C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 475/08 (2006.01) A61K 31/519 (2006.01)
Patent
CA 2675246
This invention is in the field of chemical restructuring of antimetabolite agents known to have poor oral bioavailability and to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concerns orotate derivatives of the methotrexate and trimetrexate, that are found to improve the oral bioavailability and clearance compared with their respective forms- methotrexate and trimetrexate, currently in use. The present invention provides methotrexate orotate having the formula:
Cette invention concerne le domaine de la restructuration chimique d'agents d'antimétabolites connus pour avoir une faible biodisponibilité orale et pour provoquer une toxicité de tissu en tant qu'effet secondaire, en produisant leurs dérivés d'orotate. Plus particulièrement, l'invention concerne des dérivés d'orotate du méthotrexate et du trimétrexatequi s'avèrent améliorer la biodisponibilité et la clairance orales par comparaison à leurs formes respectives (méthotrexate et trimétrexate), actuellement utilisées. La présente invention propose un orotate de méthotrexate ayant la formule.
Gowling Lafleur Henderson Llp
Savvipharm Inc
LandOfFree
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