Apolipoprotein-b synthesis inhibitors

Details Apolipoprotein-b synthesis inhibitors Apolipoprotein-b synthesis inhibitors

C - Chemistry, Metallurgy

07

D

C07D 405/14 (2006.01) A61K 31/495 (2006.01) C07D 405/12 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2203274

The present invention provides novel compounds of formula (I), the N-oxides, the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula: -N=CH- (a), -CH=N- (b), -CH2-CH2- (c), -CH=CH- (d), -C(=O)-CH2- (e), -CH2-C(=O)- (f); R1 is hydrogen, C1-6alkyl, or halo; R2 is hydrogen or halo; R3 is hydrogen; C1-8alkyl; C3-6cycloalkyl or C1-8 alkyl substituted with hydroxy, oxo, C3-6cycloalkyl or aryl. Het is five- or six membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.

L'invention concerne les nouveaux composés de la formule (I), leurs N-oxydes, leurs formes stéréoisomères et leurs sels d'addition acides compatibles sur le plan pharmaceutique, dans laquelle A et B constituent ensemble un radical bivalent de la formule suivante: -N=CH- (a), -CH=N- (b), -CH¿2?-CH¿2?- (c), -CH=CH- (d), -C(=O)-CH¿2?- (e), -CH¿2?-C(=O)- (f); R?1¿ est de l'hydrogène, du C¿1-6? alkyle, ou du halo; R?2¿ de l'hydrogène ou du halo; R?3¿ de l'hydrogène; du C¿1-8? alkyle; du C¿3-6? cycloalkyle ou du C¿1-8? alkyle substitué par de l'hydroxy, de l'oxo, du C¿3-6? cycloalkyle ou de l'aryle. Het est un noyau hétérocyclique éventuellement substitué à 5 ou 6 chaînons. L'invention se rapporte à l'emploi de ces composés en médecine, en particulier en tant qu'hypolipémiants, ainsi qu'à des compositions et des procédés pharmaceutiques destinés à la préparation des composés et des compositions.

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