abstract |
Dihydrobenzodiazepine derivatives of formula (1) are described in which the dotted lines indicate the possible presence of a double bond; R1 represents (C1-18) optionally halogenated alkyl, (C1-18) optionally halogenated alkoxy, halogen, nitro, hydroxy or (C6-18) aryl (optionally substituted by (C1-10) optionally halogenated alkyl, (C1-12) possibly halogenated alkoxy, halogen, nitro or hydroxy); n represents 0, 1, 2, 3 or 4; R2 and R3 independently represent each other hydrogen; (C1-18) optionally halogenated alkyl; (C1-18) alkoxy; (C6-18) aryl; (C6-18) aryl- (C1-12) alkyl; heteroaryl; heteroaryl (C1-12) alkyl; (C6-18) aryloxy; (C6-18) aryl- (C1-12) alkoxy; heteroaryloxy; or heteroaryl (C1-12) alkoxy; in which the aryl and heteroaryl part of these radicals are optionally substituted by halogen, (C1-12) optionally halogenated alkoxy, (C1-12) optionally halogenated, nitro and hydroxy; R4 represents hydrogen, (C1-18) alkyl or (C6-18) aryl, said aryl group being eventually substituted by halogen, (C1-12) optionally halogenated alkoxy, (C1-12) optionally halogenated, nitro or hydroxy; X represents S, O or ûNT, where T represents a hydrogen atom, (C1-12) alkyl, (C6-18) aryl, (C6-18) aryl- (C1-12) alkyl or (C6-18) arylcarbonyl ; And R5, aryl, heteroaryl and heterocycle have the meanings indicated in the specification. A process for preparing these dihydrobenzodiazepine derivatives and the pharmaceutical compositions containing them is also described. Finally, the use of the compounds of formula (1) to prepare a medicament intended to prevent or treat dyslipidemias, arteriosclerosis, diabetes and its complications is described. These compounds are capable of decreasing the secretion of apo CIII. |