Dual phase drug release system

Details Dual phase drug release system Dual phase drug release system

A - Human Necessities

61

K

A61K 47/48 (2006.01)

Patent

CA 2537993

The present invention relates to conjugate comprising a carrier substituted with one or more occurrences of a moiety having the structure (I): wherein each occurrence of M is independently a modifier having a molecular weight <= 10 kDa; denotes direct of indirect attachment of M to linker LM; and each occurrence of LM is independently an optionally substituted succinamide- containing linker, whereby the modifier M is directly or indirectly attached to the succinamide linker through an amide bond, and the carrier is linked directly or indirectly to each occurrence of the succinamide linker through an ester bond. In another aspect, the invention provides compositions comprising the conjugates, methods for their preparation, and methods of use thereof in the treatment of various disorder, including, but not limited to cancer.

L'invention porte sur des conjugués comprenant un support substitué par un ou plusieurs fragments de structure (I) dans laquelle: chacun des M est indépendamment un modificateur de poids moléculaire = 10 kDa; indique une liaison directe ou indirecte de M avec le liant L?M¿; et chaque L?M¿ est indépendamment un liant facultativement substitué contenant de la succinamide. Par ailleurs, un modificateur M est directement ou indirectement fixé au liant de succinamide par une liaison amide, et le support est directement ou indirectement fixé à chacun des M par une liaison ester. L'invention porte en outre: sur des compositions contenant lesdits conjugués, sur leur procédé de préparation, et sur leurs méthodes d'utilisation pour le traitement de divers maux dont, non exclusivement, le cancer.

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