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Tubulisin derivatives
专利权人:
R & D BIOPHARMACEUTICALS GMBH
发明人:
RICHTER, WOLFGANG
申请号:
ES08758446
公开号:
ES2463693T3
申请日:
2008.05.09
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of Formula (IV): ** Formula ** wherein R2 is C1-C4 alkyl, R6 is C1-C6 alkyl, R7 is C1-C6 alkyl, CH2OR19 or CH2OCOR20, wherein R19 is alkyl, especially isopropyl, R20 it is C2-C6 alkenyl, phenyl or CH2-phenyl, R9 is C1-C6 alkyl, R10 is H, OH, O-alkyl or O-acetyl; f is 1 or 2; R11 has the following structure: wherein R21 is H, OH, halogen, NH2, alkyloxy, phenyl, alkyl amino or dialkyl amino; R16 is H or a C1-C6 alkyl group; R17 is CO2H, CO2R18, CONHNH2, OH, NH2, SH or an optionally substituted alkyl, cycloalkyl, heteroalkyl or heterocycloalkyl group, wherein R18 is an optionally substituted alkyl, heteroalkyl or heterocycloalkyl group; and p is 0, 1, 2 or 3; or a pharmacologically acceptable salt, a solvate, a hydrate or a pharmacologically acceptable formulation thereof, wherein the term "optionally substituted" refers to groups, wherein one or more H atoms can be replaced by F, Cl, Br or I, or OH, SH, NH2, NO2 .; the term "optionally substituted" also refers to groups that may be substituted exclusively or additionally with C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 heteroalkyl, C3-C10 cycloalkyl, C2-C9 heterocycloalkyl , C6-C10 aryl, C1-C9 heteroaryl, C7-C12 aralkyl or unsubstituted C2-C11 heteroaralkyl.Un compuesto de Fórmula (IV):**Fórmula** en donde R2 es alquilo C1-C4, R6 es alquilo C1-C6, R7 es alquilo C1-C6, CH2OR19 o CH2OCOR20, en donde R19 es alquilo, especialmente isopropilo, R20 es alquenilo C2-C6, fenilo o CH2-fenilo, R9 es alquilo C1-C6, R10 es H, OH, O-alquilo u O-acetilo; f es 1 ó 2; R11 tiene la siguiente estructura: en donde R21 es H, OH, halógeno, NH2, alquiloxi, fenilo, alquil-amino o dialquil-amino; R16 es H o un grupo alquilo C1-C6; R17 es CO2H, CO2R18, CONHNH2, OH, NH2, SH o un grupo alquilo, cicloalquilo, heteroalquilo o heterocicloalquilo opcionalmente sustituido, en donde R18 es un grupo alquilo, heteroalquilo o heterocicloalquilo opcionalmente sustituido; y p es 0, 1, 2 ó 3; o una sal farmacológicamente aceptable, un solvat
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