IP Library Granted Patent US 11,439,623
Granted Patent B2
US 11,439,623 · App. 16/500,700 · Granted Sep 13, 2022

Method of modulating ribonucleotide reductase

Inventors: Chris G. Dealwis (Cleveland, OH); Rajesh Viswanathan (Cleveland, OH); Sarah E. Huff (Cleveland, OH); William Harte (Cleveland, OH)
Assignee: CASE WESTERN RESERVE UNIVERSITY
A61K31/4245A61K31/4439A61K45/06
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Quick Facts
Patent No.
US 11,439,623
App. No.
16/500,700
Granted
Sep 13, 2022
Kind
B2
Abstract

A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a triazole or an oxadiazole ribonucleotide reductase modulator (RRmod), the amount being effective to inhibit neoplastic cell growth.

Claims (21)

1. A method of modulating ribonucleotide reductase activity in a neoplastic cell comprising administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRmod), the RRmod comprising an oxadiazole that is administered at an amount effective to inhibit neoplastic cell growth, wherein the RRmod is an oxadiazole having the following formula (IV):

or pharmaceutically acceptable salts thereof:

wherein R 21 is selected from the group consisting of:

2. The method of claim 1 , wherein the RRmod is selected from the group consisting of:

and

pharmaceutically acceptable salts thereof.

3. The method of claim 1 , the cell comprising a cancer cell.

4. The method of claim 3 , the cancer cell comprising a pancreatic, breast, lung, colon or glioblastoma cancer cell.

5. A method of treating a neoplastic disorder in a subject comprising:

administering to neoplastic cells of the subject a therapeutically effective amount of a pharmaceutical composition, the composition comprising a reductase allosteric modulator (RRmod), the RRmod including an oxadiazole that is administered at an amount effective to inhibit neoplastic cell growth, wherein the RRmod is an oxadiazole having the following formula (IV):

or pharmaceutically acceptable salts thereof:

wherein R 21 is selected from the group consisting of:

6. The method of claim 5 , wherein the RRmod is selected from the group consisting of:

and

pharmaceutically acceptable salts thereof.

7. The method of claim 5 , the neoplastic disorder comprising cancer.

8. The method of claim 7 , wherein the cancer includes pancreatic, breast, lung, colon or glioblastoma cancer.

9. The method of claim 5 , further administering another therapeutic agent in conjunction with the RRmod.

10. The method of claim 9 , the other therapeutic agent comprising at least one of a chemotherapeutic agent, an antimetabolite, a DNA damaging agent, a ribonucleotide reductase inhibiting agent, an antitumorgenic agent, an antimitotic agent, an antiviral agent, an antineoplastic agent, an immunotherapeutic agent, and a radiotherapeutic agent.

11. The method of claim 1 , wherein the RRmod has a cellular cytotoxicity 1050 of 10 μm against HCT-116 and PANC-1 cancer cell lines.

12. The method of claim 5 , wherein the RRmod has a cellular cytotoxicity 1050 of 10 μm against HCT-116 and PANC-1 cancer cell lines.

Assignments (2)
CONFIRMATORY LICENSE Recorded Sep 8, 2023
From: CASE WESTERN RESERVE UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 064851/0953 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 20, 2022
From: DEALWIS, CHRIS; VISWANATHAN, RAJESH; HUFF, SARAH E.; HARTE, WILLIAM
To: CASE WESTERN RESERVE UNIVERSITY
Reel/Frame 059967/0770 →
Continuity (2)
Provisional Application 62481458 · Apr 4, 2017
Related Publication 20210113533A1 · Apr 22, 2021