	US 11,980,631 B2
	β-lactamase inhibitors
Jürgen Brem, Oxford (GB); Christopher J. Schofield, Oxford (GB); Samuel T. Cahill, Oxford (GB); Karina Calvopina, Oxford (GB); Philip Hinchcliffe, Oxford (GB); Ricky Cain, Oxford (GB); James Spencer, Oxford (GB); Collin W. G. Fishwick, Oxford (GB); and Matthew B. Avison, Oxford (GB)
Assigned to OXFORD UNIVERSITY INNOVATION LIMITED, Oxford (GB)
Appl. No. 16/614,052
Filed by Oxford University Innovation Limited, Oxford (GB)
PCT Filed May 18, 2018, PCT No. PCT/GB2018/051353 § 371(c)(1), (2) Date Nov. 15, 2019, PCT Pub. No. WO2018/211289, PCT Pub. Date Nov. 22, 2018.
Claims priority of application No. 1708002 (GB), filed on May 18, 2017.
Prior Publication US 2021/0275552 A1, Sep. 9, 2021
Int. Cl. A61K 31/69 (2006.01); A61K 31/407 (2006.01); A61K 31/427 (2006.01); A61K 31/431 (2006.01); A61K 31/546 (2006.01); A61P 31/04 (2006.01)

CPC A61K 31/69 (2013.01) [A61K 31/407 (2013.01); A61K 31/427 (2013.01); A61K 31/431 (2013.01); A61K 31/546 (2013.01); A61P 31/04 (2018.01)]

7 Claims

1. A combination therapeutic product comprising a β-lactamase inhibitor of Formula Ic, or a pharmaceutically acceptable salt thereof, and one or more β-lactam antibiotics, wherein the β-lactamase inhibitor of Formula Ic has the structural formula shown below:

wherein:

n is 0 or 1;

R₁is a substituent group of the formula:

—X—Z

wherein

X is —N(R^A3)—C(O), wherein R^A3is selected from hydrogen or (1-2C)alkyl; and

Z is (1-6C)alkyl, aryl or (3-6C)cycloalkyl;

and wherein Z is optionally further substituted by one or more substituent groups independently selected from oxo, halo, cyano, nitro, hydroxy, carboxy, NR^A6R^A7, —(CH₂)_p—NR^A6R^A7(wherein p is selected from 1 or 2 (1-4C)alkoxy, (1-4C)alkyl or (1-4C)alkanoyl; wherein R^A6and R^A7are each independently selected from hydrogen, (1-4C)alkyl or (1-4C)alkylamino; and

R₂is a substituent of the formula —C(O)OR_2A, wherein R_2Ais selected from hydrogen, (1-6C)alkyl or (3-8C)cycloalkyl.