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COMPUESTOS PEPTÍDICOS ÚTILES COMO AGENTES ANTIBACTERIANOS
专利权人:
UNIVERSIDAD DE BARCELONA
发明人:
RABANAL ANGLADA, FRANCESC,RABANAL ANGLADA, Francesc,CAJAL VISA, YOLANDA,CAJAL VISA, Yolanda,GARCIA SUBIRATS, MARIA,GARCIA SUBIRATS, Maria,RODRIGUEZ NUNEZ, MONTSERRAT,RODRÍGUEZ NÚÑEZ, Montserrat
申请号:
ESES2011/070153
公开号:
WO2011/110716A3
申请日:
2011.03.09
申请国别(地区):
WO
年份:
2012
代理人:
摘要:
The invention relates to peptide compounds that can be used as antibacterial agents, said compounds having formula (I), in which: R0 is branched (C8-C11) alkyl, CH3-(CH2)m-, CH3-O-(CH2CH2O)2CH2- or phenyl-(CH2)x- m = 6-10 x = 1-3 R1, R3, R4, R7 and R8 are selected independently from the formula GF-(CH2)n-, with n = 1-4 and GF = -NH2 or -NH-C(=NH)-NH2 R2 is -CH(CH3)(OH), -CH(CH3)2, -CH2NH2 or -CH2OH R5 and R6 are selected independently from H, linear or branched -(C1-C4) alkyl, -(CH2)-R10, -CH2-CH2-S-CH3 and -CH-(CH3)-OH R9 is CONH2, -CH(CH3)(OH) or CONHR11 R10 is phenyl, 3-indolyl, 4-imidazolyl, 4-hydroxyphenyl, α- or β-naphthyl or 2-, 3- or 4-pyridyl R11 is a specific peptide sequence u is CH2 or S v is NH or S w is CH2 or CO provided that when R9 is CONH2, then (a) R5 or R6 is -CH(CH3)(OH), or (b) R5 and R6 are H or (c) the configuration of C bonded to R9 is S, or (d) the configuration of C bonded to R5 is R and provided that when R9 is CH(CH3)OH, then R8 is GF(CH2)n wherein n is 3 and GF is NH-C(=NH)-NH2, and R7 is GF(CH2)n wherein n is 2 and GF is NH2. These compoundshave been found to be useful in the treatment of bacterial infections.Los compuestos de formula (I), donde: R0 es (C8-C11)-alquilo ramificado, CH3-(CH2)m-, CH3-O-(CH2CH2O)2CH2-, o fenil-(CH2)x- m = 6-10 x = 1-3 R1, R3, R4, R7, y R8 se seleccionan independientemente de la formula GF-(CH2)n- con n = 1-4 y GF = -NH2 o -NH-C(=NH)-NH2 R2 es -CH(CH3)(OH), -CH(CH3)2, -CH2NH2 o -CH2OH R5 y R6 se seleccionan independientemente entre H, -(C1-C4)-alquilo lineal o ramificado, -(CH2)-R10, -CH2-CH2-S-CH3 y -CH-(CH3)-OH R9 es CONH2, -CH(CH3)(OH) o CONHR11 R10 es fenilo, 3- indolilo, 4-imidazolilo, 4-hidroxifenilo, α o β-naftilo o 2-, 3- o 4-piridilo R11 es una secuencia peptidica especifica u es CH2 o S v es NH o S w es CH2 o CO con la condicion de que cuando R9 es CONH2, entonces (a) R5 o R6 es -CH(CH3)(OH), o (b) R5 y R6 son H o (c) la configuracion del C unido a R9 es S o (d) la configuracion del C unido a R5 e
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