ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "БИОФАРМ-МЕМОРЕЙН";TKACHENKO, ;OBSCHESTVO S OGRANICHENNOY OTVETSTVENNOSTJU "BIOPHARM-MEMORIEN";NENAYDENKO, Vаlеntin Gеоrgiеviсh;НЕНАЙДЕНКО, Валентин Георгиевич
发明人:
NENAYDENKO, Vаlеntin Gеоrgiеviсh,НЕНАЙДЕНКО, Валентин Георгиевич,TKACHENKO, Sergey Evgenievich,ТКАЧЕНКО, Сергей Евгеньевич,BACHURIN, Sergey Olegovich,БАЧУРИН, Сергей Олегович,KABAKOV, Vladimir Evgenie
申请号:
RURU2011/000662
公开号:
WO2012/030258A1
申请日:
2011.08.30
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
The invention relates to a novel class of non-peptide heterocyclic low-molecular peptide mimetics of secretory amyloid precursor protein (sAPP mimetics) capable of acting effectively upon the processes of the formation, storage and regeneration of normal and pathological memory. The compounds can also be used for studying (in vitro and in vivo) biochemical signaling, neurotrophic and neuroprotective processes related to the secretory protein sAPP and for studying the mechanisms of the formation, storage and regeneration of memory. Specifically, the invention relates to (azaheterocyclyl)alkyl derivative amides of 2-(het)arylglycines of general formula (I) in which: n and m can have the values 0, 1, 2 and 3; the symbol (#) here and hereinafter signifies the possible presence of a chiral centre; R represents optionally substituted C5-C10aryl or a 5-7-membered hetaryl containing 1-3 heteroatoms selected from nitrogen, oxygen and sulphur and optionally condensed with a benzene ring; A1 and A2 independently represent an optionally substituted, 3-7-membered, saturated, partially saturated or aromatic azaheterocycle which contains from 1 to 3 atoms of nitrogen in the cycle and is optionally condensed with a benzene ring; or their pharmaceutically acceptable salts or alkyl esters in the form of individual optical isomers, or combinations thereof.L'invention concerne une nouvelle classe de mimétiques peptidiques hétérocycliques de faible masse moléculaire de nature non peptidique de la protéine précurseur sécrétoire de l'amyloïde (mimétiques de sAPP) qui sont capables d'agir efficacement sur les processus de formation, mémorisation et régénération de la mémoire normale et pathologique. Les composés de l'invention peuvent également être utilisés dans l'étude (in vitro et in vivo) de la signalisation biochimique, des processus neurotrophiques et neuroprotecteurs liés à sAPP par la protéine sécrétoire et dans l'étude de mécanismes de formation, mémorisation et régénération de la