Valency platform molecules comprising aminooxy groups

Details Valency platform molecules comprising aminooxy groups Valency platform molecules comprising aminooxy groups

C - Chemistry, Metallurgy

07

C

C07C 271/16 (2006.01) A61K 47/48 (2006.01) C07C 271/20 (2006.01) C07C 323/57 (2006.01) C07C 323/60 (2006.01) C07D 295/185 (2006.01) C07D 295/20 (2006.01) C07D 295/205 (2006.01) C08G 65/329 (2006.01) C08G 65/333 (2006.01) C08G 83/00 (2006.01)

Patent

CA 2376057

Molecules comprising aminooxy groups are provided, wherein the aminooxy groups provide attachment sites for the covalent attachment of other molecules. In one embodiment, polyoxyethylene molecules comprising aminooxy groups are provided that can be conjugated to wide variety of biologically active molecules including poly(amino acids). In another embodiment, valency platform molecules comprising aminooxy groups are provided. The aminooxy groups can be used to form covalent bonds with biological molecules such as poly(amino acids). The aminooxy groups can, for example, react with poly(amino acids) modified to contain carbonyl groups, such as glyoxyl groups, to form a conjugate of the valency platform molecule and the biologically active molecule via an oxime bond. The valency platform molecules comprising aminooxy groups are advantageously reactive in the formation of conjugates, and they also can be readily synthesized to form a composition with very low polydispersity.

L'invention porte sur des molécules comportant des groupes amino-oxy qui constituent des sites de fixations covalentes d'autres molécules. Dans l'une des exécutions il s'agit de molécules de polyoxyéthylène, molécules comportant des groupes amino-oxy pouvant être conjugués à une grande variété de molécules bioactives dont des poly(acides aminés). Dans une autre exécution, il s'agit de molécules à plate-forme de valences comportant des groupes amino-oxy pouvant servir à former des liaisons covalentes avec des molécules biologiques telles que des poly(acides aminés). Les groupes amino-oxy peuvent par exemple réagir avec des poly(acides aminés), et notamment avec des poly(acides aminés) modifiés pour contenir des groupes carbonyle tels que des groupes glyoxyle pour former un conjugué de la molécule à plate-forme de valence et de la molécule biologiquement active via une liaison oxyme. Les molécules à plate-forme de valence comportant des groupes amino-oxy réagissent facilement pour former des conjugués et se synthétisent aisément pour former une composition à très faible polydispersité.

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