Naphthoquinone derivatives useful for prevention of amyloid deposits and treatment of diseases involving amyloidogenesis
AssigneeRamot at Tel-Aviv University Ltd.
InventorsRoni SCHERZER, Ehud GAZIT, Daniel SEGAL
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Abstract
The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.
Claims17
A method for treating a disease associated with amyloidogenesis in an individual in need thereof, comprising administering to the individual an effective amount of a substituted 3-amino-1,4-naphthoquinone represented by the structure of the general formula (I):
- wherein
- each R1 independently is selected from the group consisting of H and OH;
- R2 is selected from the group consisting of H, a halogen, —NR5R6 wherein R5 and R6 are selected from the group consisting of H, a saturated or unsaturated cyclic moiety comprising from 5 to 8 atoms, an unsubstituted or substituted aryl and NR5R6 wherein R5 and R6 together form a saturated or unsaturated hetero cyclic ring comprising from 5 to 8 atoms;
- R3 comprises a heterocyclic amino acid side chain selected from the group consisting of tryptophan, histidine and proline
- and
- R4 is H;
- or NR3R4 is an amino acid residue.
A method for treating a disease associated with amyloidogenesis in an individual in need thereof, comprising administering to the individual an effective amount of a substituted 3-amino-1,4-naphthoquinone of any of the structures of formulae III-XII,
- XIV-XVI and XIX-XXV:
Dependencies are inferred from the claim text.