DERIVADOS HETEROCICLICOS INHIBIDORES DE LA ELASTASA LEUCOCITICA HUMANA (ELH)

• Main Authors: NASH KEVIN, TELAN LEILA, ROSENTRETER ULRICH, FITZGERALD MARY F, BARFACKER LARS, GIELEN HEIKE, SCHLEMMER KARL-HEINZ, ALLERHEILIGEN SWEN, ALBRECHT BARBARA, LI VOLKHART, KELDENICH JORG, MEURER DIRK
• Format: Patent
• Language: Spanish
• Published: 25.02.2005
• 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

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE A ES UN ANILLO ARILO O HETEROARILO; R1, R2 Y R3 SON CADA UNO H, HALOGENO, NITRO, ENTRE OTROS; R4 ES TRIFLUOROMETILCARBONILO, HIDROXICARBONILO, HETEROARILO, ENTRE OTROS; R5 ES ALQUILO C1-C4 SUSTITUIDO O NO, AMINO; R6 ES H, FORMILO, AMINOCARBONILO, ENTRE OTROS; R7 ES HALOGENO, CIANO, ALQUILO C1-C6, ENTRE OTROS; Y1, Y2, Y3, Y4 E Y5 SON CADA UNO CH, N, CUYOS ANILLOS PUEDEN CONTENER 0-2 ATOMOS DE N. SON COMPUESTOS PREFERIDOS: ETIL 4-(4-CIANOFENIL)-6-METIL-2-OXO-1-[3-(TRIFLUOROMETIL)FENIL]-1,2,3,4-TETRAHIDRO-5-PIRIMIDINCARBOXILATO; (1S)-2-METOXI-1-METIL 2-OXOETIL 4-(4-CIANOFENIL)-6-METIL-2-OXO-1-[3-(TRIFLUOROMETIL)FENIL]-1,2,3,4-TETRAHIDRO-5-PIRIMIDINCARBOXILATO Y ETIL 6-(BROMOMETIL)-4-(4-CIANOFENIL)-2-OXO-1-[3-(TRIFLUOROMETIL)FENIL]-1,2,3,4-TETRAHIDRO-5-PIRIMIDINCARBOXILATO. SE REFIERE TAMBIEN A UNA FORMULACION FARMACEUTICA UTIL EN EL TRATAMIENTO DE EPOC, SINDROME CORONARIO AGUDO, INSUFICIENCIA CARDIACA POR INIHIBICION DE LA ELASTASA NEUTROFILICA HUMANA (ENH) Compounds of formula (I) and salts, hydrates and/or solvates thereof and their tautomeric forms in which A is an aryl or heteroaryl ring, each of R , R and R are independently H or various substituents, R , R , R and R are various substituents and each of Y , Y Y , Y , and Y are independently CH or N so that the ring contains 0, 1 or 2 nitrogen atoms. In particular, A is a phenyl ring, each of Y -Y is CH and R is an alkoxycarbonyl residue. The compounds may be inhibitors of human leukocyte elastase (HLE, also known as human neutrophil elastase or HNE) and as such may be useful in the treatment of chronic obstructuive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.