Molecular containers and methods of making and using same

摘要

Acyclic CB[n]-type compounds, methods of making such compounds, and uses of the compounds. For example, these compounds can be used as nanocontainers to solubilize pharmaceutical agents. Also provided are compositions and methods of using them for therapy or prophylaxis of a wide variety of conditions for which therapy or prophylaxis is desirable.

主权项

1. A composition comprising a pharmaceutical agent, wherein the pharmaceutical agent has a solubility of 33 mg/mL to less than 0.1 mg/mL in an aqueous solvent, wherein the pharmaceutical agent is non-covalently complexed to a compound having the following structure: or a salt, a partial salt, a hydrate, or a stereoisomer thereof, wherein each R is independently hydrogen, C1 to C20 alkyl group, C3 to C20 carbocyclic group, C1 to C20 heterocyclic group, carboxylic acid group, ester group, amide group, hydroxy, or ether group; wherein, optionally, adjacent R groups form a C3 to C20 carbocyclic ring or heterocyclic ring; wherein eachis independently a C5 to C20 carbocyclic ring system or C2 to C20 heterocyclic ring system, wherein the ring system comprises one or more rings;
wherein at least one ring system has at least one solubilizing group selected from sulfonic acid group, sulfonate salt group, phosphonic acid group, phosphonate salt group, and polyethylene glycol group; wherein, optionally, the ring system has a targeting group; wherein n is 1 to 5.