Pharmaceuticals in joint-linker configurations for treating pathological blood clots

摘要

The present disclosure provides various molecular constructs having a targeting element and an effector element. Methods for treating various diseases using such molecular constructs are also disclosed.

主权项

1. A molecular construct comprising a first linker unit and a second linker unit, wherein,
the first linker unit comprises,
a first center core comprising a plurality of amine groups,a first linking arm linked to the first center core,a first element linked to the first linking arm, andoptionally, a first coupling arm linked to the first center core; the second linker unit comprises,
a second center core comprising a plurality of amine groups,a second linking arm linked to the second center core,a second element linked to the second linking arm, andoptionally, a second coupling arm linked to the second center core; and the first and second linker units are coupled to each other via copper catalyzed azide-alkyne cycloaddition (CuAAC) reaction, strained-promoted azide-alkyne click chemistry (SPAAC) reaction or inverse electron demand Diels-Alder (iEDDA) reaction occurred between any of the followings: the first and second center cores, the first coupling arm and the second center core, the first and second coupling arms, or the first center core and the second coupling arm; wherein,
the first element is an scFv specific for fibrin, and the second element is a tissue plasminogen activator or an inhibitor of Factor Xa or thrombin.