5h-thieno [3,4-c] pyrrole-4, 6-dione derivatives against...

C - Chemistry – Metallurgy – 07 – D

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C07D 495/04 (2006.01) A61K 31/407 (2006.01) C07D 209/00 (2006.01) C07D 333/00 (2006.01)

Patent

CA 2623965

The invention relates to 5H-thieno[3,4-c]pyrrole-4,6-dione derivatives represented by formula ('), its various pharmaceutically acceptable salts, its preparation and its use as active ingredient in the medicament which can inhibit release of tumor necrosis factor (TNF) in organism: (') in which R1 represents H, C1-6 alkyl, OR4, OC(O)R5, NO2, NHC(O)R6, NR7R8; R2 represents H, halogen, C1-6 alkyl; R3 represents H, methyl, isopropyl, allyl, benzyl, CH2CO2(C1-6 alkyl), CH2(CH2)nR9; in which R4, R5, R6, R7 and R8 represent H, C1-6 alkyl; R9 represents H, C1-6 alkyl, OH, OC1-6 alkyl, NH2, NHC1-6 alkyl, N(C1-6 alkyl)2, CO2(C1-6 alkyl); n is 1, 2, 3, 4.

La présente invention concerne des dérivés de 5H-thiéno[3,4-c]pyrrole-4,6-dione représentés par la formule (`), leurs divers sels pharmaceutiquement acceptables, leurs préparation et leur utilisation en tant que principe actif dans le médicament capable d~inhiber la libération du facteur de nécrose tumorale (TNF) dans l~organisme : (`) où R1 représente H, alkyle en C1-6, OR4, OC(O)R5, NO2, NHC(O)R6, NR7R8; R2 représente H, halogène, alkyle en C1-6; R3 représente H, méthyle, isopropyle, allyle, benzyle, CH2CO2(C1-6 alkyle), CH2(CH2)nR9; R4, R5, R6, R7 et R8 représentent H, alkyle en C1-6; R9 représente H, alkyle en C1-6, OH, OC1-6 alkyle, NH2, NHC1-6 alkyle, N(C1-6 alkyle)2, CO2(C1-6 alkyle); n est 1, 2, 3, 4.

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