SHTYRLIN, Yurj Grigor'evich,ШТЫРЛИН, Юрий Григорьевич,IKSANOVA, Al'fiya Gabdulakhatovna,ИКСАНОВА, Альфия Габдулахатовна,BADEEV, Yurij Vladimirovich,БАДЕЕВ, Юрий Владимирович,BALAKIN, Konstantin Valer'
申请号：
RURU2017/000809
公开号：
WO2018/084749A1
申请日:
2017.10.31
申请国别(地区):
RU
年份:
2018
代理人:
摘要：
The invention relates to the chemistry of medical compounds, and particularly to a group of chiral conjugates (optically active hybrid molecules) of oligo-ether polyol structure, which are inhibitors of ATP-dependent reverse transporters of cells (OEP inhibitors). An OEP inhibitor is a conjugate having an equimolar ratio of optically active polyoxypropylene hexol and polyoxypropylene glycol. The claimed method by which the conjugate is produced allows the production of a preparation which increases the efficacy of medicines by means of inhibiting the multi-drug resistance mechanisms of cells. The resulting preparation may be used in biology, pharmacology, pharmaceutics, medicine, and agriculture. The OEP inhibitor is produced by hydroxypropylation of a mixture of sorbitol and a bifunctional oxygen-containing compound in the presence of a hydroxide of an alkaline or alkaline earth metal. The bifunctional oxygen-containing compound used may be water, propylene glycol, dipropylene glycol, tripropylene glycol, tetrapropylene glycol, pentapropylene glycol, hexapropylene glycol, heptapropylene glycol or a mixture thereof. The inhibitor is a conjugate of polyoxypropylene glycol having a molecular mass of from 300 to 500 Da and polyoxypropylene hexol having a molecular mass of from 1000 to 1500 Da in an equimolar ratio, with a hydroxyl value within a range of 215-240 mg KOH/g.L'invention concerne la chimie des médicaments et notamment le groupe de conjugués chiraux (molécules hybrides optiquement actives) de nature des oligoétherpolyoles qui sont des inhibiteurs de transporteurs inverses des cellules dépendant des aTP. L'inhibiteur de l'invention est un conjugué présentant un rapport équimolaire d'un polyoxypropylène hexol et d'un polyoxypropylène glycol. Le procédé de l'invention qui permet d'obtenir un conjugué assure la possibilité de production de la préparation qui augmente l'efficacité d'action des médicaments grâce à l'inhibition des mécanismes de résistance multiple
