IP Library Granted Patent US 10,478,421
Granted Patent B1
US 10,478,421 · App. 16/148,839 · Granted Nov 19, 2019

Sortilin binding compounds, formulations, and uses thereof

Inventors: Robert Pleasants Sparks (Urbana, IL); Wayne Charles Guida (St. Pete Beach, FL); Janet Lindsay DeHoff-Sparks (Pittsford, NY)
Assignees: University of Florida; University of Rochester
A61K31/40A61K31/167A61K31/381C07D207/09C07D333/46
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Quick Facts
Patent No.
US 10,478,421
App. No.
16/148,839
Granted
Nov 19, 2019
Kind
B1
Abstract

Provided herein are compounds and formulations thereof that can be capable of binding to sortilin or an analogue thereof. Also provided herein are methods of administering the compounds and formulation provided herein to a subject in need thereof.

Claims (22)

1. A method comprising:

administering an amount of a compound according to Formula 2A

or a pharmaceutical formulation thereof and an amount of compound 541

or a pharmaceutical formulation thereof to a subject.

2. The method of claim 1 , wherein the subject suffers from a disease whose pathology involves a ligand of sortilin or analogue thereof.

3. The method of claim 2 , wherein the disease is hypercholesteremia or Alzheimer's disease.

4. The method of claim 2 , wherein the ligand of sortilin or analogue thereof is PCSK9, apolipoprotein B100, phosphatidylinositides, anionic phospholipids, anionic phospholipids contained on VLDL, amyloid beta, amyloid precursor protein, neurotensin or analogues of neurotensin, lipoprotein lipase, apolipoprotein AV or apolipoprotein E.

5. The method of claim 2 , wherein the ligand of sortilin or analogue thereof is an apolipoprotein.

6. The method of claim 2 , wherein the ligand of sortilin or analogue thereof is PCSK9.

7. The method of claim 1 , wherein the compound having a structure according to Formula 2A or pharmaceutical formulation thereof and compound 541 or pharmaceutical formulation thereof are administered simultaneously.

8. The method of claim 1 , wherein the compound having a structure according to Formula 2A or pharmaceutical formulation thereof and compound 541 or pharmaceutical formulation thereof are administered sequentially.

9. A method of inhibiting binding of a sortilin ligand to sortilin in a subject, the method comprising:

administering to the subject an effective amount of a compound according to Formula 2A or a pharmaceutical formulation thereof

and an effective amount of compound 541 or a pharmaceutical formulation thereof

wherein the sortilin ligand is selected from the group consisting of: PCSK9, apolipoprotein B100, phosphatidylinositides, anionic phospholipids, anionic phospholipids contained on VLDL, amyloid beta, amyloid precursor protein, neurotensin or analogues of neurotensin, lipoprotein lipase, apolipoprotein AV and apolipoprotein E.

10. The method of claim 9 , wherein the subject suffers from hypercholesteremia or Alzheimer's disease.

11. The method of claim 9 , wherein the subject suffers from hepatic steatosis.

12. A pharmaceutical formulation comprising:

an effective amount of a compound having a structure according to Formula 2A

an effective amount of compound 541

 and

a pharmaceutically acceptable carrier.

Assignments (4)
LICENSE Recorded Jan 21, 2026
From: UNIVERSITY OF SOUTH FLORIDA
To: NATIONAL INSTITUTES OF HEALTH
Reel/Frame 074463/0299 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 26, 2019
From: SPARKS, ROBERT PLEASANTS; GUIDA, WAYNE CHARLES
To: UNIVERSITY OF SOUTH FLORIDA
Reel/Frame 048437/0742 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 26, 2019
From: DEHOFF-SPARKS, JANET LINDSAY
To: UNIVERSITY OF ROCHESTER
Reel/Frame 048437/0753 →
CONFIRMATORY LICENSE Recorded Dec 20, 2018
From: UNIVERSITY OF SOUTH FLORIDA
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 047967/0959 →
Continuity (2)
Continuation 15431568 · Feb 13, 2017
Provisional Application 62294412 · Feb 12, 2016
Cited By (2)
US 12,297,277 US 12,358,991