Patent classifications
A61K49/0039
TUBULAR SUPRAMOLECULAR POLYMERS
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.
MOLECULAR RENAL PROBES FOR DETECTING ACUTE KIDNEY INJURY
Disclosed herein are compounds or salts and/or solvates of formula I, II and III, where the compounds or salts and/or solvates have the following structures: (X).sub.a—Y—(Z).sub.b I; II; or X′—Y′ III; where X, Y, Z, Y′, a, b, R.sub.4, R.sub.6 and R.sub.7 are as defined herein.
##STR00001##
Conjugate and block copolymer containing fluorescent chromophore and preparation method therefor and use thereof
A conjugate containing a fluorescent chromophore, which has any structure selected from C1 to C3. The conjugate containing the fluorescent chromophore provided by the described embodiments includes one fluorescent chromophore and two highly reactive groups R1 and R2 linked to the fluorescent chromophore by a covalent bond. The fluorescent chromophore in the conjugate initially has no or only weak fluorescence emission capability, and only after the two highly reactive groups react together with the corresponding molecule, the fluorescent chromophore has strong fluorescence emission. Therefore, the efficiency of conjugation of drug molecules to targeting molecules can be monitored in situ by the infrared fluorescence emission intensity and applied to the target-mediated drug delivery. ##STR00001##
SELECTIVE HYDROGEN SULFIDE PROBE AND USES THEREOF
Provided herein is a compound of formula I:
##STR00001##
and the use thereof for detecting the presence of hydrogen sulfide in cells or tissues in vitro or in vivo. The detecting may be useful, for example, in diagnosing cancer or other diseases related to imbalanced hydrogen sulfide (H.sub.2S) production such as neurodegenerative diseases.
INORGANIC NANOCAGES, AND METHODS OF MAKING AND USING SAME
Provided are inorganic nanocages. The inorganic nanocages may be non-metal nanocages, transition metal oxide nanocages, or transition metal nanocages. Non-metal nanocages may include metal oxides. The inorganic nanocages can be made using micelles formed using pore expander molecules. The inorganic nanocages may be used as catalysts, drug delivery agents, diagnostic agents, therapeutic agents, and theranostic agents.
Quinone-containing conjugates
Conjugates comprise a drug or probe, a cell binding agent, and a quinone-containing linker. The quinone-containing linker may be reduced intracellularly to trigger release of the drug or probe. These conjugates may selectively deliver a drug or probe to a site of action of interest for local release of the active drug or probe.
CU(I)-CATALYZED AZIDE-ALKYNE CYCLOADDITIONS (CUAAC) LIGANDS AND METHODS FOR CARRYING OUT CU(I)-CATALYZED AZIDE-ALKYNE CYCLOADDITION REACTIONS
A Cu(I)-Catalyzed Azide-Alkyne Cycloadditions (CuAAC) ligand comprising: a catalytic core; a fluorous tag; and a linker binding the fluorous tag to the catalytic core. A method for carrying out a Cu(I)-Catalyzed Azide-Alkyne Cycloaddition reaction, comprising: combining in a solution an alkyne-tagged component, an azide-tagged component and a Cu(I)-Catalyzed Azide-Alkyne Cycloadditions (CuAAC) ligand comprising: a catalytic core; a fluorous tag; and a linker binding the fluorous tag to the catalytic core; filtering the solution through a solid phase extraction filter to remove Cu(I)-ligand catalyst and/or excess ligand.
Delivery system in micellar form having modular spectral response based on enzyme-responsive amphiphilic PEG-dendron hybrid polymers
The present invention relates to new molecular design that allows micelles to report their activation and disassembly by an enzymatic trigger. The molecular design is based on introduction of a labeling moiety selected from a fluorescent dye, a dark quencher, combinations of dyes or dyes/quenchers, and a fluorinated moiety (a .sup.19F-magenetic resonance (MR) probe for turn ON/OFF of a .sup.19F-MR signal) through covalent binding to the focal point of amphiphilic polymer-dendron hybrids with the labeling moiety. At the assembled micellar state, the dyes are closely packed and hence the probability for intermolecular interactions increases significantly, leading to alteration of the fluorescent properties (signal quench or shift) or the .sup.19F-MR signal (OFF state) of the micelles. Upon enzymatic cleavage of the hydrophobic end-groups from enzyme-responsive dendron, the polymers become hydrophilic and disassemble. This structural change is then translated into a spectral change as dye-dye interactions are halted and the dyes regain their intrinsic fluorescent properties, or alternatively by turn ON the .sup.19F-MR signal. The high modularity of the design allows the introduction of various types of dyes and thus enables rational adjustment of the spectral response. Two major types of responses are described: Turn-On/Off and spectral shift, depending on the type of labeling dye. The present invention further provides methods of use of the hybrid delivery system and to a kit comprising the same.
CELL PENETRATING PEPTIDES AND METHODS OF MAKING AND USING THEREOF
Disclosed herein are compounds having activity as cell penetrating peptides. In some examples, the compounds can comprise a cell penetrating peptide moiety and a cargo moiety. The cargo moiety can comprise one or more detectable moieties, one or more therapeutic moieties, one or more targeting moieties, or any combination thereof. In some examples, the cell penetrating peptide moiety is cyclic. In some examples, the cell penetrating peptide moiety and cargo moiety together are cyclic. In some examples, the cell penetrating peptide moiety is cyclic and the cargo moiety is appended to the cyclic cell penetrating peptide moiety structure. In some examples, the cargo moiety is cyclic and the cell penetrating peptide moiety is cyclic, and together they form a fused bicyclic system.
Cell penetrating peptides and methods of making and using thereof
Disclosed herein are compounds having activity as cell penetrating peptides. In some examples, the compounds can comprise a cell penetrating peptide moiety and a cargo moiety. The cargo moiety can comprise one or more detectable moieties, one or more therapeutic moieties, one or more targeting moieties, or any combination thereof. In some examples, the cell penetrating peptide moiety is cyclic. In some examples, the cell penetrating peptide moiety and cargo moiety together are cyclic. In some examples, the cell penetrating peptide moiety is cyclic and the cargo moiety is appended to the cyclic cell penetrating peptide moiety structure. In some examples, the cargo moiety is cyclic and the cell penetrating peptide moiety is cyclic, and together they form a fused bicyclic system.