Novel urea derivatives having nitrogen aromatic heterocycle

C - Chemistry – Metallurgy – 07 – D

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C07D 213/40 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) A61K 31/47 (2006.01) A61K 31/505 (2006.01) C07D 207/325 (2006.01) C07D 209/16 (2006.01) C07D 213/36 (2006.01) C07D 215/12 (2006.01) C07D 233/61 (2006.01) C07D 233/64 (2006.01) C07D 235/16 (2006.01) C07D 239/26 (2006.01)

Patent

CA 2339525

Novel urea derivatives represented by general formula (I) and salts thereof, which exhibit an inhibitory effect against the production of TNF-.alpha. and are useful as remedies for various diseases, particularly autoimmune diseases such as rheumatoid arthritis, wherein R1 is H, alkyl, phenyl or formula (II) R2 is H, alkyl, carboxyl, an ester thereof or the like; R3 and R4 are each H, alkyl, cycloalkyl or the like; R5 is H, alkyl, hydroxyl or the like; R6 is a nitrogenous aromatic heterocycle; and A1 and A2 are each alkylene.

Cette invention se rapporte à de nouveaux dérivés d'urée, représentés par la formule générale (I), et à des sels de ces dérivés, qui possèdent un effet inhibiteur contre la production de TNF-.alpha. et qui sont utiles comme médicaments contre diverses maladies, notamment les maladies auto-immunes telles que l'arthrite rhumatoïde. Dans cette formule (I), R?1¿ représente H, alkyle, phényle ou (II), R?2¿ représente H, alkyle, carboxyle, un ester de ceux-ci ou similaires; R?3¿ et R?4¿ représentent chacun H, alkyle, cycloalkyle ou similaires; R?5¿ représente H, alkyle, hydroxyle ou similaires; R?6¿ représente un hétérocycle aromatique azoté; et A?1¿ et A?2¿ représentent chacun alkylène.

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