abstract |
Taught are derivatives of 5H-thieno (3,4-c) pyrrole-4,6-dione, their organic, and inorganic salts, methods of synthesis of these derivatives, and their application as active pharmaceutical-ingredients useful as inhibitors of TNFα, the derivative being represented by the general formula (I):n nin which R 1 represents H, C 1-6 alkyl, OR 4 , OC(O)R 5 , NO 2 , NHC(O)R 6 , or NR 7 R 8 ; R 2 represents H, a halogen, or C 1-6 alkyl; R 3 represents H, methyl, isopropyl, allyl, benzyl, CH 2 CO 2 (C 1-6 alkyl), or CH 2 (CH 2 ) n R 9 ; R 4 , R 5 , R 6 , R 7 , and R 8 each independently and at each occurrence represents H, or C 1-6 alkyl; R 9 represents H, C 1-6 alkyl, OH, OC 1-6 alkyl, NH 2 , NHC 1-6 alkyl, N(C 1-6 alkyl) 2 , or CO 2 (C 1-6 alkyl); and n represents 1, 2, 3, or 4. |