Multibinding inhibitors of topoisomerase

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/00 (2006.01) A61K 38/00 (2006.01) A61K 39/00 (2006.01) A61K 39/395 (2006.01) A61K 39/44 (2006.01) A61K 47/48 (2006.01) A61K 51/00 (2006.01) C07C 233/36 (2006.01) C07C 233/78 (2006.01) C07C 237/24 (2006.01) C07C 271/20 (2006.01) C07C 335/08 (2006.01) C07C 335/32 (2006.01) C07D 207/333 (2006.01) C07D 211/58 (2006.01) C07D 215/56 (2006.01) C07D 233/90 (2006.01) C07D 235/30 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 405/04 (2006.01) C07D 413/14 (2006.01) C07D 471/04

Patent

CA 2321166

Disclosed are multibinding compounds which inhibit topoisomerases which are essential enzymes in higher encaryotes for DNA replication and repair. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligant is capable of binding to a topoisomerase and the distance between ligands is between about 2-50 .ANG.. The multibinding compounds of this invention are useful in the treatment and prevention of cancer, microbial infections and the like.

L'invention concerne des composés à liaisons multiples inhibant des topoisomérases qui sont des enzymes essentielles dans des eucaryotes supérieurs de réplication et de réparation d'ADN. Les composés à liaisons multiples de la présente invention contiennent 2 à 10 ligands à fixation covalente à une ou plusieurs séquences de liaison. Chaque ligand est capable de se lier à une topoisomérase et la distance entre ligands est comprise entre 2 et 50 .ANG.. Les composés à liaisons multiples de la présente invention s'utilisent pour le traitement et la prévention du cancer, d'infections microbiennes et analogues.

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