US 11,920,136 B2
Transglutaminase-mediated conjugation
Jaume Pons, San Francisco, CA (US); Hong I. Wan, Foster City, CA (US); Tracy Chia-Chien Kuo, San Mateo, CA (US); Curt W. Bradshaw, San Francisco, CA (US); Son Lam, San Francisco, CA (US); Bang Janet Sim, Brisbane, CA (US); Edward HyungSuk Ha, Cambridge, MA (US); and Sukumar Sakamuri, San Diego, CA (US)
Assigned to TALLAC THERAPEUTICS, INC., Burlingame, CA (US)
Filed by Tallac Therapeutics, Inc., Burlingame, CA (US)
Filed on Feb. 26, 2021, as Appl. No. 17/187,579.
Claims priority of provisional application 63/110,854, filed on Nov. 6, 2020.
Claims priority of provisional application 62/983,463, filed on Feb. 28, 2020.
Prior Publication US 2022/0380768 A1, Dec. 1, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. C12N 15/117 (2010.01); A61K 47/68 (2017.01); A61P 35/00 (2006.01); C07K 16/28 (2006.01); C07K 16/30 (2006.01); C07K 16/32 (2006.01); C07K 19/00 (2006.01)
CPC C12N 15/117 (2013.01) [A61K 47/6807 (2017.08); A61K 47/6811 (2017.08); A61K 47/6849 (2017.08); A61K 47/6851 (2017.08); A61K 47/6889 (2017.08); A61P 35/00 (2018.01); C07K 16/2803 (2013.01); C07K 16/30 (2013.01); C07K 16/32 (2013.01); C07K 19/00 (2013.01); C07K 2317/52 (2013.01); C07K 2317/56 (2013.01); C07K 2317/565 (2013.01); C07K 2317/71 (2013.01); C12N 2310/17 (2013.01); C12N 2310/313 (2013.01); C12N 2310/315 (2013.01); C12N 2310/3513 (2013.01)] 47 Claims
 
1. An immunomodulating oligonucleotide of Formula (C):

OG Complex Work Unit Chemistry

OG Complex Work Unit Chemistry

OG Complex Work Unit Chemistry
wherein
custom character* and custom character** indicate the points of attachment within the oligonucleotide;
each T1 is independently O or S;
each T2 is S−;
T3 is a group

OG Complex Work Unit Chemistry
 wherein custom character indicates the point of attachment to the rest of the oligonucleotide;
Z is O or S;
U5′ is —H or halogen;
R5′ is —H or methoxy;
Rc1 is —H or methoxy;
Rg1, Rg2, Rg3, and V are H;
R3′ is methoxy;
R1 is —(CH2)3—OH;
R2 is —H or methyl; and
n is an integer from 0 to 2,
or a pharmaceutically acceptable salt thereof.