申请人:Genentech, Inc.
公开号:US10729738B2
公开(公告)日:2020-08-04
The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.
本发明一般涉及二硫化物药物共轭物,其中由至少一个烃基或取代烃基取代的含硫碳原子组成的连接体通过二硫键与靶向载体的半胱氨酸硫原子共轭,并且连接体进一步与药物分子共轭。 本发明进一步涉及适合通过二硫键与靶向载体共轭的活化连接体-药物共轭物。 本发明进一步涉及制备受阻二硫化物药物共轭物的方法。