FLYGARE, John A.,GUNZNER-TOSTE, Janet L.,PILLOW, Thomas,HOWARD, Philip Wilson,MASTERSON, Luke
申请号：
ES12780356
公开号：
ES2556584T3
申请日:
2012.10.12
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A conjugate of formula (A): ** Formula ** dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3； R2 is independently selected from H, OH,>； = O,>； = CH2, CN, R, OR,>； = CH-RD,>； = C (RD) 2, O-SO2-R, CO2R and COR, and optionally additionally select from halo or dihalo； wherein RD is independently selected from R, CO2R, COR, CHO, CO2H, and halo； R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR ', NO2, Me3Sn and halo； R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR ', NO2, Me3Sn and halo； And between a simple link and a group of formulas A1 or A2: ** Formula ** where N shows where the group joins the N10 of the PBD portion； RL1 and RL2 are independently selected from H and methyl, or together with the carbon atom to which they are attached they form a cyclopropylene group； CBA represents a cell binding agent； Q is independently selected from O, S and NH； R11 is H or R or, where Q is O, SO3M, where M is a metal cation； R and R 'are each independently selected from C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups, and optionally in relation to the NRR', R and R 'group together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring of 4, 5, 6 or 7 members； wherein R12, R16, R19 and R17 are as defined for R2, R6, R9 and R7, respectively； wherein R "is a C3-12 alkylene group, the chain of which may be interrupted by one or more heteroatoms, for example, O, S, N (H), NMe and / or aromatic rings, for example, benzene or pyridine, rings which are optionally substituted； X and X 'are independently selected from O, S and N (H).Un conjugado de fórmula (A):**Fórmula** las líneas de puntos indican la presencia opcional de un doble enlace entre C1 y C2 o C2 y C3； R2 se selecciona independientemente entre H, OH, >；=O, >；=CH2, CN, R, OR, >；=CH-RD, >；=C(RD)2, O-SO2-R, CO2R y COR, y opcionalmente se selecciona adicionalmente de halo o
