WILSON, FRANCIS XAVIER,JOHNSON, PETER DAVID,VICKERS, RICHARD,STORER, RICHARD,WYNNE, GRAHAM MICHAEL,ROACH, ALAN GEOFFREY,DE MOOR, OLIVIER,DORGAN, COLIN RICHARD,DAVIS, PAUL JAMES
申请号：
ES09795514
公开号：
ES2537059T3
申请日:
2009.12.01
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
A compound of formula (I): ** Formula ** in which: L1 is a direct bond； each of R1 and R2 is independently selected from H and optionally substituted C1-6 alkyl, aryl, heteroaryl, carbocyclyl and heterocyclyl, the optional substitution being with one or more substituents selected from halo, CN, NO2, R6, OR6, N ( R6) 2, COR6, CO2R6, SO2R6, NR7COR6, NR7CO2R6, NR7SO2R6, NR7CONR6R7, CONR6R7 and SO2NR6R7, provided that at least one of R1 and R2 is cyclic； Each R5 is independently selected from H, halo, C1-6 alkyl, OR7, N (R7) 2, CN and NO2； each of X1 and X2 is independently selected from N and CR3； X3 is selected from NR4, O and S； X4 is NH； and R3 is selected from H, halo and C1-6 alkyl； R4 is selected from H and C1-6 alkyl； R6 is selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C4-C7 carbocyclyl, C4-C7 heterocyclyl and 5- or 6-membered aryl or heteroaryl, any of which may be optionally substituted with one or more halo atoms； and R7 is selected from hydrogen and C1-C4 alkyl, any of which is optionally substituted with one or more halo atoms； or a pharmaceutically acceptable N-oxide, salt, hydrate or solvate thereof for use in a method of treating: infection with Clostridium difficile or disease associated with Clostridium difficile (CDAD) selected from: (a) colitis； (b) pseudomembranous colitis； and (c) diarrhea caused by Clostridium difficile.Un compuesto de fórmula (I): **Fórmula** en la que: L1 es un enlace directo； cada uno de R1 y R2 se selecciona independientemente entre H y alquilo C1-6 opcionalmente sustituido, arilo, heteroarilo, carbociclilo y heterociclilo, siendo la sustitución opcional con uno o más sustituyentes seleccionados entre halo, CN, NO2, R6, OR6, N(R6)2, COR6, CO2R6, SO2R6, NR7COR6, NR7CO2R6, NR7SO2R6, NR7CONR6R7, CONR6R7 y SO2NR6R7, con la condición de que al menos uno de R1 y R2 sea cíclico； Cada R5 se selecciona independientemente entre H, halo, alquilo C1-6, OR7, N(R7)2, CN y NO2； cada uno de X1 y X2 se selecciona independientemen
