HIV-INHIBITING BENZENEACETAMIDE DERIVATIVES

摘要

A compound for use as a medicine having the formula (I) a pharmaceutically acceptable acid addition salt form or a stereochemically isomeric form thereof, wherein R1 and R2 each independently are hydrogen, C1-6alkyl or C3-6cycloalkyl; or R1 and R2 taken together with the nitrogen atom bearing said R1 and R2 may form a pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl or 4-C1-4alkylpiperazinyl group; X is O or S; R3 is hydrogen or C1-6alkyl; R4, R5 and R6 each independently are hydrogen, halo, C1-6alkyl, C1-6alkyloxy, nitro, trifluoromethyl, cyano, aminomethyl, carboxyl, C1-4alkyloxycarbonyl, C1-4alkyl-carbonyl, aminocarbonyl or hydroxy; R7 is hydrogen or halo; and R8, R9 and R10 each independently are hydrogen, halo, C1-6alkyl, C1-6alkyloxy, nitro, hydroxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, (trifluoromethyl)carbonyl, aminocarbonyl, (cyclopropyl)carbonyl or a radical C1-6alkyl-(C=Y)-wherein =Y represents =O, =N-OH, =N-OCH3, =N-NH2 or =N-N(CH3)2; provided that (1) R1 is other than n-propyl when R2, R3, R4, R5, R6, R7, R9 and R10 represent hydrogen, R8 represents 4-ethoxy and X represents oxygen, and (2) X is other than sulfur, when R1, R2, R3, R6, R7, R8, R9 and R10 represent hydrogen and R4 and R5 represent 3,4-dimethoxy. Novel compounds, pharmaceutical compositions containing said compounds of formula (I), and processes for preparing said compositions.