首页> 外国专利> MORFOLINILO CONTAINING BENCIMIDAZOLS AS INHIBITORS OF THE REPLICATION OF RESPIRATORY SYNTHETIC VIRUSES.

MORFOLINILO CONTAINING BENCIMIDAZOLS AS INHIBITORS OF THE REPLICATION OF RESPIRATORY SYNTHETIC VIRUSES.

机译:含有苯甲咪唑的吗啡起抑制呼吸道合成病毒复制作用。

摘要

A compound having the formula (See formula) An N-oxide, addition salt, quaternary amino, metal complex, or a stereochemically isomeric form thereof; where G is a direct bond or C1-10alkanediyl optionally substituted by one or more substituents individually selected from the group of substituents consisting of hydroxy, C1-6alkyloxy, Ar1C1-6alkyloxy, C1-6alkylthio, Ar1C1-6alkylthio , HO (-CH2-CH2-O) n-, C1-6alkyloxy (-CH2-CH2-O) n- or Ar1C1-6alkyloxy (-CH2-CH2-O) n-; R1 is Ar1 or a monocyclic or bicyclic heterocycle selected from piperidinyl, piperazinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthyridinyl, 1H-imidazo [4,5-b] pyridinyl, 3H-imidazo [4,5-b] pyridinyl, imidazo [1,2-a] pyridinyl 2,3-dihydro-1,4-dioxino [2,3-b] pyridyl or a radical of the formula (See formula) where each of the mentioned monocyclic or bicyclic heterocycles can be optionally substituted by one or, when if possible, more like 2,3,4 or 5 substituents selected individually, from the group of substituents consisting of halo, hydroxy, amino, cyano, carboxyl, C1-6 alkyl, C1-6alkyloxy, C1- 6alkylthio, C1-6alkyloxyC1-6alkyl, Ar1, Ar1C1-6Alkyl, Ar1C1-6alkyloxy, hydroxyC1-6Alkyl, mono- or di (C1-6alkyl) amino, mono- or di (C1-6alkyl) aminoC1-6alkyl, polyhaloC1-6alkyl, C1-6alkylcarbonylamino, C1-6Al NR5c-, Ar1-SO2-NR5c-, C1-6alkyloxycarbonyl, -C (= O) -NR5cR5d, HO (-CH2-CH2-O) n-, halo (-CH2-CH2-O) n-, C1-6alkyloxy (-CH2-CH2-O) n-, Ar1C1-6alkyloxy (-CH2-CH2-O) n- and mono- or di (C1-6alkyl) amino (-CH2-CH2-O) n-; each n is independently 1, 2, 3 or 4; each m is independently 1 or 2; each p is independently 1 or 2; each t is independently 0, 1 or 2; Q is R7, pyrrolidinyl substituted by R7, piperidinyl substituted by R7 or homopiperidinyl substituted by R7 where R7 is C1-6 alkyl substituted by a heterocycle or R7 is C1-6 alkyl substituted by both an OR8 radical and a heterocycle, where the heterocycle mentioned It is selected from the group consisting of oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrotiazepine-hexahydrotiazepine , 1,1-dioxo-hexahydrotiazepine; where each of the mentioned heterocycles can be optionally substituted by one or two substituents selected from the group consisting of C1-6 alkyl, hydroxyC1-6 alkyl, aminocarbonylC1-6 alkyl, hydroxy, carboxyl, C1-4alkyloxycarbonyl, aminocarbonyl, mono- or di (C1-4alkyl) aminocarbonyl, C1-4alkylcarbonylamino, aminosulfonyl and mono- or di (C1-4alkyl) aminosulfonyl; R8 is ...
机译:具有下式的化合物(参见下式):N-氧化物,加成盐,季氨基,金属络合物或其立体化学异构形式;其中G是直接键或任选地被一个或多个取代基取代的C1-10烷二基,所述取代基分别选自羟基,C1-6烷氧基,Ar1C1-6烷氧基,C1-6烷硫基,Ar1C1-6烷硫基,HO(-CH2-CH2 -O)正-,C 1-6烷氧基(-CH 2 -CH 2 -O)正-或Ar 1 -C 1-6烷氧基(-CH 2 -CH 2 -O)正-; R1是AR1或一个单环或哌啶基,哌嗪基,吡啶基,吡嗪基,哒嗪基,嘧啶基,呋喃基,四氢呋喃基,噻吩基,吡咯基,噻唑基,恶唑基,咪唑基,异噻唑基,吡唑基,异恶唑基,恶二唑基,喹啉基,喹喔啉基,苯并呋喃基选择双环杂环,苯并噻吩基,苯并咪唑基,苯并恶唑基,苯并噻唑基,吡啶并吡啶基,萘啶基,1H-咪唑并[4,5-b]吡啶基,3H-咪唑并[4,5-b]吡啶基,咪唑并[1,2-a]吡啶基二氢-1,4-二氧杂[2,3-b]吡啶基或下式的基团(参见式),其中每个提及的单环或双环杂环可任选被一个取代,或在可能的情况下,更像2,分别选自卤素,羟基,氨基,氰基,羧基,C 1-6烷基,C 1-6烷氧基,C 1-6烷硫基,C 1-6烷氧基C 1-6烷基,Ar 1,Ar 1 C 1-6烷基的3,4或5个取代基,Ar 1 C 1-6烷氧基,羟基C 1-6烷基,单或二(C 1-6烷基)氨基,单或二(C 1-6烷基) )氨基C1-6烷基,多卤代C1-6烷基,C1-6烷基羰基氨基,C1-6Al NR5c-,Ar1-SO2-NR5c-,C1-6烷氧羰基,-C(= O)-NR5cR5d,HO(-CH2-CH2-O)n ,卤素(-CH2-CH2-O)正,C1-6烷氧基(-CH2-CH2-O)正,Ar1C1-6烷氧基(-CH2-CH2-O)正和单或二(C1-6烷基)氨基(-CH2-CH2-O)n-;每个n独立地是1、2、3或4;每个m独立为1或2;每个p独立地为1或2;每个t独立地为0、1或2; Q是R 7,被R 7取代的吡咯烷基,被R 7取代的哌啶基或被R 7取代的高哌啶基,其中R 7是被杂环取代的C 1-6烷基或R 7是被OR 8基团和杂环均取代的C 1-6烷基,它选自由恶唑烷,噻唑烷,1-氧代噻唑烷,1,1-二氧噻唑烷,吗啉基,硫吗啉基,1-氧代硫吗啉基,1,1-二氧代硫吗啉基,六氢氧杂ze庚因,六氢二氮杂卓-六氢噻庚因组成的组二氧六氢噻氮平;其中每个所述杂环可任选地被一个或两个选自C 1-6烷基,羟基C 1-6烷基,氨基羰基C 1-6烷基,羟基,羧基,C 1-4烷氧基羰基,氨基羰基,单或二取代基的取代基取代(C1-4烷基)氨基羰基,C1-4烷基羰基氨基,氨基磺酰基和单或二(C1-4烷基)氨基磺酰基; R8是...

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