BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF

摘要

Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents. Other embodiments relate to pharmaceutical compositions containing boronic acid derivatives and additional excipient such as meglumine.

主权项

1. A compound having the structure of Formula (I) or Formula (I.1):or pharmaceutically acceptable salts thereof, wherein:
G is selected from the group consisting of —H, —NR1R2, —CH2N3, —C(O)NR1R2, —CH2C(O)NR1R2, —CH2S(O)2NR1R2, —CH2—Y—Z, —CH2—Y—X, and —SR3; Y is selected from a group consisting of —S—, —S(O)—, —S(O)2—, —O—, and —NR1—; R is selected from a group consisting of —H, —C1-9alkyl, —CR1R2OC(O)C1-9alkyl, —CR1R2OC(O)OC1-9alkyl, and R1 and R2 are each independently selected from the group consisting of —H and —C1-4alkyl; R3 is —C1-4alkyl; R4 is present 1 to 3 times and each R4 is independently selected from the group consisting of —H, —C1-4alkyl, —OH, —O—C1-4alkyl, —S—C1-4alkyl, halogen, and —CF3, Z is selected from the group consisting of aryl optionally substituted with C1-4alkyl, amino, hydroxy, or halogen; heteroaryl optionally substituted with C1-4alkyl, amino, hydroxy, or halogen; and heterocycle optionally substituted with C1-4alkyl, amino, hydroxy, or halogen; X is selected from the group consisting of —C1-4alkyl, —CH2R5, —CH(R5)2, and —C(R5)3; and R5 is selected from the group consisting of a halogen, cyano, and azido.