首页> 外国专利> BENZIMIDAZOLES AND IMIDAZOPYRIDINES AS RESPIRATORY SYNCYTIAL VIRUS REPLICATION INHIBITORS

BENZIMIDAZOLES AND IMIDAZOPYRIDINES AS RESPIRATORY SYNCYTIAL VIRUS REPLICATION INHIBITORS

机译:苯并咪唑和咪唑啉类作为呼吸道合胞病毒复制抑制剂

摘要

The present invention concerns compounds of formula (I), prodrugs, N-oxides,addition salts, quaternary amines, metal complexes and stereochemicallyisomeric forms thereof wherein -a1=a2-a3=a4- represents a radical of formula -CH=CH-CH=CH-; -N=CH-CH=CH-; -CH=N-CH=CH-; -CH=CH-N=CH-; -CH=CH-CH=N-; whereineach hydrogen atom may optionally be substituted; Q is a radical of formulae(b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula -NR2- or -CH(NR2R4)-; X1 isNR4, S, S(=O), S(=O)2, O, CH2, C(=O), CH(=CH2), CH(OH), CH(CH3), CH(OCH3),CH(SCH3), CH(NR5aR5b), CH2-NR4 or NR4-CH2; X2 is a direct bond, CH2, C(=O),NR4, C1-4alkyl-NR4, NR4-C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; andwhereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3; provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the .alpha. positionrelative to a nitrogen atom; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is an optionally substituted bicyclic heterocycle; R2 ishydrogen, formyl, C1-6alkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl,homopiperidinyl, C3-7cycloalkyl or C1-10alkyl substituted with N(R6)2 andoptionally with another substituent; R3 is hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy, arylC1-6alkyl or arylC1-6alkyloxy, R4 is hydrogen, C1-6alkyl orarylC1-6alkyl; R5a, R5b, R5c and R5d are hydrogen or C1-6alkyl; or R5a andR5b, or R5c and R5d taken together from a bivalent radical of formula -(CH2)s-wherein S is 4 or 5; R6 is hydrogen, C1-4alkyl, formyl, hydroxyC1-6alkyl, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; aryl is optionally substituted phenyl;Het is pyridyl, pyrimidinyl, pyryzinyl, pyridazinyl; as respiratory syncytialvirus replication inhibitors; their preparation, compositions containing themand their use as a medicine.
机译:本发明涉及式(I)的化合物,前药,N-氧化物,加成盐,季胺,金属络合物和立体化学-a1 = a2-a3 = a4-表示式-基团的异构体CH = CH-CH = CH-; -N = CH-CH = CH-; -CH = N-CH = CH-; -CH = CH-N = CH-; -CH = CH-CH = N-;其中每个氢原子可任选被取代; Q是公式的一个基(b-1),(b-2),(b-3),(b-4),(b-5),(b-6),(b-7)和(b-8),其中Alk是C1-6烷二基; Y1是式-NR2-或-CH(NR2R4)-的二价基团; X1是NR4,S,S(= O),S(= O)2,O,CH2,C(= O),CH(= CH2),CH(OH),CH(CH3),CH(OCH3),CH(SCH3),CH(NR5aR5b),CH2-NR4或NR4-CH2; X2是直接键CH2 C(= O)NR 4,C 1-4烷基-NR 4,NR 4 -C 1-4烷基,t为2至5;你是1到5; v是2或3;和从而使Alk和(b-3),(b-4),(b-5),(b-6),(b-7)和(b-8),可以选择用R3代替;前提是当R3为羟基或C1-6烷氧基,则R3不能取代α中的氢原子。位置相对于氮原子; G是直接键或可选取代的C1-10烷二基; R1是任选取代的双环杂环; R2是氢,甲酰基,C 1-6烷基羰基,杂羰基,吡咯烷基,哌啶基,高哌啶基,C3-7环烷基或被N(R6)2取代的C1-10烷基任选地具有另一个取代基; R3是氢,羟基,C1-6烷基,C1-6烷氧基,芳基C1-6烷基或芳基C1-6烷氧基,R4为氢,C1-6烷基或芳基C 1-6烷基; R5a,R5b,R5c和R5d是氢或C1-6烷基;或R5a和从式-(CH 2)s-的二价基团一起得到R 5b或R 5c和R 5d其中S为4或5; R6是氢,C1-4烷基,甲酰基,羟基C1-6烷基,C1-6-烷基羰基或C 1-6烷氧基羰基;芳基是任选取代的苯基;Het是吡啶基,嘧啶基,吡嗪基,哒嗪基;作为呼吸道合胞体病毒复制抑制剂;他们的准备,包含他们的成分及其作为药物的用途。

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号