Ховард, Филип Уилсон,Флайгер, Джон А.,Пиллоу, Томас,Вэй, Биньцин
申请号：
EA201591277
公开号：
EA201591277A1
申请日:
2014.03.13
申请国别(地区):
EA
年份:
2016
代理人:
摘要：
Conjugated compounds of the formula (A) where R is a, and R and R are independently selected from H, F, C saturated alkyl, Salkenyl, and the indicated alkyl and alkenyl groups are optionally substituted by a group, C 1-4 alkyl ether and C 1-6 alkyl ether； or in the case when one of the R and R is H, the other is selected from nitrile and C1-6 alkyl ether； R1 and R4 are independently selected from H, R, OH, OR, SH, SR, NH, NHR, NRR ', NO, MeSn and halogen； R is independently selected from H, R, OH, OR, SH, SR, NH, NHR, NRR ', NO, MeSn, and halogen； Y is selected from formulas A1, A2, A3, A4, A5, and A6: L is a linker attached to a cell-binding agent； CBA is a cell binding agent； n is an integer selected from the range from 0 to 48； R1 is a Calkylene group； or (a) R 2 is H and R 3 is OH, OR, where R 2 is C 1-6 alkyl； or (b) R and R form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are attached； or (c) R5 is H and R4 is OSOM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation； each of R and R ′ is independently selected from an optionally substituted C1-6 alkyl, Superheroclyl and Saryl groups, and optionally with respect to the group NRR ′, R and R ′ together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6 - or a 7-membered heterocyclic ring； where R, R, R, R, R and R are as defined for R, R, R, R, R and R, respectively； where Z represents CH or N； where T and T 'are independently selected from a simple bond or C1-6 alkylene, in the carbon chain of which one or more heteroatoms may be included, for example, O, S, N (H), NMe, provided that the number of atoms in the shortest chain between X and X 'is from 3 to 12 atoms； and X and X 'are independently selected from O, S, and N (H).Конъюгированные соединения формулы (А)где Rпредставляет собой, причем Rи Rнезависимо выбраны из Н, F, Cнасыщенного алкила, Салкенила, причем указанные алкильная и алкенильная группы возможно
