IP Library Granted Patent US 12,721,833
Granted Patent B2
US 12,721,833 · App. 17/912,477 · Granted Sep 1, 2026

Small molecule anticancer agents, combinations and uses thereof

Inventors: Brian Keith Law (Gainesville, FL); Ronald K. Castellano (Gainesville, FL); Stephan Jahn (Gainesville, FL); Elham Yaaghubi (Gainesville, FL)
Assignee: University of Florida Research Foundation, Incorporated
A61K31/385A61P35/00C07D339/08
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Quick Facts
Patent No.
US 12,721,833
App. No.
17/912,477
Granted
Sep 1, 2026
Kind
B2
Abstract

The invention relates to methods of treating cell proliferative disorders. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.

Claims (46)

1 . A compound of Formula I, or salt thereof:

wherein,

(i) R 3 is halo or haloalkoxy; and R 4 is halo or haloalkoxy; or

(ii) R 3 is H or C 1 -C 6 alkoxy; and R 4 is halo or haloalkoxy; or

(iii) R 3 is halo or haloalkoxy; and R 4 is H or C 1 -C 6 alkoxy.

2 . The compound of claim 1 , or a salt thereof:

wherein,

R 3 is halo; and R 4 is halo; or

R 3 is halo; and R 4 is haloalkoxy.

3 . The compound of claim 1 , or a salt thereof:

wherein,

R 3 is haloalkoxy; and R 4 is haloalkoxy; or

R 3 is haloalkoxy; and R 4 is halo.

4 . The compound of claim 1 , or salt thereof:

wherein,

R 3 is H; and R 4 is halo; or

R 3 is H; and R 4 is haloalkoxy.

5 . The compound of claim 1 , or salt thereof:

wherein,

R 3 is C 1 -C 6 alkoxy; and R 4 is halo; or

R 3 is C 1 -C 6 alkoxy; and R 4 is haloalkoxy.

6 . The compound of claim 1 , or salt thereof:

wherein,

R 3 is halo or haloalkoxy; and R 4 is H; or

R 3 is halo or haloalkoxy; and R 4 is C 1 -C 6 alkoxy.

7 . The compound of claim 1 , or a salt thereof, according to:

(a) Formula (II):

or salt thereof;

(b) Formula (III):

or salt thereof; or

(c) any of Formula (IV-XI):

or salt thereof.

8 . The compound or a salt thereof of claim 1 , wherein the compound is of the formula:

 or salt thereof.

9 . A pharmaceutical composition comprising a compound of claim 1 , or salt thereof, and a pharmaceutically acceptable carrier.

10 . The composition of claim 9 , further comprising an additional therapeutic agent.

11 . A method of inhibiting cell proliferation comprising administering to a subject in need thereof a therapeutically effective amount of a compound of claim 1 , or salt thereof, wherein the cell proliferation is modulated by HER2, HER3, and/or EGFR.

12 . The method of claim 11 , wherein the cell is a cancer cell.

13 . The method of claim 12 , wherein the cancer cell proliferation is modulated by HER2 mediated.

14 . The method of claim 12 , wherein the cancer cell is a breast cancer cell.

15 . The method of claim 14 , wherein the breast cancer cell is a HER2-positive breast cancer cell.

16 . The method of claim 14 , wherein the breast cancer cell proliferation is modulated by EGFR.

17 . A method of inhibiting cancer cell metastasis comprising administering to a subject in need thereof a therapeutically effective amount a compound of claim 1 , or a salt thereof, wherein the cancer cell metastasis is modulated by HER2, HER3, and/or EGFR.

18 . A method of treating cancer in a subject comprising administering to the subject a compound of claim 1 , or a salt thereof, wherein the cancer is modulated by HER2, HER3, and/or EGFR.

19 . The method of claim 18 , wherein the cancer is breast cancer, pancreatic cancer, prostate, oral, or non-small cell lung cancer (NSCLC).

20 . A kit for treating a cell proliferative disorder, the kit comprising a compound of claim 1 , or a salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 12, 2022
From: LAW, BRIAN KEITH; CASTELLANO, RONALD K.; JAHN, STEPHAN; YAAGHUBI, ELHAM
To: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INCORPORATED
Reel/Frame 062053/0327 →
Continuity (3)
Provisional Application 63067651 · Aug 19, 2020
Provisional Application 62990544 · Mar 17, 2020
Related Publication 20230122505A1 · Apr 20, 2023
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