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N-Pyrrolidin-3YL-Amide Derivatives As Serotonin and Noradrenalin Re-Uptake Inhibitors

机译:N-吡咯烷酮-3YL-酰胺衍生物作为5-羟色胺和去甲肾上腺素的再摄取抑制剂

摘要

A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1 is H, C1-6alkyl, —C(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8allkyl, C1-8alkoxy, OH, halo, CF3, OCHF2, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; A is S or O; D is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; R2 represents aryl1 or het1, each of which is substituted by at least one substituent independently selected from B, provided that when R2 is substituted by halo then it is also substituted with at least one other substituent independently selected from B other than halo; B represents aryl2, het2, Oaryl2, Ohet2, Sarl2, Shet2, SC1-6alkyl, halogen, CHF2, OCHF2, CF2CF3, CH2CF3, CF2CH3, aryl2-C1-4alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl, C3-6cycloalkylC1-4alkoxy, C3-6cycloalkyl-O—C1-4 alkyl, C3-6cycloalkyl-C1-4alkoxy-C1-4alkyl, OC3-6cycloalkyl, SC3-6cycloalkyl; wherein the aryl2 and het2 groups are optionally substituted by at least one group selected from C1-6alkyl, C3-6cycloalkyl, C1-6alkoxy, OC3-6cycloalkyl, halo, CN, OH, CF3, CHF2, OCF3, OCHF2, hydroxyC1$alkyl, C1-4alkoxy-C1-4alkyl, SC1-6alkyl and SCF3; n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre; R3 is H, C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, aryl3, het3, aryl3-C1-4alkyl or het3-C1-4alkyl, wherein the C3-8cycloalkyl, aryl3 or het3 groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, CN, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; at each occurrence aryl, aryl1, aryl2 and aryl3 independently represent phenyl, naphthyl, anthracyl or phenanthryl; het1 represents an aromatic 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to an aryl group; at each occurrence het, het2, and het3 independently represents an aromatic or non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6membered heterocycle which contains at least one N, O or S heteroatom.;
机译:式(I)的化合物及其药学和/或兽医学可接受的衍生物,其中:R 1 是H,C 1-6 烷基,-C(A)D ,C 3-8 环烷基,芳基,het,芳基-C 1-4 烷基或het-C 1-4 烷基,其中环烷基,芳基或het基团任选地被至少一个独立地选自C 1-8 烷基,C 1-8 烷氧基,OH,卤素,CF 3 ,OCHF 2 ,OCF3,SCF 3 ,羟基-C 1-6 烷基,C 1- 4 烷氧基-C 1-6 烷基和C 1-4 烷基-SC 1-4 烷基; A是S或O; D是H,C 1-6 烷基,芳基,杂基,芳基-C 1-4 烷基或杂-C 1-4 烷基; R 2 表示芳基 1 或het 1 ,其中每个均被至少一个独立地选自B的取代基取代,条件是当R < Sup> 2 被卤素取代,然后还被至少一个独立的选自卤素以外的其他取代基取代; B代表芳基 2 ,het 2 ,芳基 2 ,Ohet 2 ,Sarl 2 ,Shet 2 ,SC 1-6 烷基,卤素,CHF 2 ,OCHF 2 ,CF 2 CF 3 ,CH 2 CF 3 ,CF2CH 3 ,芳基 2 -C 1-4 烷基,C 3-6 环烷基,C 3-6 环烷基-C 1- 4 烷基,C 3-6 环烷基C 1-4 烷氧基,C 3-6 环烷基-OC 1-4 烷基,C 3-6 环烷基-C 1-4 烷氧基-C 1-4 烷基,OC < Sub> 3-6 环烷基,SC 3-6 环烷基;其中芳基 2 和het 2 基团任选地被选自C 1-6 烷基,C 3中的至少一个取代-6 环烷基,C 1-6 烷氧基,OC 3-6 环烷基,卤素,CN,OH,CF 3 , CHF 2 ,OCF 3 ,OCHF 2 ,羟基C 1 $烷基,C 1-4 < / Sub>烷氧基-C 1-4 烷基,SC 1-6 烷基和SCF 3 ; n为1或2,条件是当n为1时,m为0或1且当n为2时,m为0,其中如果m为0,则*表示手性中心; R 3 是H,C 1-6 烷基,C 3-8 环烷基,C 3-8 环烷基C 1-6 烷基,芳基 3 ,het 3 ,芳基 3 -C 1-4 < / Sub>烷基或het 3 -C 1-4 烷基,其中C 3-8 环烷基,芳基 3 或het 3 基团任选被至少一个独立选自C 1-6 烷基,C 1-6 烷氧基的取代基取代, CN,OH,卤素,CF 3 ,OCF 3 ,SCF 3 ,羟基-C 1-6 烷基,C 1-4 烷氧基-C 1-6 烷基和C 1-4 烷基-SC 1-4 < / sub>烷基;在每次出现时,芳基,芳基 1 ,芳基 2 和芳基 3 独立地表示苯基,萘基,蒽基或菲基; het 1 表示芳香的5或6元杂环,其中至少含有一个N,O或S杂原子,可与芳基稠合。在每次出现het,het 2 和het 3 时,分别代表一个芳香族或非芳香族的4、5或6元杂环,其中至少包含一个N, O或S杂原子,其任选稠合至5或6元碳环基团或包含至少一个N,O或S杂原子的第二4、5或6元杂环。

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