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НОВЫЕ КОНЪЮГАТЫ СВЯЗЫВАЮЩЕЕ СОЕДИНЕНИЕ - АКТИВНОЕ СОЕДИНЕНИЕ (ADC) И ИХ ПРИМЕНЕНИЕ
专利权人:
СИЭТЛ ДЖЕНЕТИКС; ИНК. (US)
发明人:
ЛЕРХЕН Ханс-Георг (DE),ЛИНДЕН Ларс (DE),ЭЛЬ ШЕЙХ Шериф (DE),ВИЛЛУДА Йорг (DE),КОПИТЦ Шарлотте Кристине (DE),ШУМАХЕР Иоахим (DE),ГРЕВЕН Зимоне (DE),МАЛЕРТ Кристоф (DE),ШТЕЛЬТЕ-ЛЮДВИГ Беатрикс (DE),ГОЛЬ
申请号:
RU2013151600/04
公开号:
RU2013151600A
申请日:
2012.04.20
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. A conjugate binding compound - an active compound of general formula (Ia) where n is a number from 1 to 50, AK is a binding compound, the group §-GLBL-§§ is a linker gde§ denotes the binding point with a group of AK i§ § indicates binding point with the nitrogen atom, D represents a group of formula wherein # denotes the binding point with the nitrogen atom, R is hydrogen or methyl, R is isobutyl, sec-butyl, tert-butyl, phenyl, benzyl, 1-hydroxyethyl, 4-hydroxybenzyl 4-hydroxy-3-nitrobenzyl, 4-hydro xylo-3-aminobenzyl, 1-phenylethyl, diphenylmethyl, 1H-imidazol-4-ylmethyl or 1H-indol-3-ylmethyl, iliRi together with the carbon atom to which they are attached form a (1S, 2R) -2-phenyl- cyclopropane-1,1-diyl formula wherein # denotes the binding point with the adjacent nitrogen atom, # Denotes the binding point to the carbonyl group, the ring A to present thereon a group of NO is a mono-or bicyclic, optionally containing substituents heterocycle of formula wherein # denotes the point of binding to the carbonyl group, R is hydrogen, hydroxy or benzyloxy, R is hydrogen or methyl, R is isobutyl, sec-butyl, tert-butyl, phenyl, benzyl, 1-hydroxyethyl, 4-hydroxybenzyl, 4-hydroxy-3-nitrobenzyl, 4-hydroxy-3-aminobenzyl, 1-phenylethyl, diphenylmethyl, 1H-imidazol 4-ylmethyl or 1H-indo L-3-ylmethyl, iliRi together with the carbon atom to which they are attached form a (1S, 2R) -2-phenyl-cyclopropane-1,1-diyl formula wherein # denotes the binding point with the adjacent nitrogen atom, # denotes the point of binding to group T Tpredstavlyaet a group of formula -C (= O) -OR, -C (= O) -NRR, -C (= O) -NH-NH-R or -CH-OR,
来源网站:
中国工程科技知识中心
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