US 12,453,785 B2
Macrocyclic chelators and methods of use thereof
Rhys Salter, Doylestown, PA (US); Vadim Dudkin, Chalfont, PA (US); Fengbin Song, Doylestown, PA (US); Wei Zhang, Malvern, PA (US); Shalom Goldberg, Merion Station, PA (US); and John Keith, San Diego, CA (US)
Assigned to Janssen Biotech, Inc., Horsham, PA (US)
Filed by JANSSEN BIOTECH, INC., Horsham, PA (US)
Filed on Jun. 30, 2022, as Appl. No. 17/810,316.
Application 17/810,316 is a continuation of application No. 16/869,771, filed on May 8, 2020, granted, now 11,576,986.
Claims priority of provisional application 62/846,044, filed on May 10, 2019.
Prior Publication US 2023/0110178 A1, Apr. 13, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 51/02 (2006.01); A61K 51/04 (2006.01); A61K 51/10 (2006.01)
CPC A61K 51/025 (2013.01) [A61K 51/0482 (2013.01); A61K 51/1027 (2013.01); A61K 51/1093 (2013.01)] 18 Claims
 
1. A chelator selected from the group consisting of:

OG Complex Work Unit Chemistry
wherein:
L1 is a linker selected from a substituted or unsubstituted alkyl, a substituted or unsubstituted heteroalkyl moiety, a substituted or unsubstituted aryl or heteroaryl, and a polyethylene glycol (PEG) moiety, wherein the alkyl, heteroalkyl, aryl, and heteroaryl are unsubstituted or substituted with one to three groups selected from alkyl, cycloalkyl, alkoxy, alkenyl, cycloalkenyl, alkynyl, cycloalkynyl, aryl, heterocyclyl, heteroaryl, halogen, hydroxy, amide, alkylthio, amino, alkylamino, aminoalkyl, hydroxyalkyl, hydroxyl, and carboxyl;
R11 is a —NH2, —NCS, —NCO, —N3, alkynyl, cycloalkynyl, —C(O)R13, —COOR13, —CON(R13)2, maleimido, acyl halide, tetrazine, or trans-cyclooctene, or R11 comprises an antibody or antigen binding fragment thereof, scaffold protein, small molecule, or aptamer; and
each R13 is independently hydrogen or alkyl.