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Azaindol Derivatives with a combination of nicotinic acetylcholine receptor partial agonism and inhibition of reuptake of dopamine

机译:含烟碱乙酰胆碱受体部分激动和多巴胺再摄取抑制作用的氮杂吲哚衍生物

摘要

These compounds have a combination of nicotinic acetylcholine receptor partial agonism and inhibition of dopamine reuptake.It also relates to pharmaceutical compositions containing these Compounds, to methods for preparing Compounds, Methods for preparing Intermediates useful for their Synthesis, and Methods for preparing compositions and Uses of such compounds and compositions.Particularly use in Administration to patients to achieve a therapeutic effect in Disorders involving nicotinic receptors and / or dopamine Transporter or that can be treated via the Manipulation of such receptors.Claim 1: azaindol derived Compounds, characterized by the General formula (1), where X, y and Z represent independently N or C, with the condition that the Ring contains at least one n Atom, and not more than 2; M and N are independently either 1 or 0 (Zero), the condition d And when Z and x represents represent Carbon and NitrogenM is 0 (Zero); R2 and R3 are independently Hydrogen, halogen, alkyl alquinilo C1 C1 - 3, - 3, - NH c1-3 alkyl, hydroxyl, alkyl of C1 - 3oxi, or a Group piperidinilo, pirrolidinilo, tetrahidropiridinilo, morfolinilo, azepanilo, 1 - aza Bicyclo [2.2.2] octanilo or 1 - aza Bicyclo [2.2.2] oct - 2 - enilo, or insubstituido or group that is substituted with one or more substituents selected from Halogen, c1-3 alkyl, phenyl or benzyl; R4, R5 and R6 independently represent Hydrogen, halogen, alkyl of C1 - C2 alquinilo 3, - 3, - NH c1-3 alkyl or alkyl, hydroxyl - 3oxi C1, C That exists only when ondicion R4 and R5 only when z = C, c = tautomeros; and,N - Oxides and stereoisomers thereof, and pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomeros, stereoisomers and N - oxides, compounds that have a combination of nicotinic acetylcholine receptor partial agonism and R Nhibicion reuptake of dopamine.
机译:这些化合物具有烟碱型乙酰胆碱受体部分激动和多巴胺再摄取抑制的组合,还涉及含有这些化合物的药物组合物,化合物的制备方法,可用于其合成的中间体的制备方法以及其制备方法和用途特别用于向患者给药以在涉及烟碱样受体和/或多巴胺转运蛋白的疾病中获得治疗效果,或可通过操纵此类受体进行治疗。权利要求1:氮杂吲哚衍生的化合物,其特征为式(1),其中X,y和Z独立地代表N或C,条件是环含有至少一个n原子且不超过2个; M和N独立地为1或0(零),条件d And当Z和x代表碳和氮时M为0(零); R 2和R 3独立地是氢,卤素,烷基Alquinilo C1-3,-3,-NH c1-3烷基,羟基,C1-3oxi的烷基,或哌啶子基,吡咯烷基,四hidiridinilo,morfolinilo,阿塞帕尼洛,1-氮杂双环[2.2.2]辛基或1-氮杂双环[2.2.2] oct-2-烯基,或被一个或多个选自卤素,c1-3烷基,苯基或苄基的取代基取代的取代基或取代基; R 4,R 5和R 6独立地表示氢,卤素,C 1 -C 2烷基喹啉3,-3--NH c1-3烷基或烷基,羟基-3 oxi C 1,C仅在符号R 4和R 5仅在z = C时存在,c =互变异构体;以及,N-的氧化物和立体异构体,以及所述式(1)化合物及其互变异构体,立体异构体和N-氧化物的药理学上可接受的盐,水合物和溶剂化物,这些化合物具有烟碱性乙酰胆碱受体部分激动和R Nhibicion再摄取的组合多巴胺。

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