Chemically modified small molecules

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) C07C 43/11 (2006.01) C07D 489/08 (2006.01)

Patent

CA 2549730

The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water- soluble oligomer.

La présente invention concerne des médicaments à petites molécules chimiquement modifiées par fixation d'un oligomère soluble dans l'eau obtenu à partir d'une composition oligomère soluble dans l'eau monodispersée ou bimodale. Un conjugué de cette invention, lorsqu'il est administré via n'importe quelle voie d'administration, présente une vitesse de traversée de membrane biologique réduite comparée à la vitesse de traversée de la membrane biologique du médicament à petites molécules fixées à l'oligomère soluble dans l'eau.

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