A61K49/0021

PROGRAMMABLE POLYMERIC DRUGS

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I):

##STR00001##

or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, L, L.sup.1, L.sup.2, L.sup.3, M and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.

ATHEROSCLEROSIS IMAGING AGENTS AND METHODS OF USING THE SAME

Methods for detecting the presence of atherosclerotic structures in order to diagnose or prevent atherosclerosis are provided herein. In particular, it has been found that methylene blue injected intravenously acts as an excellent indicator because the compound targets high-risk plaque, atheroma, macrophages, and other atherosclerotic structures formed within the endothelial walls of a vessel of a subject. Because the compound provides a unique binding profile with uptake only in plaque or atheroma, and not the normal or healthy vascular interstitial tissue, methylene blue maintains a good plaque-to-background ratio for imaging purposes. This enables healthcare providers to determine the status of atherosclerosis development in vivo within a patient with higher certainty and at lower costs. The disclosed methods allow for high-resolution mapping of plaque build-up, plaque pathobiology, and other atherosclerotic structures within a vessel of a subject by using methylene blue as an imaging agent.

FLUORESCENT PROBES FOR MONOACYLGLYCEROL LIPASE (MAGL)

The invention provides fluorescent probes having the general formula (I)

##STR00001##

wherein X, Y, L and R.sup.1 to R.sup.4 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

BIOHYBRID PEPTIDOGLYCAN OLIGOMERS

The invention relates to a compound of formula Ia and/or formula Ib: or a pharmaceutically acceptable salt, solvate or prodrug thereof, where the groups are defined herein. The invention also relates to a pharmaceutical formulation comprising the compound for treating or detecting a microbial infection in a subject, a method of determining antimicrobial resistance of a microbial infection using the compound, and a method of determining an effective dose of one or more antimicrobial agents to kill a microorganism using the compound.

TUBULAR SUPRAMOLECULAR POLYMERS
20220211858 · 2022-07-07 ·

The present invention provides the design of a class of prodrugs for self-assembly into therapeutic tubular supramolecular polymers and their use in a wide variety of applications. The therapeutic tubular supramolecular polymers can be used to formulate drugs and imaging agents for in vitro and in vivo uses.

IMAGING WITH LIPOSOME-BASED CONTRAST AGENTS BASED ON MODULATION OF MEMBRANE WATER PERMEABILITY

The present disclosure provides imaging and contrast agents, and methods of using the agents. According to some embodiments of the disclosure, agents and methods for magnetic resonance imaging and related technologies are provided.

PROTECTED TRIAZABUTADIENE COMPOSITIONS FOR CELLULAR STUDIES IN INTACT BIOLOGICAL SYSTEMS

Protected triazabutadiene molecules, such as those according to Formula D or variations thereof, as probes for cellular studies in intact biological systems. The protected triazabutadiene probes selectively release benzene diazonium ions (BDIs) intracellularly, providing a tool for accessing and/or labeling intracellular proteins or molecules prior to cell lysis. The present invention also includes methods for synthesizing the protected triazabutadienes, the protected triazabutadienes themselves, and methods of use.

DENDRIMER COMPOSITIONS AND USE IN TREATMENT OF NECROTIZING ENTEROCOLITIS AND OTHER GASTROINTESTINAL DISORDERS

A dendrimer formulation, such as a PAMAM dendrimer or a multiarm PEG polymeric formulation has been developed for oral administration to the gastrointestinal tract for treatment of inflammatory diseases associated with infection or cancer. In the preferred embodiment, the dendrimers are in the form of dendrimer nanoparticles comprising poly(amidoamine) (PAMAM) hydroxyl-terminated dendrimers covalently linked to at least one therapeutic, prophylactic or diagnostic agent for treatment of one or more symptoms of necrotizing enterocolitis.

Compositions and methods for assessing gut function

Compositions and methods for assessing gut function are disclosed. They are designed to provide accurate, rapid, point-of-care or in-community assessment of enteric dysfunction.

Compositions and methods for assessing gut function

Compositions and methods for assessing gut function are disclosed. They are designed to provide accurate, rapid, point-of-care or in-community assessment of enteric dysfunction.