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US 10,478,513 B2Granted
Nitroxide containing amyloid binding agents for imaging and therapeutic uses
AssigneeThe Regents of the University of Califonia
InventorsJohn Voss, Ruiwu Liu
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Abstract
The present invention provides methods of using nitroxide spin-labeled amyloid beta-binding compounds to image amyloid. The present invention also provides nitroxide spin-labeled amyloid beta-binding compounds.
Claims15
A method of imaging amyloid, comprising:
- administering to a subject an effective amount of a compound having the structure of Formula I:
- X—(Y)n (I)
- wherein
- X is an amyloid beta binding compound selected from the group consisting of:
- wherein
- Ra and Rb are each independently H or C1-4 alkyl;
- Z is selected from the group consisting of I, 123I, 125I, 131I, Br, 76Br, 77Br, F, 18F, and —O-tosyl;
- and
- q is an integer from 2 to 5;
- Y is a nitroxide selected from the group consisting of:
- n is an integer from 1 to 3;
- such that the compound binds to the amyloid;
- and
- detecting the compound bound to the amyloid, thereby imaging the amyloid.
11 more elements
A compound having the formula:
- wherein
- R1 and R2 are each independently H or a nitroxide selected from the group consisting of:
- wherein at least one of R1 and R2 is a nitroxide.
A compound having the formula:
- wherein
- R1 and R2 are each independently H,
- or a nitroxide selected from the group consisting of:
- wherein at least one of R1 and R2 is a nitroxide.
1 more element
A compound having the formula:
- wherein
- R1 is selected from the group consisting of:
- and
- R2 is selected from the group consisting of OH, OCH3, OCH2CH3, OCH2CH2F, CH3, and (OCH2CH2)3F.
1 more element
A compound having the formula:
- wherein
- R1 is selected from the group consisting of:
- and
- R2 is selected from the group consisting of OH, OCH3, OCH2CH3, OCH2CH2F, CH3, and (OCH2CH2)3F.
1 more element
A compound selected from the group consisting of:
A method of treating a disorder, the method comprising administering to a subject in need thereof, a therapeutically effective amount of a Formula I:
- X—(Y)n (I)
- wherein X is an amyloid beta binding compound selected from the group consisting of:
- wherein
- Ra and Rb each independently H or C1-4 alkyl,
- Z is selected from the group consisting of I, 123I, 125I, 131I, Br, 76Br, 77Br, F, 18F, and O-tosyl, and q is an integer from 2 to 5;
- Y is a nitroxide selected from the group consisting of:
- and
- n is an integer from 1 to 3;
- wherein the disorder is selected from the group consisting of Alzheimer's disease, diabetes, Parkinson's disease, spongiform encephalopathy, Huntington's disease, thyroid carcinoma, atrial amyloidosis, atherosclerosis, arthritis, prolactinomas, polyneuropathy, corneal dystrophy, and cerebral amyloid angiopathy.
6 more elements
Dependencies are inferred from the claim text.