A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 47/48 (2006.01) A61K 31/704 (2006.01) A61K 49/00 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) G01N 33/52 (2006.01)
Patent
CA 2203622
The compound (W-Z-M) according to the invention comprises a component (M) chosen from the group consisting of markers and therapeutic agents possessing an intracellular active site (A.S.), linked to a ligand (W--Z) comprising an arm (Z) linked to a terminal group (W), characterized in that the linkage between the arm (Z) of the ligand (W-Z) and the component (M) prevents intracellular entry of the compound (W-Z-M) and/or inhibits expression of the marker (M), in that said linkage can be selectively cleaved by factors secreted by target cells so as to permit expression of the marker (M) or entry of the therapeutic agent (M) into said target cells, and in that the terminal group (W) provides for the stability of the compound (W-Z-M) in the serum and the circulating blood.
Le composé (W-Z-M) selon l'invention comprend un élément (M) choisi parmi le groupe constitué par les marqueurs et les agents thérapeutiques possédant un site actif intracellulaire (S.A.), lié à un ligand (W-Z), comprenant un bras (Z) lié à un groupement terminal (W), caractérisé en ce que la liaison entre le bras (Z) du ligand (W-Z) et l'élément (M) empêche la pénétration intracellulaire du composé (W-Z-M) et/ou inhibe l'expression du marqueur (M), en ce que ladite liaison est clivable sélectivement par des facteurs sécrétés par des cellules cibles de manière à permettre l'expression du marqueur (M) ou la pénétration de l'agent thérapeutique (M) dans lesdites cellules cibles, et en que le groupement terminal (W) assure la stabilité du composé (W-Z-M) dans le sérum et le sang circulant.
Baurain Roger
Trouet Andre
Gowling Lafleur Henderson Llp
La Region Wallonne
Universite Catholique de Louvain
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