A series of 3-(arylalkyl)-2,4,5-trioxoimidazolidine-1-acids (1) was prepared and tested for aldose reductase (AR) and aldehyde reductase (ALR) inhibitory activities. These compounds showed strong inhibitory activity against AR without significant inhibitory activity for ALR. The ratio of IC50(ALR)/IC50(AR) was > 1000 in some compouds. On the basis of pharmacological tests such as the recovery of reduced motor nerve conduction velocity and toxicological profile, 3-(3-nitrobenzyl)-2,4,5-trioxoimidazolidine-1-acid (NZ-314) was selected as the candidate for clinical development.
[EN] GUANIDINE COMPOUNDS AND USE THEREOF<br/>[FR] COMPOSÉS DE GUANIDINE ET LEUR UTILISATION
申请人:HANALL BIOPHARMA CO LTD
公开号:WO2015160220A1
公开(公告)日:2015-10-22
The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.
New amino-alkyl-amide derivatives as CCR3 receptor ligands
申请人:PAPPNE BEHR Agnes
公开号:US20080280961A1
公开(公告)日:2008-11-13
The invention relates to a compound of the general formula (I),
as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound.
The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
Amino-alkyl amide derivatives as CCR3 receptor ligands
申请人:Sanofi-Aventis
公开号:US08044078B2
公开(公告)日:2011-10-25
The invention relates to a compound of the general formula (I),
as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
Compounds and methods for inhibition of HIV and related viruses
申请人:Medivir Aktiebolag
公开号:EP0540143A2
公开(公告)日:1993-05-05
Treatment of Aids, inhibition of the replication of HIV and related viruses, and formulations using thiourea derivative compounds or salts thereof are disclosed. Also disclosed are novel thiourea compounds.
公开了治疗艾滋病、抑制 HIV 和相关病毒复制以及使用硫脲衍生物化合物或其盐的制剂。还公开了新型硫脲化合物。
AMIDOMALONAMIDES AND THEIR USE AS INHIBITORS OF MATRIX METALLOPROTEINASE