RUF Sven (DE),РУФ Свен (DE),PERNERSHTORFER Jozef (DE),ПЕРНЕРШТОРФЕР Йозеф (DE),SADOVSKI Torsten (DE),САДОВСКИ Торстен (DE),KHORSTIK Georg (DE),ХОРСТИК Георг (DE),SHROJDER German (DE),ШРОЙДЕР Герман (D,RUF Sven,РУФ Свен,PERNERSHTORFER Jozef,ПЕРНЕРШТОРФЕР Йозеф,SADOVSKI Torsten,САДОВСКИ Торстен,KHORSTIK Georg,ХОРСТИК Георг,SHROJDER German,ШРОЙДЕР Герман,BUNING Kristian,БУНИНГ Кристиан,VIRT Klaus,ВИРТ
申请号：
RU2014106999
公开号：
RU0002617843C2
申请日:
2012.07.25
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formulas Iaand Ib,in any of its stereoisomeric form or its physiologically acceptable salt, where G R71-O-C(O)-； R1 represents hydrogen； R2 represents hydrogen； R10 represents R11； R11 represents Ar； R30 is selected from the group including a (C3-C7)-cycloalkyl and R32-CuH2u-, where u means an integer chosen from the series containing 0, 1, 2 and 3； R32 represents a phenyl, optionally substituted by one or more identical or different substituents selected from the group comprising a halogen, a (C1-C6)-alkyl, R33 and (C1-C6)- alkyl-O-； R33 is a phenyl optionally substituted by one substitute selected from a halogen； R40 is selected from the group consisting of hydrogen and (C1-C4)-alkyl, or R30 and R40 together represent (CH2)x, where x is an integer selected from the group comprising 2, 3, 4 and 5； R50 is hydrogen； R60 is hydrogen； R71 is hydrogen； Ar, independently of each other Ar group, is selected from the group comprisng a phenyl and an aromatic 5-membered or 6-membered monocyclic heterocycle containing one or two heteroatoms selected from nitrogen and attached via a ring carbon atom, where the phenyl and the heterocycle all are optionally substituted by one or more identical or different substituents selected from the group comprising a halogen, a (C1-C6)-alkyl, (C1-C6) alkyl-O- and CF3； where all the alkyl substituents, independently from each other and independently of any other substituents, are optionally substituted by one or more fluorine atoms. The invention also relates to obtaining the compound of formulas Ia and Ib, or a physiologically acceptable salt thereof, that is prepared by reacting a compound of formula IIa or IIb with the compound. The compound of formulas Ia and Ib or its physiologically acceptable salt is intended for use as a pharmaceutical agent having the inhibitory activity against cathepsin A.EFFECT: substituted derivatives of the 3-thiazoleaminepropionic acid as protease
