Antibody-drug conjugates
AssigneeCho Pharma, Inc.
InventorsNan-Horng Lin, Charng-Sheng Tsai, Ting-Chun Hung, Hong-Yang Chuang
Life of this patent
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Abstract
An antibody-drug conjugate (ADC) has a structure represented by Formula (I): a pharmaceutically acceptable salt thereof wherein Ab is an antibody without glycans (i.e., the protein portion an antibody); G1 and G2 are glycan moieties, which may be the same or different; Cn1 and Cn2 are conjugation moieties, which may be the same or different; L1 and L2 are linker moieties, which may be the same or different; D1 and D2; are drug units which may be the same or different; and x and y are independently an integer from 0 to 8, provided that x+y≠0.
Claims11
An antibody-drug conjugate (ADC) comprising a structure represented by Formula (I):
- [D2-L2-Cn2yG2-Ab-G1Cn1-L1-D1]x Formula (I)
- or a pharmaceutically acceptable salt thereof, wherein
- Ab is an antibody without glycans;
- G1 and G2 are each a glycan moiety;
- Cn1 and Cn2 are each a conjugation moiety;
- L1 and L2 are each a linker moiety;
- D1 and D2 are each a drug unit which may be the same or different;
- and
- x and y are independently an integer from 0 to 1, provided that x+y≠0,
- wherein the glycan moiety has a structure shown as,
- Formula (II-2b):
- wherein
- [Ab] indicates an attachment site for the antibody;
- and
- [Cn] indicates an attachment site for the conjugation moiety;
- wherein the conjugation moiety has a structure of Formula (III-1):
- wherein
- Q is a Y1+Y2 spacer, wherein Y1 and Y2 are independently selected from the group consisting of a direct bond, —(CH2)n—, —O—, —NH—, —C(O)—, —C(O)NH—, —NHC(O)—, —(CH2)nO—, —O(CH2)n—, —(CH2)n—C(O)—, —C(O)(CH2)n—, —(CH2)n—NH—, —NH—(CH2)n—, —(CH2)n—NHC(O)—, —C(O)(CH2)n—NHC(O)—, (CH2)nSCH2C(O)—, and —(CH2CH2O)m—;
- n is an integer from 1 to 8, inclusive;
- m is an integer from 1 to 4, inclusive;
- [G] indicates an attachment site for the glycan moiety;
- and
- [L] indicated an attachment site for the linker moiety;
- wherein the linker moiety has the structure of Formula (IV-1) or Formula (IV-2):
- wherein
- [Cn] indicates an attachment site for the conjugation moiety;
- [D] indicates an attachment site for the drug unit;
- and
- n is an integer from 0 to 6, inclusive.
Dependencies are inferred from the claim text.