Water-soluble polymer conjugates of retinoic acid

Details Water-soluble polymer conjugates of retinoic acid Water-soluble polymer conjugates of retinoic acid

A - Human Necessities

61

K

A61K 47/48 (2006.01) A61K 9/00 (2006.01) A61K 9/16 (2006.01) A61K 31/07 (2006.01) A61P 11/00 (2006.01)

Patent

CA 2464346

The present invention provides water-soluble polymer conjugates of retinoic acid. The conjugates of the invention are prepared by covalent attachment of a water-soluble and non-peptidic polymer such as polyethylene glycol to a retinoid such as retinoic acid. The polymer portion of the conjugate may be linear (i.e., prepared using an end-capped or methoxy PEG or a linear bifunctional PEG), branched or forked. The conjugates of the invention are water soluble, and are, in particular, useful for inhalation therapy of conditions of the respiratory tract responsive to retinoid therapy.

L'invention concerne des conjugués polymères hydrosolubles d'acide rétinoïque, qui sont préparés par fixation covalente d'un polymère hydrosoluble et non peptidique tel qu'un polyéthylène glycol à un rétinoïde, par exemple de l'acide rétinoïque. La partie polymère du conjugué peut être linéaire (c'est-à-dire préparée au moyen d'un PEG coiffé aux extrémités ou méthoxy PEG ou un PEG bifonctionnel linéaire), ramifiée ou bifurquée. Ces conjugués, qui sont hydrosolubles, servent notamment en inhalothérapie d'états des voies respiratoires réagissant à un traitement par rétinoïdes.

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