发明名称 Sulfamide linker, conjugates thereof, and methods of preparation
摘要 The present invention relates to a compound comprising an alpha-end and an omega-end, the compound comprising on the alpha-end a reactive group Q1 capable of reacting with a functional group F1 present on a biomolecule and on the omega-end a target molecule, the compound further comprising a group according to formula (1) or a salt thereof:;;Said compound may also be referred to as a linker-conjugate. The invention also relates to a process for the preparation of a bioconjugate, the process comprising the step of reacting a reactive group Q1 of a linker-conjugate according to the invention with a functional group F1 of a biomolecule. The invention further relates to a bioconjugate obtainable by the process according to the invention.
申请公布号 US9636421(B2) 申请公布日期 2017.05.02
申请号 US201615360610 申请日期 2016.11.23
申请人 Synaffix B.V. 发明人 Verkade Jorge Merijn Mathieu;Wijdeven Maria Antonia;Van de Sande Petrus Josephus Jacobus Maria;Van Berkel Sander Sebastiaan;Van Delft Floris Louis
分类号 A61K31/18;A61K31/175;C07K1/13;C07K1/04;A61K47/48;C07K16/32 主分类号 A61K31/18
代理机构 Foley & Lardner LLP 代理人 Foley & Lardner LLP ;Talapatra Sunit
主权项 1. A process for the preparation of a bioconjugate, the process comprising the step of reacting a reactive group Q1 of a linker-conjugate with a functional group F1 of a glycoprotein (B) under condition such that the reactive group Q1 is reacted with the functional group F1 of the glycoprotein to covalently link the glycoprotein to the linker-conjugate, wherein the linker-conjugate is a compound comprising a group according to formula (1)  covalently linked to an alpha-end at one side of the formula (1) and an omega-end at the other side of the formula (1), the alpha-end comprising the reactive group Q1 capable of reacting with the functional group F1 present on the glycoprotein (B) and the omega-end comprising a target molecule (D) selected from the group consisting of an active substance, a reporter molecule, a polymer, a solid surface, a hydrogel, a nanoparticle, a microparticle and a biomolecule, wherein: the wavy lines indicate covalent linkages to the alpha end and the omega end, a is 0 or 1; and R1 is selected from the group consisting of hydrogen, C1-C24 alkyl groups, C3-C24 cycloalkyl groups, C2-C24 (hetero)aryl groups, C3-C24 alkyl(hetero)aryl groups and C3-C24 (hetero)arylalkyl groups, the C1-C24 alkyl groups, C3-C24 cycloalkyl groups, C2-C24 (hetero)aryl groups, C3-C24 alkyl(hetero)aryl groups and C3-C24 (hetero)arylalkyl groups optionally substituted and optionally interrupted by one or more heteroatoms selected from O, S and NR3 wherein R3 is independently selected from the group consisting of hydrogen and C1-C4 alkyl groups, or R1 is a second target molecule D, wherein the second target molecule is optionally connected to N via a spacer moiety; and wherein Q1 is a (hetero)cyclooctynyl group or a bicycle[6.1.0]non-4-yn-9yl] group, and F1 is an azide group.
地址 Oss NL