US 12,251,446 B2
Nucleic acid conjugate
Keiji Uehara, Tokyo (JP); Yasuhiro Suzuki, Tokyo (JP); Toshimasa Harumoto, Tokyo (JP); Hiroto Iwai, Tokyo (JP); and Asana Makino, Tokyo (JP)
Assigned to KYOWA KIRIN CO., LTD., Tokyo (JP)
Appl. No. 16/314,015
Filed by Kyowa Kirin Co., Ltd., Tokyo (JP)
PCT Filed Jun. 30, 2017, PCT No. PCT/JP2017/024268
§ 371(c)(1), (2) Date Dec. 28, 2018,
PCT Pub. No. WO2018/004004, PCT Pub. Date Jan. 4, 2018.
Claims priority of application No. 2016-131054 (JP), filed on Jun. 30, 2016.
Prior Publication US 2019/0192674 A1, Jun. 27, 2019
Int. Cl. A61K 47/00 (2006.01); A61K 9/00 (2006.01); A61K 31/7088 (2006.01); A61K 47/54 (2017.01); A61K 47/60 (2017.01); A61K 48/00 (2006.01); C07H 21/02 (2006.01); C12N 15/09 (2006.01); C12N 15/113 (2010.01)
CPC A61K 47/60 (2017.08) [A61K 9/0019 (2013.01); A61K 31/7088 (2013.01); A61K 47/54 (2017.08); A61K 48/00 (2013.01); C07H 21/02 (2013.01); C12N 15/09 (2013.01); C12N 15/113 (2013.01)] 12 Claims
 
1. A nucleic acid conjugate in which a sugar chain ligand is bonded to an siRNA or an antisense oligonucleotide (ASO) via a linker, wherein the sugar chain ligand has the following structure:

OG Complex Work Unit Chemistry
wherein
R1 and R2 are 4-hydroxybenzyl,
Y1 and Y2 are each NR3, and
R3 is a hydrogen atom.