公开(公告)号：US20070275977A1

公开(公告)日：2007-11-29

申请号：US11743049

申请日：2007-05-01

申请人： Marcel Van Aar ,  Peter Van Amsterdam ,  Gerrit Barf ,  Johan Bakker ,  Cathaline Den Besten ,  Arnoldus Herremans ,  Jan Zorgdrager

发明人： Marcel Van Aar ,  Peter Van Amsterdam ,  Gerrit Barf ,  Johan Bakker ,  Cathaline Den Besten ,  Arnoldus Herremans ,  Jan Zorgdrager

IPC分类号： A61K31/496 ,  C07D405/14

CPC分类号： C07D405/12

摘要： N-oxides of certain pyridylmethylpiperazine and -piperidine derivatives are provided as alternatives to or as “prodrugs” of their respective parent compounds, as well as pharmaceutical compositions containing these N-oxides, methods for preparing them, and compositions comprising them. The N-oxides have the formula (a) wherein the substituents have the meanings given in the description, and wherein the oxidized nitrogen atom can be the nitrogen atom in the pyridyl ring of R5, 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 both the nitrogen atom connected to R5 via a methylene group, and the nitrogen atom in the pyridyl ring of R5, and tautomers, stereoisomers, pharmacologically acceptable salts, hydrates, and solvates thereof. In addition, the N-oxides and compositions can be used as medicaments useful in the treatment of affections or diseases of the central nervous system caused by disturbances in either the dopaminergic or serotinergic systems.

摘要翻译： 提供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“前体药物”的替代物或含有这些N-氧化物的药物组合物，其制备方法和包含它们的组合物。 N-氧化物具有式（a），其中取代基具有本说明书中给出的含义，其中氧化的氮原子可以是R 5的吡啶环中的氮原子，或氮 哌啶环中的一个原子（当Z为碳时）或哌嗪环中的氮原子之一（当Z为氮时），或通过亚甲基与R 5连接的氮原子， 和R 5的吡啶环中的氮原子，以及互变异构体，立体异构体，药理学上可接受的盐，水合物和溶剂化物。 此外，N-氧化物和组合物可以用作治疗由多巴胺能或血清素能系统中的紊乱引起的中枢神经系统的情感或疾病的药物。

公开(公告)号：US20070043059A1

公开(公告)日：2007-02-22

申请号：US11504050

申请日：2006-08-15

申请人： Theodorus Koopman ,  Hendrik Koster ,  Peter Van Amsterdam ,  Roelof Feenstra ,  Marinus Verhage ,  Andrew McCreary ,  Mayke Hesselink ,  Gustaaf Van Scharrenburg

发明人： Theodorus Koopman ,  Hendrik Koster ,  Peter Van Amsterdam ,  Roelof Feenstra ,  Marinus Verhage ,  Andrew McCreary ,  Mayke Hesselink ,  Gustaaf Van Scharrenburg

IPC分类号： A61K31/496 ,  A61K31/4545 ,  A61K31/454 ,  C07D413/14 ,  C07D413/04

CPC分类号： C07D263/58 ,  C07D413/04

摘要： The present disclosure relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The disclosure also relates to the use of the compounds for the manufacture of a medicament giving a beneficial effect. The disclosure also relates to the use of the compounds for the manufacture of a medicament for treating or preventing a disease or condition. The disclosure further relates to the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

摘要翻译： 本公开内容涉及某些哌嗪和哌啶衍生物的N-氧化物以及这些化合物的制备方法。 本公开还涉及该化合物在制备产生有益效果的药物中的用途。 本公开还涉及化合物在制备用于治疗或预防疾病或病症的药物中的用途。 本发明还涉及中枢神经系统疾病的治疗，特别是焦虑症的治疗，包括广泛性焦虑障碍和恐慌症，强迫症，侵略，成瘾（包括渴望），抑郁症，孤独症，眩晕，精神分裂症等精神病 疾病，帕金森病和认知和记忆障碍。 化合物具有通式（1），其中符号具有说明书中给出的含义。