IP Library Granted Patent US 10,532,983
Granted Patent B2
US 10,532,983 · App. 15/215,103 · Granted Jan 14, 2020

Quinolone-3-diarylethers

Inventors: Michael Riscoe (Tualatin, OR); Aaron Nilsen (Portland, OR); Galen Miley (Portland, OR); Rolf Winter (Portland, OR); Sovitj Pou (Portland, OR); Jane Xu Kelly (Portland, OR); Rozalia Dodean (Portland, OR)
Assignee: Oregon Health & Science University
C07D215/22C07D405/12C07D409/12
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Quick Facts
Patent No.
US 10,532,983
App. No.
15/215,103
Granted
Jan 14, 2020
Kind
B2
Abstract

Disclosed are derivative compounds of ELQ-300 that include an ester at position 4. These compounds have enhanced properties relative to ELQ-300. Also disclosed are pharmaceutical compositions comprising the compounds and methods of treating and preventing malaria infections involving administering the pharmaceutical compositions to the subject.

Claims (10)

1. A compound of the structure:

wherein X is halogen and R is a carbonate ester, or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 wherein X is selected from fluoro and chloro, or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 wherein R is selected from methyl carbonate; ethyl carbonate; 2-methoxyethylcarbonate; 2-(2-methoxyethoxy)ethyl carbonate; (2-(2-(2-methoxyethoxy)ethoxy)ethyl) carbonate; allyl carbonate; tert-butyl carbonate; ((2,2-dimethyl-1,3-dioxolan-4-yl)methyl) carbonate; ((2-oxo-1,3-dioxolan-4-yl)methyl) carbonate; 2,3-dihydroxypropyl carbonate; and 1,1-dioxidotetrahydrothiophen-3-yl carbonate, or a pharmaceutically acceptable salt thereof.

4. The compound of claim 3 wherein X is chloro, or a pharmaceutically acceptable salt thereof.

5. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 3 wherein X is fluoro, or a pharmaceutically acceptable salt thereof.

7. The compound of claim 2 wherein X is fluoro, or a pharmaceutically acceptable salt thereof.

8. The compound of claim 2 wherein X is chloro, or a pharmaceutically acceptable salt thereof.

Continuity (3)
Provisional Application 62194636 · Jul 20, 2015
Provisional Application 62343319 · May 31, 2016
Related Publication 20170022164A1 · Jan 26, 2017