APOLIPOPROTEIN-B SYNTHESIS INHIBITORS

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-...

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Main Authors ROBERT JOZEF MARIA HENDRICKX, LUC ALFONS LEO VAN DER EYCKEN, JAN HEERES, DE CHAFFOY DE COURCELLES, LEO JACOBUS JOZEF BACKX, DIDIER ROBERT GUY GABRIEL
Format Patent
LanguageEnglish
Spanish
Published 31.07.1997
Edition6
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
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Summary: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. La presente invencion provee compuestos novedosos de formula (I): (Ver Formula); los N-oxidos, las formas esteroquímicamente isoméricas de los mismos y la salácida de adicion farmacéuticamente aceptable de los mismos, en los que A y B tomados juntos forman un radical bivalente de formula: -N=CH- (a) -CH=N- (b), -CH2-CH2- (c), CH=CH- (d), -C(=0)-CH2- (e) Y -CH2-C(=0)- (f); R1 es hidrogeno, alquilo de C1-6 o halo; R2 es hidrogeno o halo; R2 es hidrogeno; alquilo de C1-8, cicloalquilo de C3-6 o alquilo de C1-8 sustituidos con hidroxi, oxo, cicloalquilo o arilo de C3-6; Hst es un anillo heterociclico opcionalmente substituido de cinco o seis miembros; se describe el uso como medicina, especialmente como un agente disminusor de lipidos, así como composiciones farmacéuticas y procedimientos para preparar compuestos y composiciones.
Bibliography:Application Number: MX19970003074