IP Library Granted Patent US 8,980,884
Granted Patent B2
US 8,980,884 · App. 13/484,725 · Granted Mar 17, 2015

Methods for treating Alzheimer's disease

Inventor: Luigi Puglielli (Madison, WI)
Assignee: Wisconsin Alumni Research Foundation
A61K31/00A61K31/496A61K31/136A61K31/498A61K31/538
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Quick Facts
Patent No.
US 8,980,884
App. No.
13/484,725
Granted
Mar 17, 2015
Kind
B2
Abstract

Pharmaceutical compositions for treating Alzheimer's disease are disclosed. The pharmaceutical compositions include a compound having the general formula: and a pharmaceutically acceptable carrier. Methods for treating Alzheimer's disease, inhibiting ATase I and/or ATase 2, reducing the activity of BACE1, reducing the level of amyloid β-peptide (Aβ), and/or reducing the level of APP intracellular domain peptide (AICD) by administering such compositions are also disclosed.

Claims (14)

1. A method of treating, delaying the onset of, slowing the progression of, or alleviating at least one symptom of Alzheimer's disease comprising administering to a patient a pharmaceutical composition comprising an effective amount of an inhibitor of ATase1 and/or ATase2, wherein the inhibitor of ATase1 and/or ATase2 is a compound selected from the compounds having the following formula:

wherein:

R 1 , R 2 , R 3 , R 4 , and R 7 are each independently selected from hydrogen, halogen, —OH, —OR 9 , —SH, —SR 9 , —NH 2 , —NHR 9 , —NR 9 R 10 , and C 1 -C 10 alkyl, wherein R 9 and R 10 are independently selected from C 1 -C 5 alkyl;

R 8 is selected from hydrogen, halogen, —OH, —NH 2 , and —SH, or is absent;

R 5 and R 6 are each independently selected from hydrogen, halogen, —OH, —OR 9 , —SH, —SR 9 , —NH 2 , —NHR 9 , —NR 9 R 10 , and C 1 -C 10 alkyl, wherein R 9 and R 10 are independently selected from C 1 -C 5 alkyl; or R 5 and R 6 together are

wherein R 11 , R 12 , R 13 , and R 14 are each independently selected from hydrogen, halogen, —OH, —OR 9 , —SH, —SR 9 , —NH 2 , —NHR 9 , —NR 9 R 10 , and C 1 -C 10 alkyl, wherein R 9 and R 10 are independently selected from C 1 -C 5 alkyl;

X 1 is selected from N, NH, and O;

X 2 is selected from N and O;

X 3 is selected from —OH, ═O, —NH 2 , ═NH, —SH, and ═S; and

wherein the X 1 to carbon a (C a ) bond and the carbon b (C b ) to carbon c (C c ) bond are both double bonds, or the C a to C b bond is a double bond;

or pharmaceutically acceptable salts thereof;

whereby Alzheimer's disease in the patient is delayed in onset, or slowed in progression, or whereby at least one symptom of Alzheimer's disease is alleviated.

2. The method of claim 1 , wherein the inhibitor of ATase1 and/or ATase2 is selected from the group consisting of:

and pharmaceutically acceptable salts thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 26, 2013
From: PUGLIELLI, LUIGI
To: WISCONSIN ALUMNI RESEARCH FOUNDATION
Reel/Frame 029876/0255 →
CONFIRMATORY LICENSE Recorded Jun 11, 2012
From: WISCONSIN ALUMNI RESEARCH FOUNDATION
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 028350/0311 →
Continuity (2)
Provisional Application 61492146 · Jun 1, 2011
Related Publication 20120329789A1 · Dec 27, 2012