Piperazine compounds and medicinal use thereof

C - Chemistry – Metallurgy – 07 – D

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C07D 213/74 (2006.01) A61K 31/495 (2006.01) C07D 233/90 (2006.01) C07D 239/42 (2006.01) C07D 239/46 (2006.01) C07D 239/47 (2006.01) C07D 239/48 (2006.01) C07D 239/52 (2006.01) C07D 239/545 (2006.01) C07D 277/42 (2006.01) C07D 277/58 (2006.01) C07D 295/12 (2006.01) C07D 295/135 (2006.01)

Patent

CA 2306811

Piperazine compounds represented by the following general formula (I) or pharmaceutically acceptable salts thereof and drugs comprising these compounds, wherein R1 and R2 represent each hydrogen, halogeno, lower alkyl, lower alkoxy, optionally substituted amino, nitro, hydroxy or cyano; R3, R4 and R5 represent each hydrogen, halogeno, lower alkyl, lower alkoxy, nitro, optionally substituted amino or hydroxy; R6 and R7 represent each hydrogen, optionally halogenated lower alkyl, aralkyl, acyl or halogenated lower acyl; R8 and R9 represent each hydrogen or lower alkyl; Y represents lower alkylene, etc.; and the ring A represents phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl. Because of having excellent TNF-.alpha. production inhibitory effect and/or IL-10 production promoting effect, these compounds are useful as TNF-.alpha. production inhibitors and/or IL-10 production promoters with high safety. They are useful as preventives or remedies for, e.g., chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases caused by infection, autoimmune diseases, allergic diseases and other TNF- .alpha.-mediated diseases.

Composés de pipérazine de formule générale (I) ou sels pharmaceutiquement acceptables desdits composés et médicaments contenant ces composés. Dans la formule (I), R?1¿ et R?2¿ représentent chacun hydrogène, halogéno, alkyle inférieur, alcoxy inférieur, amino éventuellement substitué, nitro, hydroxy ou cyano; R?3¿, R?4¿ et R?5¿ représentent chacun hydrogène, halogéno, alkyle inférieur, alcoxy inférieur, nitro, amino éventuellement substitué ou hydroxy; R?6¿ et R?7¿ représentent chacun hydrogène, alkyle inférieur éventuellement halogéné, aralkyle, acyle ou acyle inférieur halogéné; R?8¿ et R?9¿ représentent chacun hydrogène ou alkyle inférieur; Y représente alkylène inférieur, etc.; et le noyau A représente phényle, pyrimidyle, thiazolyle, pyridyle, pyrazyle ou imidazolyle. Ces composés ayant un excellent effet d'inhibition de la production de TNF-.alpha., ou de promotion de la production de IL-10, ils sont utiles comme inhibiteurs de la production de TNF-.alpha. et/ou comme agents de promotion de la production de IL-10, et offrent une grande sécurité. Ils sont utiles pour prévenir ou soigner, par ex., les maladies inflammatoires chroniques, les maladies inflammatoires aiguës, les maladies inflammatoires causées par une infection, les maladies autoimmunes, les maladies allergiques et d'autres maladies à médiation par le TNF-.alpha..

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