Tnf-.alpha. production inhibitors

Details Tnf-.alpha. production inhibitors Tnf-.alpha. production inhibitors

C - Chemistry, Metallurgy

07

D

C07D 213/40 (2006.01) A61K 31/4409 (2006.01) A61P 19/02 (2006.01) A61P 37/00 (2006.01)

Patent

CA 2409741

A purpose of the present invention is to provide TNF-.alpha. production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-.alpha. production inhibitory activities, (see formula 1) wherein "A" is -(NR4)- , -(CR5R6)- or -O-, "B" is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and "X" is oxygen or sulfer respectively.

L'invention concerne des inhibiteurs de production de TNF-.alpha. utilisés contre les maladies auto-immunes telles que la polyarthrite rhumatoïde. De nouveaux composés représentés par la formule générale (1), ou des sels de ces derniers, présentent d'excellentes activités d'inhibition de production de TNF-.alpha. : (1), formule dans laquelle A est -(NR?4¿)-, -(CR?5¿R?6¿)-, ou -O- ; B est alcoylène ou alcénylène ; R?1¿, R?2¿, R?4¿, R?5¿, et R?6¿ sont chacun hydrogène, alkyle, alcényle, adamantylalkyle, ou un autre élément semblable ; R?3¿ est aryle ou un groupe hétérocyclique non saturé ; et X est de l'oxygène ou du soufre.

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