Multivalent platform molecules comprising high molecular...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01)

Patent

CA 2414076

Valency platform molecules comprising high molecular weight polyethylene oxide groups are provided, as well as conjugates thereof with biologically active molecules, and methods for their preparation. The high molecular weight polyethylene oxide group has, for example, a molecular weight of greater than 22,000 Daltons, for example at least 40,000 Daltons. In one embodiment, a composition comprising the valency platform molecules is provided, wherein the molecules have a polydispersity less than about 1.2. Conjugates of the valency platform molecule and a biologically active molecule, such as a saccharide, poly(saccharide), amino acid, poly(amino acid), nucleic acid or lipid also are provided. Also provided are pharmaceutically acceptable compositions comprising the conjugates disclosed herein and a pharmaceutically acceptable carrier, as well as methods of making and using the conjugates and compositions.

La présente invention concerne des molécules à plate-forme de valences renfermant des groupes poly(éthylène oxydes) de poids moléculaire élevé, ainsi que des conjugués de ces derniers avec des molécules biologiquement actives, et leurs procédés de préparation.Le groupe poly(éthylène oxyde) de poids moléculaire élevé possède, par exemple, un poids moléculaire supérieur à 22000 U.M.A., d'au moins 40000 U.M.A., par exemple. Dans un mode de réalisation, l'invention concerne une composition comprenant des molécules à plate-forme de valences présentant une polydiversité inférieure à 1,2 environ. L'invention concerne aussi des conjugués de la molécule à plate-forme de valences précitée et d'une molécule biologiquement active, telle qu'un saccharide, un polysaccharide, un acide aminé, un acide polyaminé, un acide nucléique ou un lipide. L'invention concerne enfin des compositions pharmaceutiquement acceptables comprenant les conjugués précités et un véhicule pharmaceutiquement acceptable, ainsi que des procédés de fabrication et d'utilisation des conjugués et compositions de l'invention.

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