US 12,246,010 B2
Formulations of tegavivint and related compounds
Steven David Dykstra, Apex, NC (US); Henry Havel, Houston, TX (US); Stephen Horrigan, Houston, TX (US); Roger Harrison, Houston, TX (US); Jeffrey Larson, Houston, TX (US); Jonathan Northrup, Houston, TX (US); Theodore Laslo, Wind Gap, PA (US); and Garry Gwozdz, Jim Thorpe, PA (US)
Assigned to Iterion Therapeutics, Inc., Houston, TX (US)
Filed by Iterion Therapeutics, Inc., Houston, TX (US)
Filed on Feb. 25, 2022, as Appl. No. 17/681,132.
Application 17/681,132 is a continuation of application No. 16/428,347, filed on May 31, 2019, granted, now 11,266,637.
Claims priority of provisional application 62/679,404, filed on Jun. 1, 2018.
Prior Publication US 2022/0184051 A1, Jun. 16, 2022
Int. Cl. A61K 31/15 (2006.01); A61K 9/12 (2006.01); A61K 31/18 (2006.01); A61K 31/444 (2006.01); A61K 47/26 (2006.01); A61K 47/34 (2017.01); A61P 11/00 (2006.01)
CPC A61K 31/444 (2013.01) [A61K 9/124 (2013.01); A61K 47/26 (2013.01); A61K 47/34 (2013.01); A61P 11/00 (2018.01); A61K 31/15 (2013.01); A61K 31/18 (2013.01)] 15 Claims
 
1. A composition consisting of:
a) particles of a compound of Formula I

OG Complex Work Unit Chemistry
wherein RA is hydrogen, R7 and R8 are independently selected from H and SO2NR3R4, wherein one of R7 and R8 is hydrogen and wherein NR1R2 and NR3R4 are independently 6-to 15-membered heterocycloalkyl containing one nitrogen in the ring, or a pharmaceutically acceptable salt, ester, amide, stereoisomer or geometric isomer thereof,
b) a poloxamer surfactant;
c) sorbitol; and
d) water,
wherein the compound of Formula I and the poloxamer surfactant are provided in an aqueous suspension that is milled using roller milling or high energy milling until 90% of the particles are less than or equal to about 0.23 micrometers (μm) in diameter when measured using laser diffraction, and wherein the sorbitol is provided in an aqueous solution that is added thereto.