IP Library › Granted Patent US 12,552,815
Granted Patent B2
US 12,552,815 · App. 17/923,544 · Granted Feb 17, 2026

Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof

Inventors: Scott J. Hecker (Del Mar, CA); Serge Henri Boyer (San Diego, CA); Matthew M. Bio (Belmont, MA); Yuanqing Fang (Belmont, MA); Angela Gonzales de Castro (Maastricht, NL); Laurent Lefort (Maastricht, NL); Zuolin Zhu (Sacramento, CA); Thomas Linder (Linz, AT)
Assignee: QPEX BIOPHARMA, INC.
C07F5/025B01J23/44B01J23/755C07B2200/13
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Quick Facts
Patent No.
US 12,552,815
App. No.
17/923,544
Granted
Feb 17, 2026
Kind
B2
Abstract

Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

Claims (8)

1 . A crystalline form of Compound I′:

or a solvate thereof,

wherein the crystalline form exhibits an X-ray powder diffraction pattern comprising at least three characteristic peaks, wherein said characteristic peaks are selected from the group consisting of 6.2, 11.7, 12.4, 12.8, 16.7, 17.6, 19.1, 20.2, 20.6, 21.7, 22.0, 22.7, and 24.7±0.2 degrees 2θ.

2 . The crystalline form of claim 1 , wherein the crystalline form is a monohydrate.

3 . The crystalline form of claim 1 , wherein the crystalline form has an endotherm from 150° C. to 154° C.

4 . The crystalline form of claim 1 , wherein the crystalline form has a change in mass of less than 1% with a humidity change from 5% to 75%.

5 . The crystalline form of claim 1 , wherein the crystalline form has less than 1% weight loss in TGA from 140° C. to 238° C.

6 . The crystalline form of claim 1 , wherein the crystalline form is highly crystalline.

Continuity (2)
Provisional Application 63020494 · May 5, 2020
Related Publication 20250002508A1 · Jan 2, 2025
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