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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),ЭЛЬ ШЕЙХ Шериф (DE),БАЙЕР Рудольф (DE),БРУДЕР Зандра (DE),ШТЕЛЬТЕ-ЛЮДВИГ Беатрикс (DE),ИОРИССЕН Ханна (DE),МАЛЕРТ Кристоф (DE),ГРЕВЕН Зимоне (DE),ПЕТРУЛЬ Хайке (DE),ШУМАХЕР Иоах
申请号:
RU2013151599/04
公开号:
RU2013151599A
申请日:
2012.04.20
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. Conjugate binding compound-an active compound of the general formula (Ia) wherein n is a number from 1 to 50, AK is a linking compound, preferably a chimeric humanized or human antibody, particularly preferably an EGFR antibody, a group of g-L1-B-L2 -g represents a linker, where g denotes a point of attachment to the group AK, and ߧ denotes a point of attachment to the nitrogen atom, D represents a group of formula # b Teal, 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- indol-3-ylmethyl, or R and R together with the carbon atom to which they are attached form (1S, 2R) -2-phenylcyclopropane-1, 1-diyl of formula #################################################################################################################################### & lt hydrogen, hydroxy or benzyloxy, R3 is hydrogen or methyl, R3 is isobutyl, sec-butyl, t-butyl, phenyl, benzyl, 1-hydroxyethyl, 4-hydroxybenzyl, 4-hydroxyl-3-nitrobenzyl, 4-hydroxyl -3-aminobenzyl, 1-phenylethyl, diphenylmethyl, 1H-imidazol-4-ylmethyl or 1H-indole-3-ylmethyl, or R and R together with the carbon atom to which they are attached form (1S, 2R) -2-phenylcyclopropane -1,1-diyl of formula ################################################################################################################# ring A present thereon with NO group is a mono- or bicyclic heterocycle optionally containing substituents 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-indole 3-ylmethyl, or R and R together with the carbon atom to which they are attached form a (1S, 2R) -2-phenyl-cyclopropane-1,1-diyl formula wherein # denotes
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