首页> 外国专利> 1-(1,2-Disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivative, its use, process for its preparation, pharmaceutical composition in which it is comprised as well as intermediate for its preparation

1-(1,2-Disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivative, its use, process for its preparation, pharmaceutical composition in which it is comprised as well as intermediate for its preparation

机译:1-(1,2-二取代的哌啶基)-4-(稠合的咪唑)-哌啶衍生物,其用途,其制备方法,包含其的药物组合物及其制备中间体

摘要

In the present invention, there is disclosed a 1-(1,2-disubstituted piperidinyl)-4-(fused imidazole)piperidine derivative of the general formula I, in which n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; =Q represents =O or =Nre3-; X denotes a covalent bond or -O-, -S-, -NRe3-; Re1 represents Are1, Are1alkyl containing 1 to 6 carbon atoms in the alkyl moiety or di(Are1)alkyl with 1 to 6 carbon atoms in the alkyl moiety, wherein each alkyl group is optionally substituted; Re2 represents Are2; Are2alkyl having 1 to 6 carbon atoms in the alkyl moiety, Het or Hetalkyl with 1 to 6 carbon atoms in the alkyl moiety; Re3 represents hydrogen or alkyl containing 1 to 6 carbon atoms; L denotes a piperidine derivative or a spiro piperidine derivative; Are1 represents phenyl or substituted phenyl; Are2 represents naphthalenyl; phenyl or substituted phenyl; and Het denotes a monocyclic or bicyclic heterocycle; wherein each monocyclic and bicyclic heterocycle may optionally be substituted on a carbon atom; N-oxide form thereof, pharmaceutically acceptable addition salt or a stereochemically isomeric form. The above-described derivative that is P substance antagonist can be used as a medicament. Also disclosed are a process and intermediate for its preparation as well as a pharmaceutical composition containing thereof and process for its preparation.
机译:在本发明中,公开了通式I的1-(1,2-二取代的哌啶基)-4-(稠合的咪唑)哌啶衍生物,其中n为0、1或2; m为1或2,如果m为2,则n为1; = Q代表= O或= Nre3-; X表示共价键或-O-,-S-,-NRe3-; Re1代表在烷基部分中含有1至6个碳原子的Are1,Are1烷基或在烷基部分中具有1至6个碳原子的二(Are1)烷基,其中每个烷基任选地被取代; Re2代表Are2;在烷基部分中具有1至6个碳原子的芳基烷基,在烷基部分中具有Het或具有1至6个碳原子的杂烷基; Re3代表氢或含1-6个碳原子的烷基; L表示哌啶衍生物或螺哌啶衍生物。 Are1代表苯基或取代的苯基; Are2代表萘基;苯基或取代的苯基; Het表示单环或双环杂环;其中每个单环和双环杂环可任选地在碳原子上被取代;其N-氧化物形式,药学上可接受的加成盐或立体化学异构形式。作为P物质拮抗剂的上述衍生物可以用作药物。还公开了其制备方法和中间体以及包含其的药物组合物和其制备方法。

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