Back to results
US 2016/0101197 A1Published application
MRI Imaging of Amyloid Plaque Using Liposomes
OwnerAnanth V. Annapragada, Eric A. Tanifum +1inventors
InventorsAnanth V. Annapragada, Eric A. Tanifum, Mayank Srivastava
Life of this patent
Estimating the term…
Abstract
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.
Claims20
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;
- and
- Ar, 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.
22 more elements
A method for imaging amyloid deposits in a patient, the method comprising:
- introducing into the patient a detectable quantity of a liposomal composition, the 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;
- and
- Ar, 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;
- a nonradioactive magnetic resonance imaging (MRI) contrast enhancing agent at least one of encapsulated by or bound to the membrane;
- allowing sufficient time for the liposomal composition to be associated with one or more amyloid deposits;
- and
- detecting the liposomal composition associated with the one or more amyloid deposits.
27 more elements
A kit for imaging amyloid deposits in a patient, the kit comprising:
- a liposomal composition, the 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;
- and
- Ar, 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;
- a nonradioactive magnetic resonance imaging (MRI) contrast enhancing agent at least one of encapsulated by or bound to the membrane;
- Instructions, the instructions directing a user to
- introduce into the patient a detectable quantity of the liposomal composition;
- allow sufficient time for the liposomal composition to be associated with one or more amyloid deposits;
- and
- detect the liposomal composition associated with the one or more amyloid deposits.
29 more elements
Dependencies are inferred from the claim text.