BURGESS, Antony Wilks,WALKER, Francesca,WATSON, Keith Geoffrey,WITCHARD, Helen,LESSENE, Guillaume
申请号：
ES11835350
公开号：
ES2621932T3
申请日:
2011.10.27
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A compound of Formula I, or a pharmaceutically acceptable salt, hydrate and / or prodrug thereof, wherein: ** Formula ** E and G are each independently selected from the group consisting of C1-4alkyl- , -NH-, -N (C1-4alkyl) -, -O- and, in any orientation, -NH-C1-4alkyl-, -N (C1-4alkyl) -C1-4alkyl- and -O -C1-4alkyl-； y is a simple link； K is independently selected from CH and N, and J is independently selected from NH and CH2； R1 and R2 are each 0-2 substituents where each substituent is independently selected from the group consisting of -C1-4alkyl, -OH, -O-C1-4alkyl, -N (R4) 2, -C1alkyl -4N (R415) 2, -NO2, halogen and CF3； each R4 is independently selected from the group consisting of -H, -OH, -C1-4alkyl, -C (O) O C1-4alkyl, and -C (O) R8, provided that if an R4 is -OH then the other R4 cannot be -OH； or -N (R4) 2 forms a pyrrolidinyl, piperidinyl, piperazinyl or morpholino group optionally substituted with methyl； R5 is selected from the group consisting of -C1-4alkyl and phenyl； R3 is selected from the group consisting of H, -C1-4alkyl, aryl, and alkylaryl； and wherein said prodrug is selected from (i) a compound in which an amino acid residue or a polypeptide chain of two or more amino acid residues are covalently linked to a free amino, hydroxyl or carboxylic acid group of the compound of formula I, (ii) a compound in which a carbonate, a carbamate, an amide, or an alkyl ester are covalently linked to a free amino, hydroxyl, or carboxylic acid group of the compound of formula I through the side chain of the carbonyl carbon prodrug or (iii) a compound comprising a phosphate derivative of a compound of formula I linked through a phosphorous-oxygen bond to a free hydroxyl of the compounds of formula I； wherein the phosphate derivative is a phosphate acid, a salt of a phosphate acid, or a phosphate ester.Un compuesto de Fórmula I, o una sal, un hidrato y/o un profármaco farmacéuticamente aceptables del mismo, en la que:**Fórmula** E y G se seleccionan cada uno ind
