Derivatives comprising sterols and/or stanols and specific...

C - Chemistry – Metallurgy – 07 – J

Patent

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Details

C07J 43/00 (2006.01) A61K 31/575 (2006.01) A61P 9/10 (2006.01) C07J 9/00 (2006.01)

Patent

CA 2499817

The present invention provides, in one aspect, novel derivatives comprising sterols and/or stanols and an NSAID selected from salicylic acids and arylalkanoic acids, including salts of these derivatives, and having one or more of the following formulae: a) R2-(CH2)n-CO-OR b) R2-R c) R2-CO-CO-OR d) formula (I), wherein R is a sterol or stanol moiety, R2 is derived from a salicylic acid or an arylalkanoic acid and n=1-5. Also provided are pharmaceutical compositions comprising one or more of these novel derivatives and methods of treating or preventing cardiovascular disease and its underlying conditions including, without limitation, atherosclerosis, hypercholesterolemia, hyperlipidemia, hypertension, thrombosis, coronary artery disease, and for treating and reducing inflammation including coronary plaque inflammation, bacterial-induced inflammation, viral induced inflammation and inflammation associated with acute pain and surgical procedures which comprises administering to an animal, particularly a human, a non-toxic and therapeutically effective amount of one or more of these compounds or a biologically acceptable salt thereof.

La présente invention concerne, dans un aspect, de nouveaux dérivés, qui contiennent des stérols et/ou des stanols, ainsi qu'un AINS sélectionné dans le groupe constitué par des acides salicyliques et des acides arylalcanoïques, y compris des sels desdits dérivés; et présentent une ou plusieurs des formules suivantes: a) R¿2?-(CH¿2?)¿n?-CO-OR; b) R¿2?-R; c) R¿2?-CO-CO-OR; d) la formule (I), dans lesquelles R est un fragment de stérol ou de stanol; R¿2? est dérivé de l'acide salicylique ou de l'acide arylalcanoïque; et n=1-5. L'invention concerne également des compositions pharmaceutiques contenant un ou plusieurs de ces nouveaux dérivés; des méthodes de traitement ou de prévention de maladies cardiovasculaires ou de leurs affections sous-jacentes, y compris, mais pas exclusivement, l'athérosclérose, l'hypercholestérolémie, l'hyperlipidémie, l'hypertension, la thrombose, la coronaropathie; ou des méthodes de traitement et de réduction des inflammations, y compris l'inflammation des plaques coronaires, l'inflammation d'origine bactérienne, l'inflammation d'origine virale ou l'inflammation associée à la douleur aiguë ou à des interventions chirurgicales. Ces méthodes consistent à administrer à un animal, en particulier un être humain, une quantité non toxique, thérapeutiquement efficace d'un ou de plusieurs de ces composés, ou un sel biologiquement acceptable de ces composés.

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