US 12,343,399 B2
Polymer linkers and their uses
Binyuan Sun, Needham Heights, MA (US)
Assigned to NOVACYTE THERAPEUTICS COMPANY., LTD, Beijing (CN)
Filed by NOVACYTE THERAPEUTICS COMPANY., LTD, Beijing (CN)
Filed on Nov. 16, 2022, as Appl. No. 17/988,595.
Application 16/774,829 is a division of application No. 15/572,720, granted, now 10,583,196, issued on Mar. 10, 2020, previously published as PCT/US2017/035698, filed on Jun. 2, 2017.
Application 17/988,595 is a continuation of application No. 16/774,829, filed on Jan. 28, 2020, granted, now 11,529,422.
Claims priority of provisional application 62/345,557, filed on Jun. 3, 2016.
Prior Publication US 2023/0119152 A1, Apr. 20, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 47/60 (2017.01); A61K 31/4745 (2006.01); A61K 47/16 (2006.01); A61K 47/22 (2006.01); A61K 47/68 (2017.01); A61P 35/00 (2006.01); C08G 65/00 (2006.01); C08G 65/48 (2006.01)
CPC A61K 47/60 (2017.08) [A61K 31/4745 (2013.01); A61K 47/16 (2013.01); A61K 47/22 (2013.01); A61K 47/6855 (2017.08); A61P 35/00 (2018.01); C08G 65/00 (2013.01); C08G 65/48 (2013.01)] 18 Claims
OG exemplary drawing
 
1. A compound of Formula (I) comprising block repeat block monomer (b):

OG Complex Work Unit Chemistry
wherein
L1 is a linking group selected from alkylene, heteroalkylene, cycloalkylene, heterocyclylene, arylene, heteroarylene, amidoalkylene, amidoheteroalkylene, and any combination thereof;
L2 is absent, or can be of the formula:

OG Complex Work Unit Chemistry
L2A is a linking group selected from alkylene, heteroalkylene, cycloalkylene, heterocyclylene, arylene, heteroarylene, —C(O)—, —NRc—, and any combination thereof;
L2B and L2C are independently absent or a linker group selected from alkylene, heteroalkylene, cycloalkylene, heterocyclylene, arylene, heteroarylene, amidoalkylene, amidoheteroalkylene, —C(O)—, —NRc—, and any combination thereof;
B2A and B2B are independently absent or a cleavable linker;
T is a therapeutic agent selected from the group consisting of chemotherapeutic agents, microtubule inhibitors, DNA-damaging agents and RNA transcription inhibitors, and block repeat block monomer (d):

OG Complex Work Unit Chemistry
wherein
L3 is a linker group selected from alkylene, heteroalkylene, cycloalkylene, heterocyclylene, arylene, heteroarylene, amidoalkylene, amidoheteroalkylene, and any combination thereof;
Re is a substituent selected from hydrogen, alkyl and heteroalkyl;
L4 is a group of the formula:

OG Complex Work Unit Chemistry
L4A is a linker group selected from alkylene, heteroalkylene, cycloalkylene, heterocyclylene, arylene, heteroarylene, —C(O)—, —NRc—, and any combination thereof;
L4B and L4C are independently absent or a linker group selected from alkylene, heteroalkylene, cycloalkylene, heterocyclylene, arylene, heteroarylene, amidoalkylene, amidoheteroalkylene, —C(O)—, —NRc—, and any combination thereof;
B4A and B4B are independently absent or a cleavable linker;
C4A is a group selected from

OG Complex Work Unit Chemistry
where
A is —H or a targeting moiety selected from the group consisting of an antibody, a synthetically functionalized antibody, a peptide and a targeting ligand;
“n” is independently at each occurrence an integer ranging from 0-5;
each cleavable linker B2A, B2B, B4A and B4B, if present, is independently selected from —S—S—, —C(═O)O—, —OC(═O)—, —C(═O)NRc—, —N(Rc)C(═O)—, —OC(═O)O—, —NRcC(═O)O—, —OC(═O)N(Rc)— or —N(Rc)C(═O)N(Rd)—, —C(═O)N(Rc)C(═O)—, —C(═O)S—, —SC(═O)—, —SC(═O)S—, —OC(═O)S—, —SC(═O)O—, —OC(═S)O—, —SC(═S)S—, —N(Rc)SO2—, —SO2N(Rc)—, —N(Rc)SO2N(Rd)—, —C(═O)N(Rc)N(Rd)—, —N(Rc)N(Rd)C(═O)—, —N(Rc)N(Rd)C(═O)O—, —OC(═O)N(Rc)N(Rd)—, —C(Rc)═N—NH—C(═O)—, —C(═O)NH—N═C(Rc)—, —C(Rc)═N—O—, —O—N═C(Rc)—,

OG Complex Work Unit Chemistry
Rc and Rd are independently selected at each occurrence from hydrogen, alkyl, heteroalkyl, cycloalkyl, and heterocyclyl.