[EN] IMMUNOCONJUGATE SYNTHESIS METHOD<br/>[FR] PROCÉDÉ DE SYNTHÈSE D'IMMUNOCONJUGUÉ
申请人:BOLT BIOTHERAPEUTICS INC
公开号:WO2021046347A1
公开(公告)日:2021-03-11
The invention provides a method for producing an immunoconjugate, the method comprising combining one or more compounds of Formula I and an antibody construct of Formula II to provide the immunoconjugate of Formula III, wherein TA is a therapeutic agent, L is a linker, r is an integer from 1 to 50, Ar is an aromatic moiety comprising a substituent selected from PEG, ‑SO2CX3, ‑NR3 +, ‑NO2, ‑SO3R, ‑SO2R, ‑CN, ‑CX3, ‑PO3R2, ‑OPO3R2,, and salts thereof, each R independently is H, CX3, or C1-C4 alkyl, each X independently is hydrogen or a halogen, Y is CH2, PEG, or a bond, n is an integer from 1 to 4, and PEG has the formula: –(CH2CH2O)m–(CH2)p–, where p is an integer from 1 to 5 and m is an integer from 2 to 50. The invention also provides an immunconjugate and a composition of immunoconjugates formed from said method.