IP Library Granted Patent US 8,835,500
Granted Patent B2
US 8,835,500 · App. 12/362,971 · Granted Sep 16, 2014

Pharmaceutical formulations of amyloid inhibiting compounds

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Quick Facts
Patent No.
US 8,835,500
App. No.
12/362,971
Granted
Sep 16, 2014
Kind
B2
Abstract

Therapeutic formulations and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Therapeutic formulations and methods for preventing or treating amyloidosis and/or amyloid-related disease are also described.

Claims (19)

1. An oral formulation comprising an effective amount of 3-amino-1-propanesulfonic acid to treat amyloidosis, inhibit amyloid deposition and/or treat an amyloid deposition-related disease, a pharmaceutically acceptable vehicle and an enteric coating, wherein the formulation results in lesser gastrointestinal intolerance in comparison to an immediate release dosage form comprising 3-amino-1-propanesulfonic acid.

2. An oral formulation comprising an effective amount of 3-amino-1-propanesulfonic acid, a pharmaceutically acceptable vehicle and an enteric coating,

wherein the formulation results in lesser gastrointestinal intolerance in comparison to an immediate release dosage form comprising 3-amino-1-propanesulfonic acid.

3. A formulation of claim 2 wherein the amount of 3-amino-1-propanesulfonic acid is effective for stabilizing cognitive function or decreasing the rate of decline in cognitive function.

4. A formulation of claim 2 wherein the amount of 3-amino-1-propanesulfonic acid is effective for inhibiting neurodegeneration or cellular toxicity induced by amyloid-β.

5. An oral formulation comprising 3-amino-1-propanesulfonic acid, a pharmaceutical acceptable carrier and an enteric coating wherein the formulation results in lesser gastrointestinal intolerance in comparison to an immediate release dosage form comprising 3-amino-1-propane sulfonic acid.

6. The formulation of claim 5 wherein 20% or less dissolution of 3-amino-1-propanesulfonic acid occurs in the acidic environment of the stomach but dissolution occurs in the more neutral or alkaline environments of the GI tract.

7. The formulation of claim 5 wherein less than or equal to 10% dissolution of the active ingredient occurs within 2 hours.

8. A method for stabilizing cognitive function or decreasing the rate of decline in cognitive function in a subject in need thereof comprising administering a formulation of claim 3 .

9. A method for inhibiting neurodegeneration or cellular toxicity induced by amyloid in a subject in need thereof comprising administering a formulation of claim 4 .

10. The method of claim 9 wherein said amyloid is amyloid-β.

11. A method for treating amyloidosis in a subject in need thereof comprising administering a formulation of claim 4 .

12. A method for inhibiting amyloid deposition in a subject in need thereof comprising administering a formulation of claim 4 .

13. A method for treating an amyloid-related diseases or conditions in a subject in need thereof comprising administering a formulation of claim 4 .

14. The method of claim 13 wherein said amyloid-related disease or condition is an amyloid-β-related disease or condition.

15. The method of claim 8 wherein said subject is an elderly individual.

16. The method of claim 14 wherein said amyloid-related disease or condition is selected from Alzheimer's disease, cerebral amyloid angiopathy, Down's syndrome, and mild cognitive impairment.

17. The method of claim 14 wherein said amyloid-related disease or condition is Alzheimer's disease or mild cognitive impairment.

18. A method for treating an amyloid-related disease in a human with brain amyloidosis comprising administering to the subject a therapeutic amount of a formulation of claim 3 , such that cognitive function is improved or stabilized or further deterioration in cognitive function is slowed.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 5, 2017
From: BHI LIMITED PARTNERSHIP
To: THALLION PHARMACEUTICALS INC.; BELLUS HEALTH INC.
Reel/Frame 044296/0094 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 5, 2017
From: THALLION PHARMACEUTICALS INC.
To: BELLUS HEALTH INC.
Reel/Frame 044296/0140 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 9, 2012
From: BELLUS HEALTH INC.
To: BHI LIMITED PARTNERSHIP
Reel/Frame 028758/0266 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 7, 2011
From: BELLUS HEALTH (INTERNATIONAL) LIMITED
To: BELLUS HEALTH INC.
Reel/Frame 026400/0132 →