Tnp-470 polymer conjugates and use thereof

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61K 31/336 (2006.01) A61K 47/32 (2006.01) A61K 47/42 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2480666

The present invention relates to conjugates of water-soluble polymers and o~(chloracetyl-carbamoyl) fumagillol (TNP-470) and use of those conjugates as specific intracellular carriers of the TNP-470 into tumor vessels. The present invention further relates to use of those conjugates to lower the neurotoxicity of TNP-470. Preferably, the polymer has a molecular weight in the range of 100 Da to 800 kDa. More preferably, the polymer has a molecular weight no greater than 60 kDa. Most preferably, the polymer has a molecular weight in the range of 15 kDa to 40 kDa.

La présente invention concerne des conjugués de polymères solubles dans l'eau et de o-(chloracétyl-carbamoyl) fumagillol (TNP-470) et l'utilisation de ces conjugués sous forme de porteurs intracellulaires spécifiques de TNP-470 dans des vaisseaux de tumeur. Cette invention concerne aussi l'utilisation de ces conjugués en vue d'abaisser la neurotoxicité de TNP-470. Le polymère possède de préférence une masse moléculaire comprise entre 100 Da et 800 kDa. Dans un mode de réalisation plus préféré, le polymère possède une masse moléculaire inférieure ou égale à 60 kDa. Dans un mode de réalisation encore plus préféré, le polymère possède une masse moléculaire comprise entre 15 kDa et 40 kDa.

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