	US 12,257,312 B2
	Conjugates comprising a temperature-responsive polymer and a ligand capable of binding ergosterol
Prashant Garg, Hyderabad (IN); Stephen Rimmer, Bradford (GB); and Charles William Ian Douglas, Sheffield (GB)
Assigned to HYDERABAD EYE INSTITUTE, Hyderabad (IN); UNIVERSITY OF BRADFORD, Bradford (GB); and UNIVERSITY OF SHEFFIELD, Sheffield (GB)
Appl. No. 17/055,768
Filed by Hyderabad Eye Institute, Hyderabad (IN); UNIVERSITY OF BRADFORD, Bradford (GB); and UNIVERSITY OF SHEFFIELD, Sheffield (GB)
PCT Filed May 17, 2019, PCT No. PCT/GB2019/051369 § 371(c)(1), (2) Date Nov. 16, 2020, PCT Pub. No. WO2019/220137, PCT Pub. Date Nov. 21, 2019.
Claims priority of application No. 201841018524 (IN), filed on May 17, 2018; and application No. 201841018607 (IN), filed on May 18, 2018.
Prior Publication US 2021/0228734 A1, Jul. 29, 2021
Int. Cl. A61K 47/69 (2017.01); A61K 9/06 (2006.01); A61K 31/7048 (2006.01); A61K 31/785 (2006.01); A61K 38/12 (2006.01); A61K 38/14 (2006.01); A61K 47/58 (2017.01); A61P 31/10 (2006.01); C12Q 1/04 (2006.01)

CPC A61K 47/6903 (2017.08) [A61K 9/06 (2013.01); A61K 31/7048 (2013.01); A61K 31/785 (2013.01); A61K 38/12 (2013.01); A61K 38/14 (2013.01); A61K 47/58 (2017.08); A61P 31/10 (2018.01); C12Q 1/04 (2013.01)]

13 Claims

1. A polymer conjugate, or a salt thereof, having the general formula:

P−[Q]_x

wherein:

P is a branched temperature-responsive polymer comprising a plurality of functional groups, wherein one or more of said functional groups are covalently attached to a ligand capable of binding to ergosterol;

Q is a ligand capable of binding to ergosterol; and

x is the percentage of functional groups on the branched temperature-responsive polymer, P, that are attached to Q, wherein x is greater than or equal to 10%,

wherein the branched temperature-responsive polymer, P, is branched poly(N-isopropylacrylamide); and the ligand capable of binding to ergosterol, Q, is amphotericin B, nystatin or natamycin; and

wherein each ligand capable of binding to ergosterol, Q, present in the polymer conjugate is bound to a terminus of one of the branches of the branched temperature-responsive polymer, P, by the reaction of a carboxyl group present on the branched temperature-responsive polymer, P, with an amine group present on the ligand capable of binding to ergosterol, Q, to form a —C(O)—NH-linking group.