patent US 12,403,121
Granted Patent B2
US 12,403,121 · App. 17/284,112 · Granted Sep 2, 2025

Anticancer rocaglamide derivatives

Inventors: Long-Sheng Chang (Hilliard, OH); A. Douglas Kinghorn (Columbus, OH)
Assignee: The Research Institute at Nationwide Children's Hospital
A61K31/343A61K9/0019A61K9/0053A61P35/00
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Quick Facts
Patent No.
US 12,403,121
App. No.
17/284,112
Granted
Sep 2, 2025
Kind
B2
Abstract

A method of treating nervous system cancer or soft-tissue sarcoma in a subject is described. The method includes administering a therapeutically effective amount of a compound according to formula I to a subject in need thereof: wherein R 1 is selected from the group consisting of —OH, —OAc, —OCHO, ═O, and ═NOH; R 2 is selected from the group consisting of —CON(CH 3 ) 2 , —CONHCH 3 , —CONH 2 , —COOCH 3 , —COOH, and —H, R 3 is selected from the group consisting of —H, —OH, and —OCH 3 , and R 4 is selected from the group consisting of —OH, —OCH 3 , —OCH 2 CH 3 .

Claims (15)

1. A method of treating cancer in a subject in need thereof, consisting of administering a therapeutically effective amount of a compound according to formula I to the subject:

wherein R 1 is selected from the group consisting of —OH, —OAc, —OCHO, ═O, and ═NOH; R 2 is selected from the group consisting of —CON(CH 3 ) 2 , —CONHCH 3 , —CONH 2 , —COOCH 3 , —COOH, and —H, R 3 is selected from the group consisting of —H, —OH, and —OCH 3 , and R 4 is selected from the group consisting of —OH, —OCH 3 , —OCH 2 CH 3 , and optionally a pharmaceutically acceptable carrier,

wherein the cancer is selected from malignant peripheral nerve sheath tumors, Ewing sarcoma, osteosarcoma, and rhabdomyosarcoma.

2. The method of claim 1 , wherein the subject is human.

3. The method of claim 2 , wherein the subject is a child.

4. The method of claim 1 , wherein the compound is administered together with a pharmaceutically acceptable carrier.

5. The method of claim 2 , wherein the cancer is a malignant peripheral nerve sheath tumor.

6. The method of claim 1 , wherein R 4 is —OH.

7. The method of claim 1 , wherein R 3 is —H.

8. The method of claim 1 , wherein R 1 is —OH.

9. The method of claim 1 , wherein R 2 is —CON(CH 3 ) 2 , —CONHCH 3 , or —CONH 2 .

10. The method of claim 1 , wherein the compound is rocaglamide.

11. The method of claim 1 , wherein the compound is didesmethylrocaglamide.

12. The method of claim 1 , wherein the compound is not sensitive to MDR1 inhibition.

13. The method of claim 1 , wherein the compound provided an oral bioavailability of at least about 50%.

Assignments (1)
CONFIRMATORY LICENSE Recorded Dec 4, 2023
From: CHILDREN'S HOSPITAL COLUMBUS
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 065762/0625 →
Continuity (2)
Provisional Application 62743230 · Oct 9, 2018
Related Publication 20210346337A1 · Nov 11, 2021
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