US 12,246,019 B2
Alpha polyglutamated lometrexol and uses thereof
Clet Niyikiza, Gulph Mills, PA (US); and Victor Mandla Moyo, Ringoes, NJ (US)
Assigned to L.E.A.F. HOLDINGS GROUP LLC, Gulph Mills, PA (US)
Appl. No. 16/967,538
Filed by L.E.A.F. HOLDINGS GROUP LLC, Gulph Mills, PA (US)
PCT Filed Feb. 7, 2019, PCT No. PCT/US2019/016956
§ 371(c)(1), (2) Date Aug. 5, 2020,
PCT Pub. No. WO2019/157121, PCT Pub. Date Aug. 15, 2019.
Claims priority of provisional application 62/764,943, filed on Aug. 17, 2018.
Claims priority of provisional application 62/702,732, filed on Jul. 24, 2018.
Claims priority of provisional application 62/662,374, filed on Apr. 25, 2018.
Claims priority of provisional application 62/630,634, filed on Feb. 14, 2018.
Claims priority of provisional application 62/627,741, filed on Feb. 7, 2018.
Claims priority of provisional application 62/627,714, filed on Feb. 7, 2018.
Prior Publication US 2021/0338675 A1, Nov. 4, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/519 (2006.01); A61K 9/127 (2006.01); A61K 9/1277 (2025.01); A61K 31/202 (2006.01); A61K 31/683 (2006.01); A61K 31/7032 (2006.01); A61K 31/716 (2006.01); A61K 47/60 (2017.01); A61K 47/64 (2017.01); A61K 47/68 (2017.01); A61K 47/69 (2017.01); A61P 35/00 (2006.01)
CPC A61K 31/519 (2013.01) [A61K 9/127 (2013.01); A61K 9/1277 (2013.01); A61K 31/202 (2013.01); A61K 31/683 (2013.01); A61K 31/7032 (2013.01); A61K 31/716 (2013.01); A61K 47/60 (2017.08); A61K 47/645 (2017.08); A61K 47/6849 (2017.08); A61K 47/6913 (2017.08); A61P 35/00 (2018.01)] 20 Claims
OG exemplary drawing
 
1. A liposomal composition comprising an alpha polyglutamated lometrexol encapsulated by a liposome, wherein 4, 5, 6, 2-10, 4-6, or more than 5 glutamyl groups of the alpha polyglutamated lometrexol have an alpha carboxyl group linkage; and wherein the liposome is pegylated, wherein the liposome does not contain a targeting moiety having specific affinity for a surface antigen on a target cell,
wherein the liposome does not contain a cell penetrating peptide and does not contain a mitochondria penetrating peptide,
wherein the liposome has a zeta potential that is less than or equal to zero, between 0 to −150 mV, or between −30 to −50 mV, and
wherein the liposome is capable of delivering the alpha polyglutamated lometrexol directly into a cell.