ГЕРЛАВЭ Венсан (US),ЭЛКИН Карл (US),НЭШ Хью М. (US),СОЙЕР Томи К. (US),ГРЕЙВЗ Брэдфорд Дж. (US),ФЕФАН Эрик (US)
申请号：
RU2014137107
公开号：
RU2014137107A
申请日:
2013.02.14
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. peptidomimetic macrocycle comprising an amino acid sequence that is at least about 60% identical to the amino acid sequence selected from the group consisting of amino acid sequences in Table 1, Table 1a, Table 1b and Table 1c, where the peptidomimetic macrocycle has the formula: Formula ( I) or a pharmaceutically acceptable salt thereof, wherein: each a, C, D, and E independently represent an amino acid each B is an amino acid ,, [-NH-L-CO-], [-NH-L-SO-] or [-NH-L -] are independently each represent -H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroalkyl, or heterocycloalkyl, unsubstituted or substituted by halogen or at least one of R Robrazuetformiruyuschy macrocycle linker L , coupled to the alpha position of one of said D or E amino acid each is hydrogen, alkyl, alkenyl, alkynyl, arylalkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, tsikloaril or geterotsikloaril optionally substituted with R each L and L independently represents a linker which forms a macrocycle -LL- formula, each L and L and Lnezavisimo represent alkylene, alkenylene, alkynylene, heteroalkylene, cycloalkylene, heterocycloalkylene, tsikloarilen, geterotsikloarilen or [-RKR- ], each optionally substituted with R each Rpredstavlyaet alkylene, alkenylene, alkynylene, heteroalkylene, cycloalkylene, heterocycloalkylene, arylene or heteroarylene, each K is O, S, SO, SO, CO, CO, or CONR each independently represents halogen alkyl, -OR, -N (R), -SR, -SOR, -SOR, -COR, fluorescent moiety, a radioisotope or a therapeutic agent each independently represents -H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalk
