本发明涉及以下式子的取代的imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine衍生物,其中取代基的定义在权利要求书中描述。这类化合物显示出高亲和力和选择性,适用于GABA A α5受体结合位点,可能有用作认知增强剂或用于治疗认知障碍如阿尔茨海默病。
Alkyl substituted triazole compounds as agonists of the APJ Receptor
申请人:AMGEN INC.
公开号:US11191762B2
公开(公告)日:2021-12-07
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: (I), (II) where the definitions of the variables are provided herein.
式 I 和式 II 的化合物、其药学上可接受的盐、前述任何化合物的立体异构体或其混合物是 APJ 受体的激动剂,可用于治疗心血管疾病和其他疾病。式 I 和式 II 的化合物具有如下结构:(I)、(II) 变量的定义见本文。
IMIDAZO BENZODIAZEPINE DERIVATIVES
申请人:F.HOFFMANN-LA ROCHE AG
公开号:EP1937688A1
公开(公告)日:2008-07-02
ALKYL SUBSTITUTED TRIAZOLE COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR
申请人:AMGEN INC.
公开号:US20190290647A1
公开(公告)日:2019-09-26
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: (I), (II) where the definitions of the variables are provided herein.
[EN] The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5- d][1,4]benzodiazepine derivatives of the following formula (I) wherein the definition of substituents is described in the claims. It has been found that this class of compounds show high affinity and selectivity for GABA a5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease. [FR] La présente invention a trait à des dérivés substitués d'imidazo[1,5-a][1,2,4]triazolo[1,5- d][1,4]benzodiazépine de formule (I), dans laquelle les substituants sont tels que définis dans les revendications. On a observé que cette classe de composés présentent une affinité et une sélectivité élevées pour des sites de liaison au récepteur GABA a5 et peuvent être utiles en tant que activateur cognitif ou pour le traitement de troubles cognitifs tels que la maladie d'Alzheimer.