TRIAZOLONAS COMO INHIBIDORES DE LA SINTESIS DE APOLIPOPROTEINA-B

• Main Authors: BACKX, LEO, JACOBUS, JOZEF, HEERES, JAN, DE CHAFFOY DE COURCELLES, DIDIER, ROBERT, GUY, G, LUYTS, PAUL, AUGUST, CLEMENT
• Format: Patent
• Language: Spanish
• Published: 16.05.2002
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

LA PRESENTE INVENCION SE REFIERE A NUEVOS COMPUESTOS DE FORMULA (I), DONDE R1 ES ALQUILO C1-10 , CICLOALQUILO C37 O ALQUILO C1-6 SUSTITUIDO CON CICLOALQUILO C3-7 ; R2 ES HIDROGENO O ALQUILO C1-6 ; ALK REPRESENTA ALCANODIILO C1-3 ; -A- REPRESENTA UN RADICAL DIVALENTE DE FORMULA: (A) - CH = CH - N = CH -, (B) - N = CH - N = CH -, (C) CH = N - N = CH -, (D) - CH = CH - CH = N -; EN DICHOS RADICALES DIVALENTES, UN ATOMO DE HIDROGENO PUEDE SER REEMPLAZADO POR UN ALQUILO C1-6 ; Y AR ES UN FENILO NO SUSTITU IDO; FENILO SUSTITUIDO CON HASTA DOS SUSTITUYENTES SELECCIONADOS DE ENTRE HALO, ALQUILO C1-6 O ALQUILOXI C1-6 ; N AFTILO NO SUSTITUIDO O NAFTILO SUSTITUIDO CON HASTA DOS SUSTITUYENTES SELECCIONADOS DE ENTRE HALO, ALQUILO C1-6 O ALQUILOXI C1-6 ; SUS FORMAS ISOMEROS ESTEREOQUIMICOS, Y SUS SALES DE ADICION DE ACIDO FARMACEUTICAMENTE ACEPTABLES. LA PRESENTE INVENCION SE REFIERE ADEMAS A LAS COMPOSICIONES FARMACEUTICAS QUE INCLUYEN COMPUESTOS DE FORMULA (I), SU PREPARACION ASI COMO SU USO COMO MEDICAMENTOS EN EL TRATAMIENTO DE LA HIPERLIPIDEMIA. 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 formula -CH=CH-N=CH- (a), -N=CH-N=CH- (b), -CH=N-N=CH- (c), -CH=CH-CH=N- (d); 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.