IP Library Granted Patent US 9,149,492
Granted Patent B2
US 9,149,492 · App. 14/023,952 · Granted Oct 6, 2015

Method for selectively inhibiting ACAT1 in the treatment of alzheimer's disease

Inventors: Ta-Yuan Chang (Etna, NH); Catherine C. Y. Chang (Etna, NH); Yohei Shibuya (West Lebanon, NH); Elena Bryleva (Lebanon, NH); Stephanie Murphy (West Lebanon, NH); Maximillian A. Rogers (White River Junction, VT)
Assignee: Trustees of Dartmouth College
A61K31/713A61K9/00A61K9/5184A61K31/00A61K31/167A61K31/255A61K31/395A61K31/415A61K31/44A61K31/496A61K31/55A61K31/70A61K31/7105C12N15/1137C12Y203/01009C12N2310/14C12N2310/141
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,149,492
App. No.
14/023,952
Granted
Oct 6, 2015
Kind
B2
Abstract

The present invention features methods for stimulating clearance of amyloid beta in microglia, decreasing cognitive decline associated with amyloid pathology, and treating Alzheimer's disease by selectively inhibiting the expression or activity of Acyl-CoA:Cholesterol Acyltransferase 1, but not Acyl-CoA:Cholesterol Acyltransferase 2.

Claims (18)

1. A method for stimulating clearance of amyloid beta in microglia comprising administering to a subject in need thereof an exosome-encapsulated Acyl-CoA: Cholesterol Acyltransferase 1-selective inhibitor thereby stimulating clearance of oligomeric amyloid beta in microglia in the subject.

2. The method of claim 1 , wherein the inhibitor has an IC 50 value for Acyl-CoA:Cholesterol Acyltransferase 1 which is at least twice the corresponding IC 50 value for Acyl-CoA:Cholesterol Acyltransferase 2.

3. The method of claim 1 , wherein the inhibitor inhibits the expression or activity of Acyl-CoA: Cholesterol Acyltransferase 1.

4. The method of claim 1 , wherein the inhibitor has an IC 50 value in the range of 1 nM to 100 μM.

5. The method of claim 1 , wherein the exosome-encapsulated Acyl-CoA: Cholesterol Acyltransferase 1-selective inhibitor is administered intranasally.

6. The method of claim 1 , wherein the exosome is modified with a targeting moiety.

7. A method for decreasing cognitive decline associated with amyloid pathology comprising administering to a subject in need thereof an exosome-encapsulated Acyl-CoA: Cholesterol Acyltransferase 1-selective inhibitor thereby decreasing cognitive decline associated with amyloid pathology in the subject.

8. The method of claim 7 , wherein the inhibitor has an IC 50 value for Acyl-CoA:Cholesterol Acyltransferase 1 which is at least twice the corresponding IC 50 value for Acyl-CoA:Cholesterol Acyltransferase 2.

9. The method of claim 7 , wherein the inhibitor inhibits the expression or activity of Acyl-CoA: Cholesterol Acyltransferase 1.

10. The method of claim 7 , wherein the inhibitor has an IC 50 value in the range of 1 nM to 100 μM.

11. The method of claim 7 , wherein the exosome-encapsulated Acyl-CoA: Cholesterol Acyltransferase 1-selective inhibitor is administered intranasally.

12. The method of claim 7 , wherein the exosome is modified with a targeting moiety.

13. A method for treating Alzheimer's Disease comprising administering to a subject in need thereof an exosome-encapsulated Acyl-CoA: Cholesterol Acyltransferase 1-selective inhibitor, which stimulates clearance of oligomeric amyloid beta in microglia, thereby treating the subject's Alzheimer's Disease.

14. The method of claim 13 , wherein the inhibitor has an IC 50 value for Acyl-CoA:Cholesterol Acyltransferase 1 which is at least twice the corresponding IC 50 value for Acyl-CoA:Cholesterol Acyltransferase 2.

15. The method of claim 13 , wherein the inhibitor inhibits the expression or activity of Acyl-CoA: Cholesterol Acyltransferase 1.

16. The method of claim 13 , wherein the inhibitor has an IC 50 value in the range of 1 nM to 100 μM.

17. The method of claim 13 , wherein the exosome-encapsulated Acyl-CoA: Cholesterol Acyltransferase 1-selective inhibitor is administered intranasally.

18. The method of claim 13 , wherein the exosome is modified with a targeting moiety.

Assignments (2)
CONFIRMATORY LICENSE Recorded Jan 14, 2019
From: DARTMOUTH COLLEGE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 048069/0386 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 13, 2013
From: CHANG, TA-YUAN; CHANG, CATHERINE C.Y.; SHIBUYA, YOHEI; BRYLEVA, ELENA; MURPHY, STEPHANIE; ROGERS, MAXIMILLIAN A.
To: TRUSTEES OF DARTMOUTH COLLEGE
Reel/Frame 031592/0542 →
Continuity (5)
Continuation In Part 13605206 · Sep 6, 2012
Continuation In Part 13072915 · Mar 28, 2011
Continuation In Part PCTUS2009056601 · Sep 11, 2009
Provisional Application 61103658 · Oct 8, 2008
Related Publication 20140044757A1 · Feb 13, 2014