[EN] 5- OR 6-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION<br/>[FR] DERIVES DE BENZIMIDAZOLE SUBSTITUES EN 5- OU 6- UTILISES EN TANT QU'INHIBITEURS DE LA REPLICATION DU VIRUS RESPIRATOIRE SYNCITIAL
申请人:TIBOTEC PHARM LTD
公开号:WO2005058874A1
公开(公告)日:2005-06-30
The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar2, R6, pyrrolidinyl substituted with R6, piperidinyl substituted with R6 or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Arl or a monocyclic or bicyclic heterocycle; one of R 2a and R2b is cyanoCl-6alkyl, cyanoC2-6alkenyl, Ar3Cl-6alkyl, Het-C1-6alky1, N(R8aR8b)Cl-6alkyl, Ar3C2-6alkenyl, Het-C2-6alkenyl, Ar3 aminoCl-6alkyl, HetaminoCl-6alkyl, Ar3thioC1-6 alkyl, Het-thioC1-6alkyl, Ar3sulfonylC1-6 alkyl, HetsulfonylC1-6alkyl, Ar3aminocarbonyl, Het-aminocarbonyl, Ar3(CH2)naminocarbonyl, Het-(CH2)naminocarbonyl, Ar3carbonylamino, Het-carbonylamino, Ar3(CH2)ncarbonylamino, Het-(CH2)ncarbonylamino, and the other one of R2a and R2b is hydrogen; in case R2a is hydrogen, then R3 is hydrogen; in case R2b is hydrogen, the R3 is hydrogen or C1-6alkyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
本发明涉及对呼吸道合胞病毒复制具有抑制活性的5-或6-取代
苯并咪唑衍
生物,其具有���下式(I)的结构:一种前药、N-
氧化物、加成盐、季
铵盐、
金属配合物或其立体化异构体,其中Q为Ar2、R6、用R6取代的
吡咯烷基、用R6取代的
哌啶基或用R6取代的
环己胺基,G为直链键或可选择取代的C1-10烷二基;R1为Arl或单环或双环杂环;R2a和R2b中的一个为
氰基C1-6烷基、
氰基C2-6
烯基、Ar3C1-6烷基、Het-C1-6烷基、N(R8aR8b)C1-6烷基、Ar3C2-6
烯基、Het-C2-6
烯基、Ar3
氨基C1-6烷基、Het
氨基C1-6烷基、Ar3
硫基C1-6烷基、Het-
硫基C1-6烷基、Ar3磺酰基C1-6烷基、Het-磺酰基C1-6烷基、Ar3
氨基羰基、Het-
氨基羰基、Ar3(
CH2)n
氨基羰基、Het-( )n
氨基羰基、Ar3羰基
氨基、Het-羰基
氨基、Ar3( )n羰基
氨基、Het-( )n羰基
氨基,R2a和R2b中的另一个为
氢;如果R2a为
氢,则R3为
氢;如果R2b为
氢,则R3为
氢或C1-6烷基。本发明还涉及它们的制备和包含它们的组合物,以及它们作为药物的用途。