Methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid
The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease.
1. A compound of Formula VIII:
wherein said compound is selected from the group consisting of:
or a pharmaceutically acceptable salt of any of the foregoing.
2. A pharmaceutical composition comprising a compound of claim 1 together with a pharmaceutically acceptable carrier.
3. The pharmaceutical composition of claim 2 which is suitable for oral administration.
4. The pharmaceutical composition of claim 2 , which is in the form of a hard shell gelatin capsule, soft shell gelatin capsule, cachet, pill, tablet, lozenge, powder, granule, pellet, dragee, which is optionally enteric coated, a solution, an aqueous liquid suspension, a non-aqueous liquid suspension, an oil-in-water liquid emulsion, a water-in-oil liquid emulsion, an elixir, a syrup, or a pastille.
5. A process for converting a compound of claim 1 to 3-amino-1-propanesulfonic acid (3APS) comprising contacting said compound with plasma, blood, and/or brain cells whereby said compound is metabolized to 3APS.
6. A method for treating Alzheimer's disease, mild cognitive impairment, Down's syndrome, Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch-Type, cerebral amyloid angiopathy, a degenerative dementia, a dementia of mixed vascular and degenerative origin, dementia associated with Parkinson's disease, dementia associated with progressive supranuclear palsy, dementia associated with cortical basal degeneration, or diffuse Lewy body type of Alzheimer's disease, comprising administering a therapeutically effective amount of a compound of claim 1 to a human subject in need thereof.
7. The method of claim 6 , which is for treating Alzheimer's disease, mild cognitive impairment, cerebral amyloid angiopathy, or degenerative dementia.
8. The method of claim 7 , which is for treating Alzheimer's disease.
9. The method of claim 6 wherein the compound is administered intratracheally, intranasally, ontologically, rectally, vaginally, or orally.