Potential anxiolytic agents. 2. Improvement of oral efficacy for the pyrido[1,2-a]benzimidazole (PBI) class of GABA-A receptor modulators
摘要:
We have further explored the structure-activity relationships of pyrido[1,2-a]benzimidazole (PBI) derivatives (viz. prototype 1), a novel series of central GABA-A receptor modulators, with the intent of enhancing oral efficacy. A study involving the introduction of acidic or basic groups led to the identification of RWJ-38293 (3a) as a potential anxiolytic agent.
Van Beek,L.K.H. et al., Recueil des Travaux Chimiques des Pays-Bas, 1968, vol. 87, p. 737 - 745
作者:Van Beek,L.K.H. et al.
DOI:——
日期:——
PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING DEGENERATIVE BRAIN DISEASE COMPRISING MULTI-TARGETING COMPOUNDS
申请人:UNIST Academy-Industry Research Corporation
公开号:US20160243059A1
公开(公告)日:2016-08-25
A pharmaceutical composition for treating or preventing a degenerative brain disease, the pharmaceutical composition including, as an active component, a multi-targeting compound for further improving treatment efficiency of a degenerative brain disease such as Alzheimer's disease is disclosed. The pharmaceutical composition includes a compound represented by Formula 1 or 2, wherein the compound of Formula 1 or 2 induces a gathering of amyloid-peptides in a manner of toxicity-free aggregation under conditions both in the presence and absence of metals such as copper and zinc, and also reacts with multiple targets of Alzheimer's diseases at once to inhibit toxicity thereof, the multiple targets including amyloid-peptide, metal-amyloid-peptide, a metal, and an activated oxidizing species. The pharmaceutical composition including the compound of Formula 1 or 2 may be utilized as a therapeutic agent or a health food in regard to a brain disease, including Alzheimer's disease.
US6316605B1
申请人:——
公开号:US6316605B1
公开(公告)日:2001-11-13
[EN] PHENOTHIAZIN DERIVATIVES FOR ANTIVIRAL TREATMENTS<br/>[FR] DÉRIVÉS DE PHÉNOTHIAZINE CONÇUS POUR DES TRAITEMENTS ANTIVIRAUX
申请人:PROSETTA CORP
公开号:WO2008124550A1
公开(公告)日:2008-10-16
[EN] Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C. [FR] L'invention propose des composés et des méthodes de prévention et de traitement d'infections virales. Dans certains modes de réalisation, de nouveaux composés à activité antivirale à large spectre sont proposés. Dans des modes de réalisation plus spécifiques, les composés et les procédés sont efficaces contre des virus tels que l'encéphalite équine du Venezuela, le virus du Nil occidental et l'hépatite C.