SHUDOK Manfred (DE),ШУДОК Манфред (DE),VAGNER Mikhel (DE),ВАГНЕР Михель (DE),BAUER Armin (DE),БАУЕР Армин (DE),KOLMANN Anna (DE),КОЛЬМАНН Анна (DE),SHUDOK Manfred,ШУДОК Манфред,VAGNER Mikhel,ВАГНЕР Михель,BAUER Armin,БАУЕР Армин,KOLMANN Anna,КОЛЬМАНН Анна
申请号：
RU2012144638
公开号：
RU0002621695C2
申请日:
2012.10.19
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: biotechnology.SUBSTANCE: invention relates to formula (I) compounds and physiologically acceptable salts thereof, which provide inhibitory activity against K, B and S cathepsins. In formula (I), partial cycles and , each independently from each other, are selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, dioxolane, 1,3-dioxolane and piperidine, wherein the two partial cycles are unsubstituted； X is a covalent bond； Y is -C(O)-； Z is -N(R26)-(C(R24)(R25))m-CN； R26 represents a hydrogen atom； m is integer 1； R24 and R25, and the carbon atom to which they are attached, form a cycloalkyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, which is unsubstituted； R1 represents a hydrogen atom； R2 and R3 are the same or different and each independently represents a hydrogen atom or -(C0-C3)-alkylene-C-(R27)(R28)(R29)； R27 represents a hydrogen atom, -(C1-C9)-alkyl, -(C0-C4)-alkylene-(C3-C6)-cycloalkyl； R28 and R29 are identical or different and independently represent a hydrogen atom, -(C1-C4)-alkyl； or R28 and R29 with the carbon atom to which they are attached, form -(C3-C6)-cycloalkyl； or R2 and R3 with the carbon atom to which they are attached, form a three to six member cycloalkyl, which is unsubstituted. The invention also relates to methods for formula (I) compounds preparation, methods for preparation of physiologically acceptable salts and N-oxides thereof, medicament containing them, and formula (I) compounds application for the manufacture of a medicament for prophylaxis, prevention and treatment of diseases, related to inhibitory activity against K, B and S cathepsins.EFFECT: higher efficiency of compounds application.10 cl, 2 tbl, 105 exИзобретение относится к соединениям формулы (I) и их физиологически приемлемым солям, которые обладают ингибирующей активностью в отношении катепсинов K, B и S. В формуле (I) частичные циклы и , каждый независимо друг от друга, выбирают из гр
