IP Library Granted Patent US 12,735,707
Granted Patent B2
US 12,735,707 · App. 18/351,320 · Granted Sep 15, 2026

RUNX1 inhibition for treatment of proliferative vitreoretinopathy and conditions associated with epithelial to mesenchymal transition

Inventors: Leo A. Kim (Boston, MA); Joseph F. Arboleda-Velasquez (Newton, MA); Dhanesh Amarnani (Allston, MA); Dean Eliott (Carlsbad, CA)
Assignee: Massachusetts Eye and Ear Infirmary
C12N15/113A61K9/0048A61K31/4025A61K31/5513A61K31/7105A61K45/06A61P27/02G01N33/6893C12N2310/14G01N2333/4706G01N2800/164
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Quick Facts
Patent No.
US 12,735,707
App. No.
18/351,320
Granted
Sep 15, 2026
Kind
B2
Abstract

The present subject matter provides compositions. formulations and methods for preventing or reducing proliferation or migration of retinal cells or epithelial to mesenchymal transition in ocular cells or cells from other tissues.

Claims (25)

1 . A method for treating or reducing the severity of proliferative vitreoretinopathy (PVR) in a human subject comprising: diagnosing a PVR in a subject,

wherein said diagnosing a PVR comprises the steps of:

(a) providing an ocular test sample from said subject,

(b) assaying the level of RUNX1 protein or mRNA in the test sample; and

(c) diagnosing the subject as having aberrant PVR if the level of RUNX1 protein or mRNA is elevated in the test sample compared to a normal control; and

administering to the subject a small molecule RUNX1 inhibitor that comprises the structure of Formula I:

or a pharmaceutically acceptable salt or ester thereof, wherein

each R 1 is individually selected from halogen, alkyl, aryl, heteroaryl, or alkoxy,

and R 2 is selected from aryl or heteroaryl, and

a is 0 to 4;

Formula III:

or a pharmaceutically acceptable salt or ester thereof, wherein

each R 1 is individually selected from halogen, alkyl, aryl, heteroaryl, or alkoxy,

R 2 is selected from aryl or heteroaryl;

R 3 is alkyl or aryl, and

a is 0 to 4; or

Formula V:

or a pharmaceutically acceptable salt or ester thereof, wherein

R 1 is H 3 , NH 2 , or NHC (O) CH 3 , and

X is CH 2 or C(O).

2 . The method of claim 1 , wherein the test sample from the subject is an ocular sample obtained during ocular surgery.

3 . The method of claim 1 , wherein the level of RUNX1 protein is measured by ELISA, Western blot analysis, immunohistochemistry, or immunofluorescence.

4 . The method of claim 1 , wherein the level of RUNX1 mRNA is measured by Q-RT-PCR.

5 . The method of claim 1 , wherein the small molecule is Ro5-3335, Ro24-7429, or lenalidomide.

6 . The method of claim 1 , wherein the RUNX1 inhibitor is administered during or after intraocular surgery.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 5, 2025
From: THE SCHEPENS EYE RESEARCH INSTITUTE, INC.
To: MASSACHUSETTS EYE AND EAR INFIRMARY
Reel/Frame 071027/0028 →
CONFIRMATORY LICENSE Recorded Nov 25, 2024
From: UNIVERSITY OF COLORADO
To: UNITED STATES GOVERNMENT
Reel/Frame 069393/0223 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 29, 2023
From: KIM, LEO A.; ARBOLEDA-VELASQUEZ, JOSEPH F.; AMARNANI, DHANESH
To: THE SCHEPENS EYE RESEARCH INSTITUTE, INC.
Reel/Frame 064746/0269 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 29, 2023
From: ELIOTT, DEAN
To: MASSACHUSETTS EYE AND EAR INFIRMARY
Reel/Frame 064732/0370 →
Continuity (3)
Continuation 16763880 · Nov 14, 2018
Provisional Application 62586067 · Nov 14, 2017
Related Publication 20240175022A1 · May 30, 2024
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