Pyrimidine derivatives for the prevention of hiv infection

Abstract

This invention concerns the use of a compound for the manufacture of a medicament for the prevention of HIV infection via sexual intercourse and related intimate contact between partners, wherein the compound is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein the ring containing -a=a-a=a- and -b=b-b=b- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; Ris hydrogen; aryl; formyl; Calkylcarbonyl; Calkyl; Calkyloxycarbonyl; substituted Calkyl, Calkylcarbonyl, Calkyloxycarbonyl, Calkylcarbonyloxy; substituted CalkyloxyCalkylcarbonyl; Ris hydroxy, halo, optionally substituted Calkyl, Ccycloalkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)R, —NH—S(═O)R, —C(═O)R, —NHC(═O)H, —C(═O)NHNH, —NHC(═O)R, —C(═NH)Ror a 5-membered heterocycle; Xis —NR—, —NH—NH—, —N═N—, —O—, —C(═O)—, Calkanediyl, —CHOH—, —S—, —S(═O)—, —X—Calkanediyl- or —Calkanediyl-X—; Ris NHR; NRR; —C(═O)—NHR; —C(═O)—NRR; —C(═O)—R; —CH═N—NH—C(═O)—R; substituted Calkyl; optionally substituted CalkyloxyCalkyl; substituted Calkenyl; substituted Calkynyl; Calkyl substituted with hydroxy and a second substituent; —C(═N—O—R)—Calkyl; R; or —X—R; Ris halo, hydroxy, Calkyl, Ccycloalkyl, Calkyloxy, cyano, nitro, polyhaloCalkyl, polyhaloCalkyloxy, aminocarbonyl, Calkyloxycarbonyl, Calkylcarbonyl, formyl, amino, mono- or di(Calkyl)amino; and pharmaceutical compositions comprising them.