Piperazine derivatives useful as ccr5 antagonists

Details Piperazine derivatives useful as ccr5 antagonists Piperazine derivatives useful as ccr5 antagonists

C - Chemistry, Metallurgy

07

D

C07D 211/58 (2006.01) A61K 31/496 (2006.01) A61P 19/00 (2006.01) A61P 31/12 (2006.01) C07D 401/06 (2006.01) C07D 401/10 (2006.01) C07D 405/12 (2006.01) C07D 409/06 (2006.01) C07D 413/06 (2006.01)

Patent

CA 2371583

The use of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 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.

L'invention concerne l'utilisation d'antagonistes CCR5 de formule (I), ou d'un sel pharmaceutiquement acceptable de ceux-ci. Dans cette formule, R représente phényle, pyridyle, thiophényle, ou naphtyle éventuellement substitué; R<1> symbolise hydrogène ou alkyle; R<2> désigne phényle substitué, hétéroaryle substitué, naphtyle, fluorényle, diphénylméthyle ou phénylalkyle ou hétéroarylalkyle éventuellement substitué; R<3> représente hydrogène, alkyle, alkoxyalkyle, cycloalkyle, cycloalkylalkyle, ou phényle, phénylalkyle, naphtyle, naphtylalkyle, hétéroaryle, ou hétéroarylalkyle éventuellement substitué; R<4>, R<5>, et R<7> symbolisent hydrogène ou alkyle; R<6> désigne hydrogène, alkyle, ou alkényle. Ces antagonistes permettent de traiter le VIH, le rejet de transplantations d'organe solide, les réactions du greffon contre l'hôte, l'arthrite, l'arthrite rhumatoïde, les maladies intestinales inflammatoires, la dermatite atopique, le psoriasis, l'asthme, les allergies ou la sclérose en plaques. Cette invention concerne également de nouveaux composés, des compositions pharmaceutiques renfermant ceux-ci, et la combinaison des antagonistes CCR5 de cette invention et d'agents antiviraux utilisés pour traiter le VIH, ou d'agents employés pour traiter les maladies inflammatoires.

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