DERIVADOS DE (2-TIENIL)-ALQUILAMINAS QUE TIENEN PROPIEDADES NEUROPROTECTORAS

• Main Authors: GRIFFITH, RONALD, CONRAD, SCHMIESING, RICHARD, JON, MURRAY, ROBERT, JOHN
• Format: Patent
• Language: Spanish
• Published: 16.08.1997
• Edition: 6
• 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 PRESENTAN COMPUESTOS DE LA FORMULA (I), EN DONDE: R1 REPRESENTA HIDROGENO O ALQUIL C1-C6, R2 REPRESENTA HIDROGENO, ALQUIL C1-C6, ALQUENIL C3-C6, ALQUNIL C3-C6 O CICLOALQUIL C3-C6, R3 REPRESENTA UNO O MAS RADICALES SELECCIONADOS ENTRE HIDROGENO, HIDROXIDO, ALQUIL C1-C6, ALCOXIDO C1-C6, HALOGENO, TRIFLUOROMETIL, AMINO, ALQUILAMINO C1-C6 O DI(ALQUIL C1-C6)AMINO, R4 REPRESENTA UNO O MAS RADICALES SELECCIONADOS ENTRE HIDROGENO O ALQUIL C1-C6, A REPRESENTA HIDROGENO, ALQUIL C1-C6, COC(R5R6)N(R7R8) O COOCALQUIL C1-C6, R5 REPRESENTA HIDROGENO, ALQUIL C1-C6, HIDROXIALQUIL C1-C2, MERCAPTOMETIL, (METILTIO)ALQUIL C1-C2, CARBOXIALQUIL C1-C2, 2-(ALCOXIDO C1C3)ETIL, (AMINOCARBONIL)ALQUIL C1-C2, AMINOALQUIL C1-C4, 3IMIDAZOLILMETIL, FENILMETIL O (4-HIDROXIFENIL)-METIL, O ADEMAS, R5 JUNTO CON EL NITROGENO ADYACENTE PUEDE REPRESENTAR UN ANILLO DE PIPERIDINA, PIRROLIDINA O UN ANILLO DE 2-PIRROLIDINONA, R6, R7 Y R8 REPRESENTAN INDEPENDIENTEMENTE HIDROGENO O ALQUIL C1-C6, O ADEMAS, R7 Y R8 TOMADAS JUNTO CON EL NITROGENO AL CUAL ESTAN UNIDAS PUEDEN REPRESENTAR UN ANILLO N-HETEROCICLICO C4-C5, ASIMISMO SE PRESENTAN LAS SALES DE ADICION ACIDA FARMACOLOGICAMENTE ACEPTABLES DE LOS COMPUESTOS, QUE SON UTILES COMO PRODUCTOS FARMACEUTICOS; EN PARTICULAR POSEEN PROPIEDADES BLOQUEADORES DEL N-METIL-(D)-ASPARTATO Y SON UTILES EN EL TRATAMIENTO Y/O PREVENCION DE ENFERMEDADES NEUROLOGICAS. Compounds of formula (I), in which: R1 represents hydrogen or C1-6 alkyl, R2 represents hydrogen, C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl or C3-6 cycloalkyl, R3 represents one or more radicals selected from hydrogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, halogen, trifluoromethyl, amino, C1-6 alkylamino or di(C1-6 alkyl)amino, R4 represents one or more radicals selected from hydrogen or C1-6 alkyl, A represents hydrogen, C1-6 alkyl, COC(R5R6)N(R7R8) or COOC1-6 alkyl, R5 represents hydrogen, C1-6 alkyl, hydroxy-C1-2 alkyl, mercaptomethyl, (methylthio)C1-2 alkyl, carboxy-C1-2 alkyl, 2-(C1-3 alkoxy)ethyl, (aminocarbonyl)C1-2 alkyl, amino-C1-4 alkyl, 3-imidazolylmethyl, phenylmethyl or (4-hydroxyphenyl)-methyl, or in addition, R5 together with the adjacent nitrogen may represent a piperidine, pyrrolidine or a 2-pyrrolidinone ring, R6, R7 and R8 independently represent hydrogen or C1-6 alkyl, or in addition, R7 and R8 taken together with the nitrogen to which they are attached may represent a C4-5 N heterocyclic ring, and pharmaceutically acceptable acid addition salts thereof, are useful as pharmaceuticals; in particular they possess N-methyl-(D)-aspartate blocking properties and are useful in the treatment and/or prevention of neurological disorders.