ЛЕРХЕН Ханс-Георг (DE),ХАММЕР Штефани (DE),ХАРРЕНГА Аксель (DE),КОПИТЦ Шарлотте Кристине (DE),НИЗИНГ Карл Фридрих (DE),ЗОММЕР Анетте (DE),ШТЕЛЬТЕ-ЛЮДВИГ Беатрикс (DE),МАЛЕРТ Кристоф (DE),ШУМАХЕР Йоахи
申请号：
RU2014128467
公开号：
RU2014128467A
申请日:
2012.12.12
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. A conjugate binding compound - active compound of general formula (Ia) wherein n is a number from 1 to 50, AK denotes a binding compound that binds to FGFR2, group §-GLB-§§ is a linker binding point gde§ denotes a group AK , i§§ binding point represents, with the nitrogen atom Lpredstavlyaet a line (C-C) or represents alkanediyl group formulygdep is a number from 2 to 6, ## denotes the point of binding to the group B, ## denotes the point of binding to the atom nitrogen, wherein (C) may contain from -alkanediyl 1 to 4 substituents selected independently from the group consisting of methyl, hydroxy, and benzyl, and wherein with the two carbon atom chain alkanediyl at position 1,2, 1,3 or 1,4 relative to one another, including any located therebetween carbon atoms, possibly linked to form a (C-C) cycloalkyl ring or phenyl ring, D represents a group of formula where # denotes the point of binding to the nitrogen atom, R is hydrogen or methyl, R is isopropyl, isobutyl, sec- butyl, tert-butyl, phenyl, benzyl, 1-hydroxyethyl, 4-hydroxybenzyl, 4-hydroxy-3-nitrobenzyl, 4-hydroxy-3-aminobenzyl, 1-phenylethyl, di-phenylmethyl, 1H-imidazol-4-ylmethyl or 1H-indol-3-ylmethyl, iliRi Rvmeste with the carbon atom to which they are attached form a (1S, 2R) -2-phenyl-cyclopropane-1,1-diyl group of formula wherein # denotes the binding point with the adjacent nitrogen atom, # denotes the point of binding to the carbonyl group, ring a is present with thereon NO group is a mono- or bicyclic optionally substituted heterocycle of formula where # denotes the point of binding with carbonyl group, R is hydrogen, hydroxy or
