Patent ID: 11958878
Assignee: DAIICHI SANKYO COMPANY, LIMITED
Field: Pharmaceuticals (Chemistry)
Classification: CPC A  C | IPC C

Claim 0:
1. A conjugate of an oligonucleotide and a GalNAc unit or a pharmacologically acceptable salt or solvate thereof, wherein the conjugate is selected from:
5′-Am1s-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Am1s-Te2s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1t-H-3′ (SEQ ID NO: 40) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 40,
5′-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Am1s-Te2s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1s-Ce2t—H-3′ (SEQ ID NO: 171) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 171,
5′-Um1s—Cm1s-Ce2s-Gm1s-Am1s-Te2s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1s-Ce2s—Um1t—H-3′ (SEQ ID NO: 172) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 172,
5′-Am1s-Am1s-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Am1s-Te2s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1t-H-3′ (SEQ ID NO: 42) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 42,
5′-Am1s-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Am1s-Te2s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1s-Ce2t—H-3′ (SEQ ID NO: 47) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 47,
5′-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Am1s-Te2s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1s-Ce2s—Um1t—H-3′ (SEQ ID NO: 48) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 48,
5′-Am1s-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1t-H-3′ (SEQ ID NO: 173) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 173,
5′-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1s-Ce2t—H-3′ (SEQ ID NO: 174) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 174,
5′-Um1s—Cm1s-Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1s-Ce2s—Um1t—H-3′ (SEQ ID NO: 175) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 175,
5′-Am1s-Am1s-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1t-H-3′ (SEQ ID NO: 176) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 176,
5′-Am1s-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1s-Ce2t—H-3′ (SEQ ID NO: 177) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 177,
5′-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1s-Ce2s—Um1t—H-3′ (SEQ ID NO: 178) and X18, wherein the X18 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 178,
5′-Am1s-Ae2s-Um1s—Cm1s—Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1t-H-3′ (SEQ ID NO: 173) and X20, wherein the X20 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 173,
5′-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1s-Ce2t—H-3′ (SEQ ID NO: 174) and X20, wherein the X20 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 174,
5′-Am1s-Am1s-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1t-H-3′ (SEQ ID NO: 176) and X20, wherein the X20 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 176, and
5′-Am1s-Ae2s-Um1s—Cm1s-Ce2s-Gm1s-Ae2s-Um1s-Gm1s-Gm1s-Ce2s-Gm1s-Am1s-Ae2s-Gm1sCe2t—H-3′ (SEQ ID NO: 177) and X20, wherein the X20 is a GalNAc unit attached to the 5′ end of SEQ ID NO: 177,
wherein Gm1t, Um1t, Am1s, Gm1s, Cm1s, Um1s, Ce2t, Ae2s, Ce2s, Te2s, X18 and X20 are defined as follows:, wherein the atomic bonding to phosphate group in X18 and X20 comprises formation of a phosphodiester bond by binding to the carbon atom at the 5′ end of the oligonucleotide.