Pharmaceutical composition comprising temozolomide ester

A - Human Necessities – 61 – K

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Details

A61K 31/4188 (2006.01) A61K 9/70 (2006.01) A61K 47/32 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2580910

The present invention discloses general formula I of Temozolomide-8-carboxylate compounds, the process for preparation, pharmaceutical compositions comprising the compounds and the use of the compounds and pharmaceutical compositions for the manufacture of an antitumor medicament. The said pharmaceutical composition comprises one or more general formula I Temozolomide-8-carboxylate compounds as active ingredient, together with conventional pharmaceutical carriers. The composition also comprises one or more pharmaceutically acceptable acidic material, optionally second or tertiary alcohol or ester or ether derivatives thereof. The said pharmaceutical composition can be made into various common formulations, particularly oral formulations as well as topically transdermal patches The present invention also discloses the application of the compounds and the compositions to treat tumor. (see formula I)

La présente invention expose des composés de Temozolomide-8-carboxylate de formule générale I, le procédé de préparation de ceux-ci, des compositions pharmaceutiques comprenant les composés et l'utilisation des composés et des compositions pharmaceutiques pour la fabrication d'un médicament anti-tumeur. Ladite composition pharmaceutique comprend un ou plusieurs composés de Temozolomide-8-carboxylate de formule générale I comme ingrédient actif, ainsi que des véhicules pharmaceutiques classiques. La composition comprend également une ou plusieurs substances acides acceptables du point de vue pharmaceutique, facultativement un alcool secondaire ou tertiaire ou des dérivés ester ou éther de ceux-ci. Ladite composition pharmaceutique peut être mise sous la forme de différentes formulations courantes, en particulier des formulations pour administration orale ainsi que des timbres transdermiques à application topique. La présente invention expose également l'application des composés et des compositions pour traiter une tumeur.

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