META-DIARYLANILINE OR META-DIARYLPYRIDINAMINE COMPOUND, PREPARATION METHOD AND MEDICAL USES THEREOF

摘要

Meta-diarylaniline or meta-diarylpyridinamine compounds, methods for preparing the same and uses thereof in manufacture of a medicament. The compounds according to the present application have strong inhibitory activity (at nM level) against wild-type and various drug-resistant HIV viral strains, exhibit good druggability, and can be easily synthesized.

主权项

1. A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is —NH2, —OH a halogen, —NO2, —CN, —COOH, —SO3H, —OCH3, —CH3 or —CF3; R2 is H; R3 is H, OH, a halogen, —NH2, cyano, triazo, ethynyl, —NO2, —COOH, —SO3H, —CF3, vinyl, C1-4 acyl, C1-4 ester group, trifluoroacetoxyl, C1-4 acyloxy, OCONH2, OCONHCH3, uramido, guanido, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 haloalkyl, C1-6 aminoalkyl, C1-6 ether alkyl, C1-6 alkoxy, C1-6 hydroxyalkoxy, C1-6 haloalkoxy, C1-6 aminoalkoxy, C1-6 ether alkoxy, C1-6 alkylamino, C1-6 dialkylamino, C1-6 ether alkylamino, C3-8 cycloalkyl, C3-8 cyclylalkoxy, C3-8 cyclylalkylamino, heterocyclyl, 3- to 8-membered heterocyclyl substituted by C1-4 hydroxyalkyl or C1-4 haloalkyl or C1-4 aminoalkyl or C1-4 cyanoalkyl or C1-4 ether alkyl, 3- to 8-membered heterocyclylalkyl substituted by C1-4 hydroxyalkyl or C1-4 haloalkyl or C1-4 aminoalkyl or C1-4 cyanoalkyl or C1-4 ether alkyl, 3- to 8-membered heterocyclylalkoxy substituted by C1-4 hydroxyalkyl or C1-4 haloalkyl or C1-4 aminoalkyl or C1-4 cyanoalkyl or C1-4 ether alkyl, or 3- to 8-membered heterocyclylalkylamino substituted by C1-4 hydroxyalkyl or C1-4 haloalkyl or C1-4 aminoalkyl or C1-4 cyanoalkyl or C1-4 ether alkyl; R4 is —CN, —NH2, —OH, a halogen, —NO2, —COOH, —SO3H, —OCH3, —CH3, —CF3, vinyl, ethynyl, triazo, cyanovinyl or cyanoethynyl; R5 is C1-6 alkyl, C1-6 alkoxy, a halogen or C1-6 haloalkyl; R6 is C1-6 alkyl, C1-6 alkoxy, a halogen or C1-6 haloalkyl; R6 and R5 are identical or different; R7 is —NH2, —OH, a halogen, —NO2, —CN, —COOH, —SO3H, —OCH3, —CH3, —CH═CH—CN, or —CF3; or R7 is —NH2, —OH, a halogen, —NO2, —CN, —OCH3, —CH3, —CH═CH—CN, or —CF3, linked to 1, 2, 3, or 4 —CH2—; or R7 is C1-6 aminoalkyl, C1-6 hydroxyalkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, C1-6 alkoxy, C1-6 alkyl, C1-6 alkylamino, C1-6 dialkylamino, C1-6 ether alkoxy, C2-6 alkenyl or alkynyl, ene-ene-containing conjugated or non-conjugated C2-6 hydrocarbonyl, ene-yne-containing conjugated or non-conjugated C2-6 hydrocarbonyl, ene-carbonyl-containing conjugated or non-conjugated C2-6 hydrocarbonyl, yne-carbonyl-containing conjugated or non-conjugated C2-6 hydrocarbonyl, C1-6 hydrocarbonyl substituted with one or more hydroxyl or halogen; X is —NH— or —O—; Y is —CH— or —N—; and m is 0, 1, 2, 3 or 4.