IP Library Granted Patent US 10,085,969
Granted Patent B1
US 10,085,969 · App. 15/431,568 · Granted Oct 2, 2018

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 South Florida; University of Rochester
A61K31/40A61K31/167A61K31/381C07D207/09C07D333/46
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Quick Facts
Patent No.
US 10,085,969
App. No.
15/431,568
Granted
Oct 2, 2018
Kind
B1
Abstract

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

Claims (20)

1. A method comprising:

contacting sortilin or an analogue thereof with an amount of a compound having a structure according to Formula 2A

2. The method of claim 1 , wherein the step of contacting occurs in vitro.

3. The method of claim 1 , further comprising the step of administering the compound having a structure according to Formula 2A to a subject, wherein the step of administering occurs prior to the step of contacting.

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

5. The method of claim 4 , wherein the disease is hypercholesteremia or Alzheimer's disease.

6. The method of claim 4 , 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.

7. The method of claim 4 , wherein the ligand of sortilin or analogue thereof is an apolipoprotein.

8. The method of claim 4 , wherein the ligand of sortilin or analogue thereof is PCSK9.

9. The method of claim 8 , wherein the compound is a competitive inhibitor of PCSK9 for sortilin.

10. The method of claim 6 , wherein the compound is an allosteric enhancer of the ligand of sortilin or analogue thereof.

11. The method of claim 1 , wherein the subject suffers a disease that involves sortilin in its pathology.

12. The method of claim 1 , wherein the compound is capable of specifically binding sortilin.

13. The method of claim 1 , wherein the compound is a competitive inhibitor of a sortilin ligand or an analogue thereof.

14. The method of claim 1 , wherein the compound is an allosteric enhancer of a sortilin ligand or an analogue thereof.

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

administering to the subject an effective amount of a compound according to Formula 2A

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.

16. The method of claim 13 , wherein the subject suffers from hypercholesteremia or Alzheimer's disease.

17. The method of claim 13 , wherein the subject suffers from hepatic steatosis.

Assignments (4)
LICENSE Recorded Jan 21, 2026
From: UNIVERSITY OF SOUTH FLORIDA
To: NATIONAL INSTITUTES OF HEALTH
Reel/Frame 074462/0951 →
CONFIRMATORY LICENSE Recorded May 22, 2020
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 052742/0690 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2017
From: SPARKS, ROBERT PLEASANTS; GUIDA, WAYNE CHARLES
To: UNIVERSITY OF SOUTH FLORIDA
Reel/Frame 042530/0582 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2017
From: DEHOFF-SPARKS, JANET LINDSAY
To: UNIVERSITY OF ROCHESTER
Reel/Frame 042530/0591 →
Continuity (1)
Provisional Application 62294412 · Feb 12, 2016