BORONIC ACID ESTERS AND PHARMACEUTICAL FORMULATIONS THEREOF

摘要

Provided herein are boronic acid esters of boronic acid therapeutic agents, such as bortezomib. The boronic acid esters can be used to prepare liposomal formulations of boronic acid therapeutic agents with improved properties, such as enhanced stability. This disclosure, in one aspect, relates to compositions and methods of making and using the compositions.

主权项

1. A compound defined by Formula Iwherein
P1 is hydrogen or an amino-group protecting moiety; R0 is hydrogen or an alkyl group; R1, R2, and R3 are independently hydrogen, an alkyl group, a cycloalkyl group, a heterocyclyl group, an aryl group, a heteroaryl group, or —CH2—R4; R4 is an aryl group, an alkylaryl group, an arylalkyl group, a cycloalkyl group, an alkylcycloalkyl group, a heterocyclyl group, an alkylheterocyclyl group, a heteroaryl group, an alkylheteroaryl group, an alkoxy group, or an alkylthio group; m is 0, 1, or 2; Z, together with O1 and O2, represent a moiety derived from a polyol; L is absent, or is a linking group; and A is a lipophilic moiety.