Targeted contrast agents for MRI of alpha-synuclein deposition

US11779664B2 · kind B2 · utility

Assignees

• Texas Children's Hospital · US
• Alzeca Biosciences, LLC · US

Inventors

• Eric A. Tanifum · Katy, US
• Xianwei Sun · Houston, US
• Ananth Annapragada · Manvel, US
• Carlo Medici · Reno, US

Key dates

• Filing date: May 5, 2022
• Grant date: Oct 10, 2023
• Expiry date: May 5, 2042

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2602/08
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A liposomal composition (“ADx-003”) is provided, ADx-003 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand, the targeting ligand being represented by Formula I: wherein X is —CH2—, —CH2—CH2—, —CHO—, or —O—CO—; Y is —CH—CH═CH— or A and B are independently selected from C and N; R1, R2, R3, and R4 are independently selected from —H, halogen, —OH, and —CH3; and R5, R6, and R7 are independently selected from —H, halogen, —OH, —OCH3, —NO2, —N(CH3)2, C1-C6 alkyl, or a substituted or unsubstituted C4-C6 aryl group, except that when A and/or B is N the adjacent R5 and/or R7 is —H, or a pharmaceutically acceptable salt thereof.