СЕНТЕР Питер (US),АЛЛЕЙ Стефен (US),БЕНДЖАМИН Деннис (US)
申请号：
RU2013109415/15
公开号：
RU2013109415A
申请日:
2011.08.05
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
1. A method of inhibiting fucosylation of proteins in a mammal, comprising administering to said mammal an effective amount of a fucose analog selected from the group consisting of one of the following formulas (V) or (VI): or a biologically acceptable salt or solvate of the analog, where each of formulas (V ) or (VI) may represent an alpha or beta anomer, or a corresponding aldose form； each of R, R, R, R, R and R is independently selected from the group consisting of —OH, —OC (O) H, —OC ( O) C-C1-6alkyl, -OC (O) C-Salkenyl, -OC (O) C-C1-6alkynyl, -OC (O) aryl, -OC (O) heterocycle, -OC ( ) C-Salkylene (aryl), -OC (O) C-Salkenylene (aryl), -OC (O) C-Salkynylene (aryl), -OC (O) C-Salkylene (heterocycle), -OC (O) C -Salkenylene (heterocycle), -OC (O) C-C1-6 alkynylene (heterocycle), -OOCOS (O) alkyl, -OOCOS (O) O alkyl, OOCOS (O) aryl, -OOCOS (O) O aryl, -OC ( O) CHO (CHCHO) CH, -OC (O) CHCHO (CHCHO) CH, -O-tri-C-C1-6alkylsilyl, -OC-C1-6alkyl, and a small electron withdrawing group, where each n represents an integer independently selected from 0-5 ； R represents a member selected from the group consisting of —CH, —CHX, —CHX, —CH (X ′) —C-C1-6alkyl unsubstituted or substituted by a halogen atom, —CH (X ′) —C-Salken, unsubstituted one or substituted by a halogen atom, —CH (X ′) —C-Salkine, unsubstituted or substituted by a halogen atom, —CH = C (R) R), —C (CH) = C (R) (R), —C ( R) = C = C (R) (R), -C-carbocycle unsubstituted or substituted with methyl or halogen atom, -CH (X ') - C-carbocycle unsubstituted or substituted with methyl or halogen atom, -C3 heterocycle unsubstituted or substituted by methyl or a halogen atom, —CH (X ′) - a heterocycle unsubstituted or substituted by a methyl or halogen atom, —CHN, —CHCHN and benzyloxymethyl, or R is a small electron withdrawing group； where R represents a hydrogen atom1. Способ ингибирования фукозилирования белков у млекопитающего, включающий введение указанному млекопитающему эффективного количества аналога фукозы, выбран
