Piperazine derivatives useful as CCR5 antagonists

   
   

The use of CCR5 antagonists of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R.sup.1 is hydrogen or alkyl; R.sup.2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R.sup.3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R.sup.4, R.sup.5 and R.sup.7 are hydrogen or alkyl; R.sup.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 is disclosed, 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.

El uso de los antagonistas CCR5 del ## del ## STR1 del fórmula o de una sal farmacéutico aceptable de eso, en donde R es opcionalmente fenilo, pyridyl, thiophenyl o naftílico substituido; R.sup.1 es hidrógeno o alkyl; R.sup.2 es heteroaryl fenilo, substituido substituido, naftílico, fluorenyl, diphenylmethyl o fenilo o heteroaryl-heteroaryl-alkyl opcionalmente substituido; R.sup.3 es hidrógeno, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, o fenilo, phenylalkyl, naftílico, naphthylalkyl, heteroaryl o heteroarylalkyl opcionalmente substituido; R.sup.4, R.sup.5 y R.sup.7 son hidrógeno o alkyl; R.sup.6 es hidrógeno, alkyl o alkenyl; para el tratamiento del VIH, el rechazamiento sólido del trasplante del órgano, el injerto v, la enfermedad del anfitrión, la artritis, la artritis reumatoide, la enfermedad inflamatoria del intestino, el dermatitis atópico, el psoriasis, el asma, las alergias o la esclerosis múltiple se divulga, tan bien como compuestos de la novela, las composiciones farmacéuticas que las abarcan, y la combinación de los antagonistas CCR5 de la invención conjuntamente con los agentes antivirus útiles en el tratamiento del VIH o los agentes útiles en el tratamiento de enfermedades inflamatorias.

 
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< Composition and methods for treatment of HIV infection

> Piperidinylethyl-, phenoxyethyl-, and .beta.-fluorophenethyl-substituted thiourea compounds with potent anti-HIV activity

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