IP Library Granted Patent US 11,485,697
Granted Patent B2
US 11,485,697 · App. 17/177,314 · Granted Nov 1, 2022

Antimalarial compositions and uses thereof

Inventors: Wil Joseph Andahazy (Alexandria, VA); Arnab K. Chatterjee (San Diego, CA); Case W. Mcnamara (San Marcos, CA); Federico C. Beasley (San Diego, CA); Anders Mikal Eliasen (San Diego, CA); Hank Michael James Petrassi (San Diego, CA); Jason T. Roland (San Diego, CA); Timothy Wells (Chambesy, CH); Olga Vladimirovna Zatolochnaya (Danbury, CT); Fei Zhou (San Diego, CA); Peter G. Schultz (La Jolla, CA); Anil Kumar Gupta (San Diego, CA)
Assignee: THE SCRIPPS RESEARCH INSTITUTE
C07C50/32A61K9/10A61K9/141A61K31/232A61K31/47A61K45/06A61K47/44A61P33/02A61P33/06C07C2601/14
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Quick Facts
Patent No.
US 11,485,697
App. No.
17/177,314
Granted
Nov 1, 2022
Kind
B2
Abstract

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

Claims (13)

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.

Continuity (3)
Continuation 16311869
Provisional Application 62352455 · Jun 20, 2016
Related Publication 20210179524A1 · Jun 17, 2021