ЗИМОН Вернер (DE),ЛУТЦ Кристиан (DE),МЮЛЛЕР Кристоф (DE),АНДЕРЛЬ Ян (DE)
申请号：
RU2013145314/04
公开号：
RU2013145314A
申请日:
2012.03.09
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
1. amatoksina conjugate of formula (I) wherein: R1 is H or OH R2 is H or OH R3 is NHili OH R4 is OH or OCalkil R5 is LT, where L is a linker and T means target binding fragment.2. Amatoksina The conjugate of claim 1, wherein the linker is coupled to a target-binding fragment through fragment mocheviny.3. Amatoksina The conjugate of claim 2, wherein the target binding moiety to the linker L is coupled via an amino group that is available in the target binding moiety wherein said amino moiety forms a portion of said mocheviny.4. Amatoksina The conjugate of claim 1, wherein the linker has a length of from 1 to 8 carbon atoms, including from 1 to 6 atoms, more particularly from 1 to 4 carbon atoms and most specifically of from 2 to 4 atomov.5. Amatoksina The conjugate of claim 2, wherein the linker has a length of from 1 to 8 carbon atoms, including from 1 to 6 atoms, more particularly from 1 to 4 carbon atoms and most specifically of from 2 to 4 atomov.6. Amatoksina conjugate according to any of claims 1-5 wherein the linker L represents an optionally substituted alkylene, heteroalkylene, alkenylene, heteroalkenyl, alkynyl, geteroalkinilen, cycloalkylene, heterocycloalkylene, arylene, heteroarylene, aralkylene, or geteroaralkilenovuyu gruppu.7. Amatoksina conjugate according to any of claims 1-5, wherein linker L comprises a moiety selected from the following fragments: fragment disulfide, ether, amine, ester, carboxamide, urethane and mocheviny.8. Amatoksina The conjugate of claim 1, wherein the target binding moiety binds specifically to an epitope which is present on the tumor cells, including those wherein the target binding moiety binds specifically to an epitope of epithelial cell adhesion molecule (EpCAM) .9. Amatoksina The conjugate of claim 2, wherein the target binding fragments1. Конъюгат аматоксина формулы (I)где:R1 означает H или OHR2 означает H или OHR3 означает NH2 или OHR4 означает OH или OC1-6 алкил иR5 означает L-T, где L означает линкер и T означает
