METHODS AND COMPOSITIONS FOR TREATING AMYLOID-RELATED DISEASES
First Claim
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1. A compound of Formula V:
- wherein;
A is nitrogen or oxygen;
R11 is hydrogen, salt-forming cation, ester forming group, —
(CH2)x-Q, or when A is nitrogen, A and R11 taken together may be the residue of a natural or unnatural amino acid or a salt or ester thereof, wherein A and R11 taken together are not a leucine residue;
Q is hydrogen, thiazolyl, triazolyl, imidazolyl, benzothiazolyl, or benzoimidazolyl;
x is 0, 1, 2, 3, or 4;
n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
aa is a natural or unnatural amino acid residue;
m is 1, 2, or 3;
R14 is hydrogen or protecting group;
R15 is hydrogen, alkyl or aryl; and
pharmaceutically acceptable salts, esters, or prodrugs thereof;
wherein when A is oxygen, R11 is hydrogen or a salt-forming cation, n is 2, m is 1, and R14 and R15 are both hydrogen, then aa is other than phenylalanine, and wherein when A is oxygen, R11 is hydrogen or a salt-forming cation, n is 2, 3 or 4, m is 2, and R14 and R15 are both hydrogen, then aa is other than D-phenylalanine.
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Abstract
Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
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Citations
23 Claims
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1. A compound of Formula V:
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wherein; A is nitrogen or oxygen; R11 is hydrogen, salt-forming cation, ester forming group, —
(CH2)x-Q, or when A is nitrogen, A and R11 taken together may be the residue of a natural or unnatural amino acid or a salt or ester thereof, wherein A and R11 taken together are not a leucine residue;Q is hydrogen, thiazolyl, triazolyl, imidazolyl, benzothiazolyl, or benzoimidazolyl; x is 0, 1, 2, 3, or 4; n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; aa is a natural or unnatural amino acid residue; m is 1, 2, or 3; R14 is hydrogen or protecting group; R15 is hydrogen, alkyl or aryl; and
pharmaceutically acceptable salts, esters, or prodrugs thereof;wherein when A is oxygen, R11 is hydrogen or a salt-forming cation, n is 2, m is 1, and R14 and R15 are both hydrogen, then aa is other than phenylalanine, and wherein when A is oxygen, R11 is hydrogen or a salt-forming cation, n is 2, 3 or 4, m is 2, and R14 and R15 are both hydrogen, then aa is other than D-phenylalanine. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23)
and pharmaceutically acceptable salts, esters, or prodrugs thereof.
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18. A method of treating or preventing an amyloid-related disease or condition in a subject comprising administering, to a subject in need thereof, a compound of claim 1 in an amount effective to treat or prevent an amyloid related disease.
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19. The method according to claim 18, wherein said amyloid-related disease or condition is Alzheimer'"'"'s disease, mild cognitive impairment, mild-to-moderate cognitive impairment, age-related cognitive decline, senile dementia, vascular dementia, cerebral amyloid angiopathy, inclusion body myositis, macular degeneration, or Down'"'"'s syndrome.
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20. A pharmaceutical composition comprising a compound according to claim 1.
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21. The pharmaceutical composition of claim 20, wherein said pharmaceutical composition comprises an effective amount of said compound and a pharmaceutically acceptable carrier.
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22. The pharmaceutical composition of claim 21, wherein said effective amount is effective to treat or prevent an amyloid related disease or condition.
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23. The pharmaceutical composition of claim 22, wherein said amyloid related disease or condition is Alzheimer'"'"'s disease, mild cognitive impairment, mild-to-moderate cognitive impairment, age-related cognitive decline, senile dementia, vascular dementia, cerebral amyloid angiopathy, inclusion body myositis, age-related macular degeneration, or Down'"'"'s syndrome.
Specification