首页> 外国专利> Compounds derived from N - Oxides and piridilmetilpiperazina - piperidine; Preparation Method, Pharmaceutical Composition and use for the treatment of Parkinson's disease, anxiety, Aggression,Autism, dizziness, depression, cognitive impairment

Compounds derived from N - Oxides and piridilmetilpiperazina - piperidine; Preparation Method, Pharmaceutical Composition and use for the treatment of Parkinson's disease, anxiety, Aggression,Autism, dizziness, depression, cognitive impairment

机译:衍生自N-氧化物和piridilmetilpiperazina-哌啶的化合物;制备方法,药物组合物以及用于治疗帕金森氏病,焦虑症,攻击性,自闭症,头晕,抑郁,认知障碍的用途

摘要

The invention concerns N-oxides of certain pyridylmethylpiperazine and -piperidine derivatives as alternatives or as `prodrugs' of their respective parent compounds, to pharmaceutical compositions containing these N-oxides, to methods for preparing them, and methods for preparing compositions. The invention relates to N-oxides of compounds having formula (a), wherein the symbols have the meanings given in the description, and wherein the oxidized nitrogen atom may be the nitrogen atom in the pyridyl ring of RSUB5/SUB, or the nitrogen atom in the piperidine ring (when Z is carbon) or either one of the nitrogen atoms in the piperazine ring (when Z is nitrogen), or bóth the nitrogen atom connected to RSUB5/SUB via a methylene group, ánd the nitrogen atom in the pyridyl ring of RSUB5/SUB, and tautomers, stereoisomers, pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to the uses of such N-oxides and compositions, particularly for the manufacture of a medicament useful in the treatment of affections or diseases of the central nervous system caused by disturbances in either the dopaminergic or serotinergic systems, for example Parkinson's disease, aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition or memory and in particular schizophrenia and other psychotic disorders.
机译:本发明涉及某些吡啶基甲基哌嗪和-哌啶衍生物的N-氧化物作为其各自母体化合物的替代物或“前药”,涉及包含这些N-氧化物的药物组合物,其制备方法,以及制备组合物的方法。本发明涉及具有式(a)的化合物的N-氧化物,其中符号具有说明书中给出的含义,并且其中氧化的氮原子可以是R 5 ,或哌啶环中的氮原子(当Z为碳时)或哌嗪环中的氮原子之一(当Z为氮时),或与R 5 连接的氮原子通过一个亚甲基,R 5 的吡啶基环中的氮原子及其互变异构体,立体异构体,药理学上可接受的盐,水合物和溶剂化物。本发明还涉及这种N-氧化物和组合物的用途,特别是用于制造可用于治疗由多巴胺能或血清素能系统紊乱引起的中枢神经系统疾病或疾病的药物,例如帕金森氏病。 ,攻击性,焦虑症,自闭症,眩晕,抑郁,认知或记忆障碍,尤其是精神分裂症和其他精神病。

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