DERIVADOS DE PIPERAZINA UTILES COMO ANTAGONISTAS CCR5

• Main Authors: BAROUDY BAHIGE M, MCKITTRICK BRIAN A, JOSIEN HUBERT B, PALANI ANANDAN, GILBERT ERIC, SMITH ELIZABETH M, STEENSMA RUO, VICE SUSAN F, MILLER MICHAEL W, NEUSTADT BERNARD R, CLADER JOHN W, LABROLI MARC A, LAUGHLIN MARK A, MCCOMBIE STUART W, TAGAT JAYARAM R
• Format: Patent
• Language: Spanish
• Published: 09.02.2001
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEASURING; MEASURING VOLUME, VOLUME FLOW, MASS FLOW OR LIQUIDLEVEL; MEDICAL OR VETERINARY SCIENCE; METALLURGY; METERING BY VOLUME; ORGANIC CHEMISTRY; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TESTING

SE REFIERE A DERIVADOS DE PIPERAZINA DE FORMULA II, DONDE: Ra ES R8a-FENILO, R8b-PIRIDILO, R8b-TIOFENILO, R9-NAFTILO; R1 ES H, ALQUILO C1-C6; R2 ES R9,R10,R11-FENILO, R9,R10,R11-HETEROARILO, R9,R10,R11-N-OXIDO DE HETEROARILO, R12,R13-HETEROARILO, ENTRE OTROS; R3 ES H, ALQUILO C1-C6, ALCOXI C1-C6-ALQUILO C1-C6, CICLOALQUILO C3-C10-ALQUILO C1-C6, R8-FENILO, ENTRE OTROS; R4, R5, R7, R13 SON H, ALQUILO C1-C6; R6 ES H, ALQUILO C1-C6, ALQUENILO C2-C6; R8 ES H, HALOGENO, ALQUILO C1-C6, ALCOXI C1-C6, CF3, CF3O, ENTRE OTROS; R8a ES H, HALOGENO, CF3, CF3O, CN, CF3SO2, ENTRE OTROS; R8b ES H, HALOGENO, -CF3, CF3O-, CH3C(O)-, ENTRE OTROS; R9 Y R10 SON ALQUILO C1-C6, HALOGENO, -NR17R18, OH, ENTRE OTROS; R11 ES R9, H, FENILO, NO2, CN, CH2F, CHO, ENTRE OTROS. R12 ES ALQUILO C1-C6, NH2, R14-FENILO; R14 ES H, ALQUILO C1-C6, CF3, ENTRE OTROS. LOS DERIVADOS DE PIPERAZINA SON ANTAGONISTAS SELECTIVOS DE CCR5 Y SE COMBINAN CON AGENTES ANTIVIRALES COMO INHIBIDORES DE TRANSCRIPTASA INVERSA NUCLEOSIDICA O NO NUCLEOSIDICA, INHIBIDORES DE PROTEASA, O AGENTES INMUNOSUPRESORES Y PUEDEN SER UTILES EN EL TRATAMIENTO DEL VIRUS DE VIH, RECHAZO A TRANSPLANTES DE ORGANOS, ARTRITIS, ENFERMEDAD INFLAMATORIA DEL INTESTINO, DERMATITIS ATOPICA, PSORIASIS The use is described of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R 1 is hydrogen or alkyl; R 2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R 3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R 4 , R 5 and R 7 are hydrogen or alkyl; R 6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.