St. Jude Children's Research Hospital;MMV Medicines for Malaria Venture;Rutgers, The State University Of New Jersey
发明人:
GUY, Rodney Kiplin,ZHU, Fangyi,GUIGUEMDE, Wendyam Armand,FLOYD, David,KNAPP, Spencer,STEIN, Philip,CASTRO, Steve
申请号：
ES12772470
公开号：
ES2644082T3
申请日:
2012.08.24
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A compound having a structure represented by a formula: ** (See formula) ** in which Ar1 is monocyclic heteroaryl selected from 3-pyridinyl, 4-isoxazolyl, N-methyl-4-pyrazolyl, 4-pyrazolyl, 4- isothiazolyl, 5-thiazolyl, 5-pyrimidinyl and 4-pyridazinyl； R1 is selected from hydrogen, methyl, ethyl, n-propyl, ipropyl, cyclopropyl, n-butyl, i-butyl, s-butyl, t-butyl and cyclobutyl and, if valence permits, is substituted by 0-3 groups selected from fluoro, chloro, bromo, iodo, cyano, methoxy and ethoxy； R2 and R3 are independently selected from hydrogen, C1-C4 alkyl, C1-C4 alkoxy, cyano, fluoro, chloro, bromo and iodo； wherein the ring substituents on the carbon atoms denoted with the α and β markers have a trans configuration； Ar2 has a structure represented by a formula: ** (See formula) ** in which R4a and R4b are independently selected from hydrogen, fluoro, chloro, bromo, iodo, cyano, C1-C4 alkyl, C1-C4 haloalkyl, polyhaloalkyl C1-C4, C1-C4 alkoxy, C1-C4 haloalkoxy and C1-C4 polyhaloalkoxy； R5 is selected from hydrogen, fluoro, chloro, bromo, iodo, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 polyhaloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy and C1-C4 polyhaloalkoxy； or one of the pharmaceutically acceptable salts, hydrates, solvates or polymorphs thereof, as well as their tautomers, geometric isomers and optically active forms thereof as well as their tautomers, geometric isomers and optically active forms thereof for use in the prevention and / or treatment of malaria.Un compuesto que tiene una estructura representada por una fórmula: **(Ver fórmula)** en la que Ar1 es heteroarilo monocíclico seleccionado entre 3-piridinilo, 4-isoxazolilo, N-metil-4-pirazolilo, 4-pirazolilo, 4-isotiazolilo, 5-tiazolilo, 5-pirimidinilo y 4-piridazinilo； R1 se selecciona entre hidrógeno, metilo, etilo, n-propilo, ipropilo, ciclopropilo, n-butilo, i-butilo, s-butilo, t-butilo y ciclobutilo y, si la valencia lo permite, está sustituido por 0-3 grupos seleccionados entre fluoro, cloro, bromo
