Novel triazolones as apolipoprotein-b synthesis inhibitors

Details Novel triazolones as apolipoprotein-b synthesis inhibitors Novel triazolones as apolipoprotein-b synthesis inhibitors

C - Chemistry, Metallurgy

07

D

C07D 405/14 (2006.01) A61K 31/495 (2006.01) C07D 405/06 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2217632

The present invention concerns novel compounds of formula (I), wherein R1 is C1-10alkyl, C3-7cycloalkyl or C1-6alkyl substituted with C3-7cycloalkyl; R2 is hydrogen or C1-6alkyl; Alk represents C1-3alkanediyl; -A- represents a bivalent radical of the formula: (a) -CH=CH-N=CH-, (b) -N=CH-N=CH-, (c) -CH=N- N=CH-, (d) -CH=CH-CH=N-; in said bivalent radicals a hydrogen atom may be replaced by C1-6alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C1-6alkyl or C1-6alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C1-6alkyl or C1-6alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof. The present invention further comprises the pharmaceutical compositions comprising compounds of formula (I), the preparation thereof as well as the use as a medicine in the treatment of hyperlipidemia.

La présente invention se rapporte à de nouveaux composés de formule (I), dans laquelle R?1¿ représente alkyle C¿1-10?, cycloalkyle C¿3-7? ou alkyle C¿1-6? substitué par cycloalkyle C¿3-7?; R?2¿ représente hydrogène ou alkyle C¿1-6?; Alk représente alcanediyle C¿1-3?; -A- représente un radical bivalent de formule: (a) -CH=CH-N=CH-, (b) -N=CH-N=CH, (c) -CH=N-N=CH-, (d) -CH=CH-CH=N-; dans lesdits radicaux bivalents, un atome d'hydrogène peut être remplacé par un alkyle C¿1-6?; et Ar représente phényle non substitué; phényle substitué par deux substituants au plus choisis parmi halo, alkyle C¿1-6? ou aklyloxy C¿1-6?; naphtyle non substitué; ou naphtyle substitué par deux substituants au plus choisi parmi halo, alkyle C¿1-6? ou alkyloxy C¿1-6?; leurs formes stéréochimiquement isomères ainsi que leurs sels d'addition d'acide pharmaceutiquement acceptables. La présente invention décrit également des compositions pharmaceutiques contenant les composés de formule (I), leur préparation ainsi que leur utilisation en tant que médicament dans le traitement de l'hyperlipidémie.

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