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Monomethylvaline compounds that have modifications of the phenylalanine side chain at the C-terminus
专利权人:
Inc.;Seattle Genetics
发明人:
DORONINA, Svetlana,KLINE, Toni
申请号:
ES06786489
公开号:
ES2585357T3
申请日:
2006.07.07
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound having the formula: ** Formula ** or a pharmaceutically acceptable salt or solvate thereof, wherein: R2 is selected from the group consisting of H and C1-C8 alkyl; R3 is selected from the group consisting of H, C1-C8 alkyl, C3-C8 carbocycle, aryl, C1-C8 alkylaryl, X1- (C3-C8 carbocycle), C3-C8 heterocycle and X1- (C3-C8 heterocycle) ; R4 is selected from the group consisting of H, C1-C8 alkyl, C3-C8 carbocycle, aryl, X1-aryl, C1-C8- alkyl (C3-C8 carbocycle), C3-C8 heterocycle and X1- (C3- heterocycle C8); R5 is selected from the group consisting of H and methyl; or R4 and R5 together form a carbocyclic ring and have the formula - (CRaRb) n- in which Ra and Rb are independently selected from the group consisting of H, C1-C8 alkyl and C3-C8 carbocycle and n is selected from the group consisting of 2, 3, 4, 5 and 6; R6 is selected from the group consisting of H and C1-C8 alkyl; R7 is selected from the group consisting of H, C1-C8 alkyl, C3-C8 carbocycle, aryl, X1-aryl, X1- (C3-C8 carbocycle), C3-C8 heterocycle and X1- (C3-C8 heterocycle); each R8 is independently selected from the group consisting of H, OH, C1-C8 alkyl, C3-C8 carbocycle and O- (C1-C8 alkyl); each X1 is independently C1-C10 alkylene; the remainder -NR9Z1 is a phenylalanine bioistero with a modified amino acid side chain wherein the phenylalanine bioisocyte moiety ** Formula ** is where R9 is H; R10 is benzyl; R11 is H; Z2 is CO2H; subindice n is an integer from 0 to 2; and the subindice or is an integer from 0 to 2 on condition that n + or at least 1.Un compuesto que tiene la formula:**Fórmula** o una sal o un solvato farmaceuticamente aceptables del mismo, en la que: R2 se selecciona entre el grupo que consiste en H y alquilo C1-C8; R3 se selecciona entre el grupo que consiste en H, alquilo C1-C8, carbociclo C3-C8, arilo, alquilarilo C1-C8, X1- (carbociclo C3-C8), heterociclo C3-C8 y X1-(heterociclo C3-C8); R4 se selecciona entre el grupo que consiste en H, alquilo C1-C8, carbociclo C3-C8, a
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