АНДЕРЛЬ Ян (DE),ЗИМОН Вернер (DE),МЮЛЛЕР Кристоф (DE)
申请号：
RU2013119960/15
公开号：
RU2013119960A
申请日:
2011.09.29
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
1. A conjugate comprising a linking target, a moiety connected through linker L to amatoxin, where linker L is connected to amatoxin via (i) the amatoxin amino acid 1 C atom, in particular via an amide bond； (ii) an oxygen atom bound to the C atom of amino acid 3 of the amatoxin, in particular via an ester bond, an ether bond or an urethane bond； or (iii) the 6'-atom C of amino acid 4 of the amatoxin, in particular through the oxygen atom bonded to the 6'-atom C of amino acid 4 of the amatoxin； where in each case the linker L is connected to the part connecting the target via the urea residue. 2. The conjugate according to claim 1, wherein the conjugate has a structure selected from the following structures: (i) amatoxin-γC (O) -NH-L-NH-C (O) -NH- (part linking target)； (ii) amatoxin -δC-O-C (O) -L-NH-C (O) -NH- (part, binding target)； (iii) amatoxin-δC-OL-NH-C (O) -NH- (part, binding target)； (iv) amatoxin-δС-О-С (О) -NH-L-NH-C (О) -NH- (part, binding target) and (v) amatoxin-6'COL-NH-C ( O) -NH- (part, binding target) .3. The conjugate according to claim 1 or 2, wherein the portion linking the target is connected to the linker L via an amino group present in said portion linking the target, wherein said amino group forms part of said urea residue. The conjugate according to claim 1, wherein the amatoxin is selected from α-amanitine, β-amanitine, γ-amanitine, ε-amanitine, amanine, amaninamide, amanullin, or amanullic acid, or their salts or analogues. The conjugate of claim 1, wherein linker L is an alkylene, heteroalkylene, alkenylene, heteroalkenylene, alkynylene, heteroalkynylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene, aralkylene or heteroalkylene group, optionally substituted. The conjugate according to claim 1, where the linker L is on1. Конъюгат, включающий связующую мишень часть, соединенную через линкер L с аматоксином, где линкер L соединяется с аматоксином через(i) γ-атом С аминокислоты 1 аматоксина, в частности через амидную связь；(i
