| 摘要 |
An antibody comprising a GlcNAc-S(A)x substituent is disclosed, wherein S(A)x is a sugar derivative comprising x functional groups A wherein A is independently selected from the group consisting of an azido group, a keto group and an alkynyl group and x is 1, 2, 3 or 4, wherein said GlcNAc-S(A)x substituent is bonded to the antibody via C1 of the N-acetylglucosamine of said GlcNAc-S(A)x substituent, and wherein said N-acetylglucosamine is optionally fucosylated. Also disclosed is an antibody-conjugate, in particular to an antibody-conjugate according to the Formula (20) or (20b), wherein AB is an antibody, S is a sugar or a sugar derivative, D is a molecule of interest, and wherein said N-acetylglucosamine is optionally fucosylated (b is 0 or 1).;;Also disclosed is a process for the preparation of a modified antibody, to a process for the preparation of an antibody-conjugate, and to said antibody-conjugate for use as a medicament. |
| 主权项 |
1. An antibody-conjugate according to the Formula (20) or (20b): wherein AB is an antibody, S is a sugar or a sugar derivative, GlcNAc is N-acetylglucosamine and Fuc is fucose; and wherein: b is 0 or 1; p is 0or 1; Q is —N(H)C(O)CH2— or —CH2—; x is 1, 2, 3 or 4; y is 1-20; L is a linker; D is a molecule of interest; r is 1-20; R1 is independently selected from the group consisting of hydrogen, halogen, —OR5, —NO2, —CN, —S(O)2R5, C1-C24 alkyl groups, C6-C24 (hetero)aryl groups, C7-C24 alkyl(hetero)aryl groups and C7-C24 (hetero)arylalkyl groups and wherein the alkyl groups, (hetero)aryl groups, alkyl(hetero)aryl groups and (hetero)arylalkyl groups are optionally substituted, wherein two substituents R1 may be linked together to form an annelated cycloalkyl or an annelated (hetero)arene substituent, and wherein R5 is independently selected from the group consisting of hydrogen, halogen, C1-C24 alkyl groups, C6-C24 (hetero)aryl groups, C7-C24 alkyl(hetero)aryl groups and C7-C24 (hetero)arylalkyl groups; X is C(R1)2, O, S or NR2, wherein R2 is R1 or L(D)r, and wherein L, D and r are as defined above; q is 0 or 1, with the proviso that if q is 0 then X is N-L(D)r; a is 0, 1, 2, 3, 4, 5, 6, 7or 8; a′ is 0, 1, 2, 3, 4, 5, 6, 7 or 8; and a+a′<10. |
