DERIVADOS DEL ACIDO HIDROXI-PIPECOLATO HIDROXAMICO

• Main Authors: CHUPAK LOUIS STANLEY, LETAVIC MICHAEL ANTHONY, NOE MARK CARL, MCCLURE KIM FRANCIS
• Format: Patent
• Language: Spanish
• Published: 27.09.2000
• 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 DERIVADOS DEL ACIDO HIDROXI-PIPECOLATO HIDROXAMICO DE FORMULA I, DONDE R1-R8 SON OH, H, HALOGENO, CN, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; O R1 Y R2 O R3 Y R4 O R5 Y R6 FORMAN JUNTOS UN CARBONILO; R1 Y R2 O R3 Y R4 O R5 Y R6 O R7 Y R8 FORMAN JUNTOS UN CICLOALQUILO C3-C6, OXACICLOHEXILO, TIOCICLOHEXILO, INDANILO, TETRALINILO, GRUPO a; Ar ES (ARIL C6-C10)(ALCOXI C1-C6)(ARILO C6-C10), (HETEROARIL C2-C9)METOXI(ARILO C6), (HETEROARIL C2-C9)METOXI(HETEROARILO C2-C9), ENTRE OTROS; CON LA CONDICION: QUE UNO DE R1-R8 ES OH; LOS COMPUESTOS I NO SON HIDROXIAMIDA DEL ACIDO (2R,4S)-14-(4-FLUOROBENCILOXI)-BENCENOSULFONIL]-4-HIDROXI-PIPERIDINA-2-CARBOXILICO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS HIDROXIAMIDA DEL ACIDO (2R,5R)-1-[4-(2,5-DIMETIL-BENCILOXI)-BENCENOSULFONIL]-5-HIDROXI-PIPERIDINA-2-CARBOXILICO, HIDROXIAMIDA DEL ACIDO (2R,5R)-1-[4-(5-FLUORO-2-METIL-BENCILOXI)-BENCENOSULFONIL]-5-HIDROXI-PIPERIDINA-2-CARBOXILICO, HIDROXIAMIDA DEL ACIDO (2R,4R)-4-HIDROXI-1-[4-(2-METIL-BENCILOXI)-BENCENOSULFONIL]-PIPERIDINA-2-CARBOXILICO, ENTRE OTROS. EL COMPUESTO I ES UN INHIBIDOR DE METALOPROTEINASAS Y REPROLISINAS POR LO QUE PUEDE SER UTIL PARA EL TRATAMIENTO DE ARTRITIS, ENFERMEDAD INFLAMATORIA DEL INTESTINO, ENFERMEDAD DE CROHN, ENFISEMA, SINDROME DE LA DIFICULTAD RESPIRATORIA AGUDA, ASMA A compound of the formula wherein R1, R2 R3, R4 R5, R6, R7, R8, R9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, and other diseases characterized by matrix metalloproteinase or mammalian reprolysin activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.