US 11,141,453 B1Granted

Pristinamycin compositions, LpxC compositions, their improvements, and combinations thereof

AssigneeFleurir Abx LLC

InventorJohn Lee Pace

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Abstract

New improved formulations are described, comprising at least one composition, with or without another composition, in which the at least one composition is an inhibitor of lipid A deacetylase resulting in permeabilization of an outer membrane of a susceptible microorganism to which it is provided to. The another composition is a streptogramin. Said at least one composition, alone or in combination, may be used to improve and/or treat a wide variety of bacterial infections, providing better efficacy, bioavailability, and/or pharmacokinetics, as compared with at least other or alternative inhibitors of lipid A deacetylase. When provided to a susceptible microorganism as a combination described herein, of the at least one composition and the another composition, the combination may be provided independently or may be provided together (co-combined in a same formulation, or in different formulations). Such combinations may also be provided via any route(s), and in any pharmaceutically acceptable form known, available, and/or suitable for use, such as to a subject in need thereof.

Claims20

Dependent claims

A composition comprising:

at least a first composition and second composition,
wherein the first composition and the second composition when provided are synergistic in their effect on a susceptible microorganism,
wherein the first composition is a streptogramin that interacts with ribosomal RNA of the susceptible microorganism and prevents protein synthesis of the susceptible microorganism,
wherein the second composition is an inhibitor of lipid A deacetylase resulting in permeabilization of an outer membrane of the susceptible microorganism to which it is provided to, the second composition being in the form of Formula I, Formula II, or Formula III,
wherein addition of the second composition is specifically provided to affect the outer membrane of the susceptible microorganism and sensitize the susceptible microorganism to the streptogramin, the first composition and the second composition being provided in a formulation selected from one of:
(i) a same formulation;
(ii) concomitantly in two independent formulations, and (iii) sequentially in two independent formulations,
wherein the susceptible microorganisms is selected from at least one of the group selected from Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Coxiella burnetti, Haemophilus influenzae, Moraxella catarrhalis, Legionella pneumophila, Chlamydia pneumoniae, Mycoplasma pneumoniae, Acinetobacter baumanii, Burkoholderia spp., Pseudomonas aeruginosa, Escherichia coli, extended spectrum beta-lactamase-producing Escherichia coli, carbapenemase-producing Escherichia coli, Klebsiella pneumonia, Francisella tularensis, Moraxella catarrhalis, Stenotrophomonas maltophila, and Yersinia pestis,
wherein Formula I is:
wherein Formula II is:
wherein Formula III is:
wherein R1 is any one of:
H,
wherein R2 is any one of:
H,
and
wherein R3 is any one or more of:

14 more elements

A composition comprising an inhibitor of lipid A deacetylase,

the composition being in a form of any one or more of Formula I, Formula II, and Formula III,
the lipid A deacetylase being in a susceptible microorganism,
the composition resulting in permeabilization of an outer membrane of the susceptible microorganism to which it is provided to in order to subsequently or concomitantly provide to the susceptible microorganism a streptogramin,
the composition sensitizing the susceptible microorganism to the streptogramin,
wherein the composition is for use as an antimicrobial and when the streptogramin is subsequently or concomitantly provided, a combination of the composition and the streptogramin have a bacteriostatic effect with respect to the susceptible microorganism, and
wherein a combination of the composition and the streptogramin illicits activity as is a broad-spectrum antimicrobial that also exhibits better efficacy as the combination, as compared with either the composition when used alone as an antimicrobial, or the streptogramin when used alone as an antimicrobial,
wherein Formula I is:
wherein Formula II is:
wherein Formula III is:
wherein R1 is any one of:
H,
wherein R2 is any one of:
H,
and
wherein R3 is any one or more of:

12 more elements

Dependencies are inferred from the claim text.

Facts

Application: 16/429,519Filed 3 Jun 2019 · continuation
Priority: 14 Mar 2014
Granted: 12 Oct 2021
Term ends: Not estimatedThe source records don’t support an estimate.

Classification16 codes

A61K 38/06
Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof: tripeptides
A61K 9/0019
Galenical forms characterised by the site of application: injectable compositions; Intramuscular, intravenous, arterial, subcutaneous…
A61K 9/0053
Galenical forms characterised by the site of application: mouth and digestive tract, i.e. intraoral and peroral administration
A61K 9/0073
Pulmonary tract; Aromatherapy: sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy

Family

Application61/953,721Us provisional application · filed 14 Mar 2014
Application14/659,609Parent of this continuation · filed 16 Mar 2015
Application15/401,085Parent of this continuation · filed 8 Jan 2017
US 9,539,305 B1Parent of this continuation · filed 10 Jan 2017
Application15/877,338Parent of this continuation · filed 22 Jan 2018
US 9,872,884 B1Parent of this continuation · filed 23 Jan 2018
US 10,307,457 B1Parent of this continuation
US 11,141,453 B1This patent

From the US filing history. Foreign family members aren’t listed.