[EN] NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS<br/>[FR] INHIBITEURS NON NUCLEOSIDIQUES DE LA TRANSCRIPTASE INVERSE
申请人:BOEHRINGER INGELHEIM CA LTD
公开号:WO2004026875A1
公开(公告)日:2004-04-01
Compounds represented by formula (1), wherein R1 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2 is H or methyl; R3 is H or (C1-4)alkyl; R4 is H or (C1-4)alkyl; R5 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cyclo-alkyl or (C3-7)cycloalkyl; and W is a fused phenyl-5 or 6-membered heterocycle having one or two heteroatoms selected from N or S; or W is phenyl, 1,1'-biphenyl, 2, 3-dihydro-1H-indene, 1, 2, 3, 4-tetrahydronaphthyl, or naphthyl; said W being optionally substituted with (C1-4)alkyl, which in turn can be optionally substituted with a carboxy or (C1-4)alkoxycarbonyl, or a salt or ester thereof. The compounds have inhibitory activity against Wild Type, single and double mutant strains of HIV.
由以下公式表示的化合物,其中R1为H、卤素、(C1-4)烷基、O(C1-4)烷基和卤代烷基;R2为H或甲基;R3为H或(C1-4)烷基;R4为H或(C1-4)烷基;R5为(C1-4)烷基、(C1-4)烷基(C3-7)环烷基或(C3-7)环烷基;W为具有从N或S中选择的一个或两个杂原子的融合苯基5或6成员杂环;或W为苯基、1,1'-联苯、2,3-二氢-1H-茚烯、1,2,3,4-四氢萘基或萘基;所述的W可以选择地被(C1-4)烷基取代,而该烷基可以选择地被羧基或(C1-4)烷氧羰基取代,或其盐或酯。这些化合物对HIV的野生型、单突变株和双突变株具有抑制活性。