BONFANTI, JEAN-FRANCOIS,柏法兰,柏法蘭,ANDRIES, KOENRAAD JOZEF LODEWIJK,安纳德,安納德,FORTIN, JEROME MICHEL CLAUDE,傅裘米,傅裘米,MULLER, PHILIPPE,穆菲立,穆菲立,DOUBLET, FREDERIC MARC MAURICE,陶瑞克,陶瑞克,MEYER, CHRISTOPHE,麦克利,麥克利
申请号：
TW093139735
公开号：
TWI382981B
申请日:
2004.12.20
申请国别(地区):
TW
年份:
2013
代理人:
摘要：
The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity om the replication of the respiratory syncytial virus and having the formulaa 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 R6or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl R1is Ar1or a monocyclic or bicyclic heterocycle one of R2aand R2bis cyanoC1-6alkyl, cyanoC2-6alkenyl, Ar3C1-6alkyl, Het-C1-6alkyl, N(R8aR8b)C1-6alkyl, Ar3C2-6alkenyl, Het-C2-6alkenyl, Ar3aminoC1-6alkyl, Het-aminoC1-6alkyl, Ar3thioC1-6alkyl, Het-thioC1-6alkyl, Ar3sulfonylC1-6alkyl, Het-sulfonylC1-6alkyl, Ar3aminocarbonyl, Het-aminocarbonyl, Ar3(CH2)naminocarbonyl, Het-(CH2)naminocarbonyl, Ar3carbonylamino, Het-carbonylamino, Ar3(CH2)ncarbonylamino, Het-(CH2)ncarbonylamino, and the other one of R2aand R2bis hydrogen in case R2ais hydrogen, then R3is hydrogen in case R2bis hydrogen, the R3is hydrogen or C1-6alkyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.本發明係有關一種對呼吸道融合病毒之複製作用具有抑制活性之5-或6-經取代之苯并咪唑衍生物,其如下式及其前藥、N-氧化物、加成鹽、四級胺、金屬複合物或立體化學異構型,其中Q為Ar2、R6、經R6取代之吡咯啶基、經R6取代之六氫吡啶基或經R6取代之高碳六氫吡啶基,G為一直接鍵或可視需要經取代之C1-10烷二基;R1為Ar1或單環或雙環系雜環;R2a與R2b中之一為氰基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胺基C1-6烷基、Het-胺基C1-6烷基、Ar3硫C1-6烷基、Het-硫C1-6烷基、Ar3磺醯基C1-6烷基、Het-磺醯基C1-6烷基、Ar3胺基羰基、Het-胺基羰基、Ar3(CH2)n胺基羰基、Het-(CH2)n胺基羰基、Ar3羰基胺基、Het-羰基胺基、Ar3(CH2)n羰基胺基、Het-(CH2)n羰基胺基,且R2a與R2b中另一者為氫;若R2a為氫時,則R3為氫;若R2b為氫時,則R3為氫或C1-6烷基。亦有關其製法與含其之組合物,及其作為醫藥之用途。
