Antimalarial compositions and uses thereof

Patent metadata

Field	Value
Publication number	US-11485697-B2
Application number	US-202117177314-A
Country	US
Kind code	B2
Filing date	Feb 17, 2021
Priority date	Jun 20, 2016
Publication date	Nov 1, 2022
Grant date	Nov 1, 2022

Abstract

Provided herein are compounds, compositions and method of using thereof to treat or prevent malaria.

First claim

We claim:

1. A pharmaceutical suspension comprising nanoparticles or microparticles of a crystalline compound of Formula (III) or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof:

wherein: R 11 is C 1 -C 6 alkyl.

2. The pharmaceutical suspension according to claim 1 , wherein R 11 is C 6 alkyl.

3. The pharmaceutical suspension according to claim 1 , wherein the compound of Formula (III) is

or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof.

4. The pharmaceutical suspension according to claim 1 , wherein the suspension comprises microparticles of a crystalline compound of Formula (III) with average particle size in the range of about 1 μm to about 50 μm.

5. The pharmaceutical suspension according to claim 4 , wherein the suspension comprises microparticles of a crystalline compound of Formula (III) with average particle size in the range of about 5 μm to about 20 μm.

6. The pharmaceutical suspension according to claim 5 , wherein the suspension comprises microparticles of a crystalline compound of Formula (III) with average particle size in the range of about 10 μm to about 20 μm.

7. The pharmaceutical suspension according to claim 1 , further comprising a pharmaceutically acceptable excipient selected from surfactants, solubilizers, emulsifiers, preservatives, isotonicity agents, dispersing agents, wetting agents, fillers, solvents, buffers, stabilizers, lubricants, thickening agents, suspending agents, and any combinations thereof.

8. The pharmaceutical suspension according to claim 1 , further comprising Synperonic® F108, dodecyl sodium sulfate (SLS), D-a-tocopheryl polyethylene glycol 1000 succinate (TPGS), hydroxypropyl methylcellulose (HPMC), and any combinations thereof.

9. The pharmaceutical suspension according to claim 1 , wherein the concentration of the crystalline compound of Formula (III) or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof is between about 20 mg/mL and about 300 mg/mL.

10. The pharmaceutical suspension according to claim 9 , wherein the concentration of the crystalline compound of Formula (III) or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof is at least about 100 mg/mL.

11. The pharmaceutical suspension according to claim 1 , wherein R 11 is methyl.

Assignees

• Scripps Research Inst

Inventors

• Andahazy Wil Joseph
• Chatterjee Arnab K
• Mcnamara Case W
• Beasley Federico C
• Eliasen Anders Mikal
• Petrassi Hank Michael James
• Roland Jason T
• Wells Timothy
• Zatolochnaya Olga Vladimirovna
• Zhou Fei
• Schultz Peter G
• Gupta Anil Kumar

Classifications

• A61K47/44

  Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14) · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K9/141

  Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers ((co) spray-dried products A61K9/16, (co) lyophilised products A61K9/19; the carrier being chemically bound to the active ingredient A61K47/50) · CPC title

• A61K9/10 Primary

  Dispersions; Emulsions · CPC title

• A61K31/47

  Quinolines; Isoquinolines · CPC title