5-pyridyl-1,3-azole compounds, process for producing the...

C - Chemistry – Metallurgy – 07 – D

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C07D 417/04 (2006.01) A61K 31/4439 (2006.01) A61P 1/00 (2006.01) A61P 3/10 (2006.01) A61P 7/00 (2006.01) A61P 9/00 (2006.01) A61P 29/00 (2006.01) A61P 31/12 (2006.01) A61P 43/00 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2370264

Optionally N-oxidized compounds represented by general formula (I) salts thereof which are usable as preventives or remedies for diseases in association with adenosine A3 receptor because of having excellent adenosine A3 receptor antagonism thereof wherein R1 represents hydrogen, hydrocarbyl, a heterocycle, amino or acyl; R2 represents an aromatic group; R3 represents hydrogen, pyridyl or aromatic hydrocarbyl; X represents oxygen or optionally oxidized sulfur; Y represents a bond, oxygen, optionally oxidized sulfur or NR4 (wherein R4 represents hydrogen, hydrocarbyl, or acyl); and Z represents a bond or a divalent chain hydrocarbyl. Moreover, the compounds (I) or salts thereof exhibit excellent effects of inhibiting p38MAP kinase and inhibiting TNF-.alpha. and, therefore, are also usable as preventives or remedies for diseases in association with p38MAP kinase or TNF-.alpha..

L'invention concerne des composés N-oxydés représentés éventuellement par la formule générale (I) ou leurs sels pouvant servir de préventifs ou de remèdes contre des maladies en association avec le récepteur de l'adénosine A¿3? du fait de présenter un excellent antagonisme de récepteur d'adénosine A¿3? associé. R?1¿ représente hydrogène, hydrocarbyle, un hétérocycle, amino ou acyle; R?2¿ un groupe aromatique; R?3¿ hydrogène, pyridyle ou hydrocarbyle aromatique; X oxygène ou éventuellement soufre oxydé; Y une liaison, oxygène, éventuellement du soufre oxydé ou NR?4¿ (R?4¿ représentant hydrogène, hydrocarbyle ou acyle); et Z représente une liaison ou un hydrocarbyle à chaîne bivalente. En outre, les composés (I) ou leurs sels présentent d'excellents effets d'inhibition de la kinase p38MAP et du TNF-.alpha. et, par conséquent, servent également de préventifs ou de remèdes contre des maladies en association avec la kinase p38MAP ou le TNF-.alpha..

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