US 12,239,734 B2
Gamma polyglutamated raltitrexed and uses thereof
Clet Niyikiza, Gulph Mills, PA (US); and Victor Mandla Moyo, Ringoes, NY (US)
Assigned to L.E.A.F. HOLDINGS GROUP LLC, Gulph Mills, PA (US)
Appl. No. 16/967,293
Filed by L.E.A.F. HOLDINGS GROUP LLC, Gulph Mills, PA (US)
PCT Filed Feb. 7, 2019, PCT No. PCT/US2019/016993
§ 371(c)(1), (2) Date Aug. 4, 2020,
PCT Pub. No. WO2019/157140, PCT Pub. Date Aug. 15, 2019.
Claims priority of provisional application 62/764,945, filed on Aug. 17, 2018.
Claims priority of provisional application 62/702,774, filed on Jul. 24, 2018.
Claims priority of provisional application 62/662,372, filed on Apr. 25, 2018.
Claims priority of provisional application 62/630,652, filed on Feb. 14, 2018.
Claims priority of provisional application 62/627,733, filed on Feb. 7, 2018.
Prior Publication US 2021/0023006 A1, Jan. 28, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/127 (2006.01); A61K 9/1271 (2025.01); A61K 31/282 (2006.01); A61K 31/517 (2006.01); A61K 47/26 (2006.01); C07K 16/28 (2006.01)
CPC A61K 9/1271 (2013.01) [A61K 31/517 (2013.01); A61K 47/26 (2013.01); A61K 31/282 (2013.01); C07K 16/2818 (2013.01)] 21 Claims
OG exemplary drawing
 
1. A liposomal composition comprising a gamma polyglutamated raltitrexed encapsulated by a liposome, wherein the gamma polyglutamated raltitrexed contains 2-10 glutamyl groups having gamma carboxy group linkages, wherein the liposome is pegylated and 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 agent,
wherein the liposome has a zeta potential that is less than or equal to zero, between 0 and −150 mV, or between −30 and −50 mV, and
wherein the liposome is capable of delivering the gamma polyglutamated raltitrexed directly into a cell.