MRI IMAGING OF AMYLOID PLAQUE USING LIPOSOMES

摘要

Provided are aromatic compounds, phospholipid-polymer-aromatic conjugates comprising the aromatic compounds, and liposome compositions including the phospholipid-polymer-aromatic conjugates. The liposomal compositions may be useful for imaging of Alzheimer's Disease, for example, imaging of the amyloid-β plaque deposits characteristic of Alzheimer's Disease.

主权项

1. A liposomal composition, comprising:
a membrane, comprising:
a phospholipid-polymer-aromatic conjugate, the aromatic moiety in the phospholipid-polymer-aromatic conjugate being represented by Structural Formula I:
—X—Ar—R1-Het  (I) wherein:
X is —R2—O— or —R2—N(R3)—;R1 is C2-C6 alkyl or alkenyl;R2 is a linking group comprising 1 to 6 carbon atoms that is one of: alkylene or alkoxyalkylene;R3 is hydrogen, C1-C6 alkyl, or C1-C6 alkoxyalkyl;Ar is a monocyclic or polycyclic group comprising at least one aromatic or heteroaromatic ring;Het is a monocyclic or polycyclic group comprising at least one heteroaromatic ring;R2 is substituted with zero, one or more of: hydroxyl, C1-C6 alkyl, and C1-C6 hydroxyalkyl; andAr, Het, R1, and R3 other than hydrogen are independently substituted with zero, one or more of: halogen; —OH; alkyl, —O-alkyl, aryl, —O-aryl or —(O-alkylene)1-6 optionally substituted with —OH or halogen; —NH2; —NH— alkyl; —N— dialkyl; carboxyl; sulfonyl; carbamoyl; and glycosyl.