C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 17/08 (2006.01) A61K 47/48 (2006.01) C08G 65/32 (2006.01)
Patent
CA 2191971
Biologically active conjugates are disclosed which are formed by reaction of a thiol moiety of a biologically active molecule with a non-peptidic polymer having an active sulfone moiety. Also disclosed are compounds having the formula R1-X-R2 wherein at least one of R1 and R2 is a biologically active molecule having a reactive thiol moiety which forms a covalent bond with X, a Michael acceptor-activated non-peptidic polymer. Further disclosed are methods of making the conjugates and compounds of the present invention as well as pharmaceutical compositions containing them. In addition, activated polymers suitable for attachment to a variety of molecules and surfaces are disclosed.
On décrit des conjugués biologiquement actifs qui sont formés par la réaction d'une fraction thiol d'une molécule biologiquement active avec un polymère non peptidique comportant une fraction sulfone active; des composés de formule R¿1?-X-R¿2?, dans laquelle R¿1? et/ou R¿2? représentent une molécule biologiquement active comportant une fraction thiol réactive qui forme une liaison covalente avec X, un polymère non peptidique activé par un accepteur de Michael; des procédés de préparation des conjugués et des composés de cette invention ainsi que des compositions pharmaceutiques contenant ces derniers; et des polymères activés pouvant se fixer sur diverses molécules et surfaces.
Harris Milton
Kachensky Dave
Kohno Tadahiko
Amgen Boulder Inc.
Amgen Inc.
Gowling Lafleur Henderson Llp
Shearwater Polymers Inc.
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