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US 2017/0283439 A1Published application
Probes for imaging huntingtin protein
AssigneeCCHDI Foundation Inc.
InventorsCelia Dominguez, John Wityak, Jonathan Bard, Alex Kiselyov, Christopher John Brown, Michael Edward Prime, Peter David Johnson, Daniel CLark-Frew
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Abstract
Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
Claims42
An imaging agent comprising a compound of Formula I,
- or a pharmaceutically acceptable salt thereof, wherein
- L1 is —CH═CH— or L1 is absent;
- R1 is chosen from phenyl or heteroaryl, each of which is optionally substituted with one, two, or three groups independently chosen from
- cyano,
- halo,
- heteroaryl,
- lower alkyl,
- lower alkyl substituted with one or two substituents independently chosen from lower alkoxy substituted with heteroaryl,
- —C(O)O-lower alkyl,
- hydroxyl,
- lower alkynyloxy,
- lower alkoxy, and
- lower alkoxy substituted with one or two substituents independently chosen from
- halo,
- heterocycloalkyl,
- heteroaryl,
- heteroaryl substituted with lower alkoxy,
- optionally substituted amino,
- alkyl substituted with heteroaryl, and
- alkyl substituted with heteroaryl substituted with lower alkoxy;
- or
- R1 is phenyl substituted with two groups, which taken together with the carbon atoms, to which they are bonded form a heterocycloalkenyl ring wherein said phenyl is further optionally substituted with a substituent chosen from
- halo,
- heteroaryl, and
- optionally substituted amino;
- L2 is —N(R4)— or L2 is absent;
- R2 is chosen from
- hydrogen,
- lower alkyl, and
- lower alkyl substituted with lower alkoxy, amino, (alkyl)amino, (dialkyl)amino, or hydroxy;
- for each occurrence, R3 is independently chosen from
- halo,
- cyano,
- lower alkoxy,
- lower alkyl optionally substituted with amino, (alkyl)amino, or di(alkyl)amino, and ethynyl optionally substituted with tri(alkyl)silyl;
- R4 is chosen from hydrogen and lower alkyl;
- and
- m is 0, 1, or 2,
- wherein the compound of Formula I, or a pharmaceutically acceptable salt thereof, is labeled with one or more positron-emitting radionuclides.
36 more elements
Dependencies are inferred from the claim text.