Patent classifications
A61K49/085
HETEROCHIRAL PEPTIDE-COMPLEX AND COMPOSITION FOR MEASURING NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY RESIDUAL DIPOLAR COUPLING CONTAINING SELF-ASSEMBLED INTERMEDIATES OF HETEROCHIRAL PEPTIDE-COMPLEX
The present disclosure relates to a heterochiral peptide complex, a self-assembled intermediate thereof, an alignment medium composition used for nuclear magnetic resonance spectroscopy residual dipolar coupling (NMR-RDC) measurement, which includes the same, and a method for NMR measurement for a biomolecule. Since the heterochiral peptide complex contains a β-sheet peptide and has superior structural stability against environmental factors such as heat, acidity and ionic strength, it is applicable as an alignment medium for measuring RDC for various biomolecules.
TARGETED CONTRAST AGENTS FOR MRI OF AMYLOID DEPOSITION
A liposomal composition (“ADx-001”) is provided, ADx-001 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 macrocyclic gadolinium-based imaging agent may be conjugated to a fourth phospholipid.
TARGETED CONTRAST AGENTS FOR MRI OF ALPHA-SYNUCLEIN DEPOSITION
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:
##STR00001##
wherein X is —CH.sub.2—, —CH.sub.2—CH.sub.2—, —CHO—, or —O—CO—; Y is —CH—CH═CH— or
##STR00002##
A and B are independently selected from C and N; R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from —H, halogen, —OH, and —CH.sub.3; and R.sub.5, R.sub.6, and R.sub.7 are independently selected from —H, halogen, —OH, —OCH.sub.3, —NO.sub.2, —N(CH.sub.3).sub.2, C.sub.1-C.sub.6 alkyl, or a substituted or unsubstituted C.sub.4-C.sub.6 aryl group, except that when A and/or B is N the adjacent R.sub.5 and/or R.sub.7 is —H, or a pharmaceutically acceptable salt thereof.
TARGETED CONTRAST AGENTS FOR MRI OF ALPHA-SYNUCLEIN DEPOSITION
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:
##STR00001##
wherein X is —CH.sub.2—, —CH.sub.2—CH.sub.2—, —CHO—, or —O—CO—; Y is —CH—CH═CH— or
##STR00002##
A and B are independently selected from C and N; R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from —H, halogen, —OH, and —CH.sub.3; and R.sub.5, R.sub.6, and R.sub.7 are independently selected from —H, halogen, —OH, —OCH.sub.3, —NO.sub.2, —N(CH.sub.3).sub.2, C.sub.1-C.sub.6 alkyl, or a substituted or unsubstituted C.sub.4-C.sub.6 aryl group, except that when A and/or B is N the adjacent R.sub.5 and/or R.sub.7 is —H, or a pharmaceutically acceptable salt thereof.
Manganese complexes with substituted bisphosphonates useful as imaging and therapeutic agents
Provided herein is a compound useful as a magnetic resonance imaging (MRI) contrast agent and a therapeutic agent, said compound having a structure represented by: Y—X—Z wherein, X is Mn(II), and Y and Z are each independently a bisphosphonate coupled to one or more therapeutic agents. Methods of use of the compound for MRI imaging and treatment for cancer or a microbial infection are also provided.
METHODS AND AGENTS FOR THE DETECTION AND TREATMENT OF CANCER
An agent for use in detecting, monitoring, and/or imaging cancer cells and/or cancer cell metastasis, migration, dispersal, and/or invasion, and/or for treating cancer in a subject includes a targeting peptide and at least one of a detectable moiety, therapeutic agent, or a theranostic agent that is directly or indirectly linked to the targeting peptide. The targeting peptide specifically binds to and/or complexes with a proteolytically cleaved extracellular fragment of an immunoglobulin (Ig) superfamily cell adhesion molecule that is expressed by a cancer cell or another cell in the cancer cell microenvironment.
TARGETING LIGANDS FOR TAU PATHOLOGY
Methods and compositions for detecting tau pathology are described. The compositions for detecting tau pathology comprise a targeting ligand that specifically binds to a cell surface marker of tau pathology, wherein the targeting ligand is linked to a liposome that includes an imaging agent. The compositions can be used in a method for imaging tau pathology in a subject that comprises administering to the subject an effective amount of the composition to a subject and imaging at least a portion of the subject to determine if that portion of the subject exhibits tau pathology. The compositions can also be used to detect tau pathology in biological samples obtained from a subject.
FIBROBLAST ACTIVATION PROTEIN-TARGETED MAGNETIC RESONANCE IMAGING AGENTS, COMPOSITIONS, AND METHODS OF USE
A conjugate comprising FL-L-IA, wherein FL is a radical of a small molecule ligand that specifically binds with fibroblast activation protein (FAP), L is a linker, which binds an FL to IA, and IA is a radical of a magnetic resonance imaging (MRI) agent, or a pharmaceutically acceptable salt thereof; a composition comprising same; and a method of using the conjugate or composition to image cells, a tissue, or an organ that express(es) FAP with magnetic resonance imaging.
POLYROTAXANES BEARING MIXED CYCLODEXTRIN SPECIES AND USES THEREOF
Various embodiments of the present invention are directed to polyrotaxanes comprising a poloxamer core and at least one cyclodextrin and methods for treating Niemann-Pick type C (NPC) and imaging (e.g., MRI) using the polyrotaxanes of the various embodiments of the present invention.
COMPOSITIONS AND METHODS FOR TARGETING CELLS
The present invention provides compositions and methods for targeting cells for therapeutic and/or diagnostic purposes, e.g., delivery of therapeutic and/or diagnostic agents to a cell. Nanoparticles and polymers functionalized with capture molecules, reporter molecules, and/or therapeutic agents are provided for the treatment or prevention of disease, including neurological diseases associated with neuroinflammation, and cancer.