Two short series of compounds with 1H‐indole skeleton, bearing hydantoin and piperazine nuclei respectively, were synthesized. Some compounds of these two series were tested for their calcium‐antagonistic activity on K+‐depolarized smooth muscle (rabbit auricolar artery and guinea‐pig taenia caeci) and their negative inotropic action on atrial muscle from guinea‐pig hearts.
合成了两个具有 1H-吲哚骨架的短系列化合物,分别带有乙内酰脲和哌嗪核。测试了这两个系列中的一些化合物对 K + 去极化平滑肌(兔耳廓动脉和豚鼠绦虫)的钙拮抗活性及其对豚鼠心脏心房肌的负性肌力作用。
Antagonists, their preparation and use
申请人:Novo Nordisk A/S
公开号:US05783575A1
公开(公告)日:1998-07-21
The present invention relates to therapeutically active non competitive antagonists, acting selectively at the metabotropic glutamate receptor. The novel compounds are useful in treating diseases in the central nervous system by modulating synaptic transmission via the metabotropic glutamate receptor.
[EN] HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND USE<br/>[FR] COMPOSES HETEROCYCLIQUES, LEUR PREPARATION ET LEUR UTILISATION
申请人:NOVO NORDISK A/S
公开号:WO1995025110A1
公开(公告)日:1995-09-21
(EN) The present invention relates to therapeutically active heterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system related to the metabotropic glutamate receptor system.(FR) Composés hétérocycliques à action thérapeutique, leur procédé d'élaboration, et compositions pharmaceutiques comprenant de tels composés. Ces nouveaux composés se révèlent utiles pour le traitement des maladies du système nerveux central liées au système récepteur du glutamate métabotrope.