IP Library Granted Patent US 10,174,054
Granted Patent B2
US 10,174,054 · App. 16/004,723 · Granted Jan 8, 2019

Compounds and methods for the treatment of Alzheimer's disease and/or cerebral amyloid angiopathy

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Quick Facts
Patent No.
US 10,174,054
App. No.
16/004,723
Granted
Jan 8, 2019
Kind
B2
Abstract

Described herein are novel compounds and methods for the treatment and/or prevention of cerebral amyloidoses such as Alzheimer's disease (AD) and/or cerebral amyloid angiopathy (CAA).

Claims (31)

1. A compound having a structure represented by formula II or IIA:

wherein: R 1 , R 3 , R 4 are independently chosen from H, C 1 -C 8 alkyl, aryl, (CH 2 ) n aryl, (CH 2 ) n heteroaryl;

n=0-8;

X=CO, SO, SO 2 , —CONH—, SO 2 NH—, SONH—;

Y=O, S, NH; and

A 1 , A 2 , B 1 , B 2 , C 1 , C 2 are independently chosen from H, OR 4 , F,

or a pharmaceutically acceptable salt, solvate, or prodrug thereof.

2. The compound of claim 1 , wherein R 4 is H.

3. The compound of claim 1 , wherein R 4 is benzyl.

4. The compound of claim 1 , wherein the compound has the following structure:

or a pharmaceutically acceptable salt, solvate, or prodrug thereof.

5. A pharmaceutical composition comprising:

a. the compound of claim 1 ; and

b. at least one pharmaceutically acceptable carrier.

6. A method for treating Alzheimer's disease and/or cerebral amyloid angiopathy in a patient at risk for developing or diagnosed with the same, the method comprising administering to the patient an effective amount of the compound of claim 1 .

7. The method of claim 6 , wherein the administration of an effective amount of the compound increases processing of one or more gangliosides selected from GM2 and GA2.

8. A method for enhancing the activity of β-hexosaminidase, the method comprising administering an effective amount of the compound of claim 1 .

9. A kit comprising:

a. the compound of claim 1 ; and

b. instructing for using the same to treat Alzheimer's disease and/or cerebral amyloid angiopathy.

10. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt, solvate, or prodrug thereof.

11. A pharmaceutical composition comprising:

a. the compound of claim 10 ; and

b. at least one pharmaceutically acceptable carrier.

12. A method for treating Alzheimer's disease and/or cerebral amyloid angiopathy in a patient at risk for developing or diagnosed with the same, the method comprising administering to the patient an effective amount of the compound of claim 10 .

13. The method of claim 12 , wherein the administration of an effective amount of the compound increases processing of one or more gangliosides selected from GM2 and GA2.

14. A method for enhancing the activity of β-hexosaminidase, the method comprising administering an effective amount of the compound of claim 10 .

15. A kit comprising:

a. the compound of claim 10 ; and

b. instructing for using the same to treat Alzheimer's disease and/or cerebral amyloid angiopathy.

Assignments (3)
SECURITY INTEREST Recorded Apr 27, 2026
From: BIOMARIN PHARMACEUTICAL INC.; AMICUS THERAPEUTICS, INC.
To: CITIBANK, N.A., AS COLLATERAL AGENT
Reel/Frame 075493/0968 →
RELEASE OF SECURITY INTEREST Recorded Apr 27, 2026
From: WILMINGTON TRUST, NATIONAL ASSOCIATION
To: AMICUS THERAPEUTICS, INC.
Reel/Frame 075494/0030 →
SECURITY INTEREST Recorded Oct 6, 2023
From: AMICUS THERAPEUTICS, INC.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 065177/0196 →