A61K47/552

Antibacterial agents: dual-targeted RNA polymerase inhibitors

The invention provides bipartite, dual-targeted inhibitors of bacterial RNA polymerase having the general structural formula (I): X-α-Y (I) wherein X is an moiety that binds to the Rif target of a bacterial RNA polymerase; Y is a moiety that binds to the bridge-helix N-terminus target of a bacterial RNA polymerase; and is a covalent bond or a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

COMPOSITIONS COMPRISING FULLERENYL MESOCHLORIN NANO-PHOTOSENSITIZERS WITH COVALENTLY BOUND ANTIBIOTICS AND THEIR USES IN COMBINATION THERAPY
20220259219 · 2022-08-18 ·

Described herein are C.sub.60/70/PS-CB-Abx and nano-C.sub.60/70PS compounds, their pharmaceutical compositions, and methods pf photodynamic therapy using the compounds and compositions.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF PAIN AND DEPENDANCE DISORDERS

Provided herein are (e.g., controlled release) compositions for the treatment of acute or chronic diseases or disorders. Described herein are processable opioid conjugates. Also described herein are compositions and methods for the treatment of central nervous system (CNS) diseases or disorders including chronic pain (e.g., cancer pain), acute pain, opioid addiction, alcohol addiction, alcohol dependence, opioid-induced constipation, and narcotic depression. Said compositions and methods comprise opioid agonists and/or opioid antagonists, which demonstrate CNS activity and/or other desirable activities. Injection of said compositions subcutaneously or intraspinally provides therapeutic benefit to individuals suffering from CNS diseases or disorders

HSP90-BINDING CONJUGATES AND COMBINATION THERAPIES THEREOF

The disclosure generally relates to a method of treating cancer comprising administering HSP90-binding conjugates or administering two distinct therapeutic agents as a combination therapy. Components of the combination therapy and methods of using the combination therapy are provided.

Beta-Lactam-Cannabinoid Conjugate Molecules
20220257778 · 2022-08-18 ·

This disclosure provides multifunctional conjugate molecules in which at least one β-lactam antibiotic is covalently attached to a cannabinoid by means of a linker. The disclosed conjugate molecules are designed to deliver therapeutic benefits as intact molecules, with release of the cannabinoid upon binding of the β-lactam antibiotic to its target conveying further therapeutic benefits, and can be used to treat bacterial infections and other disorders.

PYRROLOBENZODIAZEPINE DIMER PRODRUG AND LIGAND-LINKER CONJUGATE COMPOUND OF THE SAME

The present disclosure relates to pyrrolobenzodiazepine dimer prodrugs and ligand-linker conjugates thereof. The present disclosure also relates to compositions and uses of said prodrugs and conjugates.

CLICK CHEMISTRY CAPTURABLE PLATINUM-BASED ANTINEOPLASTIC AGENTS

A chemotherapy agent comprising a chemotherapy group and a ligand secured to the chemotherapy group is disclosed, the ligand comprising a reactive group capable of bonding to a capture substrate. A method of removing chemotherapy agents from a patient is disclosed, the method comprising providing a chemotherapy agent containing a reactive group; providing a capture substrate in contact with a patient's bloodstream; administering the chemotherapy agent to the patient; and sequestering the chemotherapy agent on the capture substrate. A system for removing chemotherapy agents is also disclosed.

ANTICANCER AGENTS

The claimed subject matter provides for a method for conjugating an active material to a Pt complex.

PEPTIDE DERIVATIVES AND CONJUGATES THEREOF FOR TREATING CANCER
20220211860 · 2022-07-07 ·

Provided herein are luteinizing hormone-releasing hormone (LHRH) peptide derivatives that target the LHRH receptor. LHRH peptide derivatives, LHRH peptide-drug conjugates (LHRH-PDCs) and methods of using the derivatives and/or conjugates thereof to treat a LHRH receptor expressing cancer are described.

Homodimeric Tobramycin Adjuvant Repurposes Novobiocin as an Effective Antibacterial Agent Against Gram-Negative Bacteria
20220249441 · 2022-08-11 ·

Low permeability across the outer membrane is a major reason why most antibiotics are ineffective against Gram-negative bacteria. Agents that permeabilize the outer membrane are typically toxic at their effective concentrations. Here, we report the development of a broad-spectrum homodimeric tobramycin adjuvant that is non-toxic and more potent than the gold standard permeabilizing agent, polymyxin B nonapeptide. In pilot studies, the adjuvant confers potent bactericidal activity on novobiocin against Gram-negative bacteria, including carbapenem-resistant and colistin-resistant strains bearing plasmid-borne mcr-1 genes. Resistance development to the combination was significantly reduced, relative to novobiocin alone, and there was no induction of cross-resistance to other antibiotics, including the gyrase-acting fluoroquinolones. Tobramycin homodimer may allow the use of lower doses of novobiocin, overcoming its twin-problem of efficacy and toxicity.