Cyclic prodrugs of peptides and peptide nucleic acids having...

Details Cyclic prodrugs of peptides and peptide nucleic acids having... Cyclic prodrugs of peptides and peptide nucleic acids having...

C - Chemistry, Metallurgy

07

K

C07K 14/435 (2006.01) A61K 38/04 (2006.01) A61K 38/16 (2006.01) C07K 1/107 (2006.01) C07K 1/113 (2006.01) C07K 5/04 (2006.01) C07K 5/107 (2006.01) C07K 7/04 (2006.01) C07K 7/06 (2006.01) C07K 14/665 (2006.01) C07K 14/70 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2219151

Provided are cyclic prodrugs of biologically active peptides and peptide nucleic acids exhibiting improved cell membrane permeability and enzymatic stability, containing 3-(2'-hydroxy-4',6'-dimethyl phenyl)-3,3-dimethyl propionic acid and its derivatives and acyloxyalkoxy linkers. Also provided are pharmaceutical compositions containing effective amounts of these cyclic prodrugs in combination with pharmaceutically acceptable carriers, excipients, or diluents.

La présente invention concerne des bioprécurseurs cycliques de peptides biologiquement actifs et d'acides nucléiques peptides faisant preuve d'une meilleure perméabilité de la membrane cellulaire. De tel bioprécurseurs, qui contiennent de l'acide propionique de 3-(2'-hydroxy-4',6'-diméthyl phényl)-3,3-diméthyle et ses dérivés, contiennent également des liants de type acyloxyalcoxy. L'invention concerne également des compositions pharmaceutiques contenant des quantités suffisantes de ces bioprécurseurs, combinés avec des vecteurs, des excipients ou des diluants admis en pharmacie.

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