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专利权人:
ACTELION PHARMACEUTICALS LTD
发明人:
CHRISTIAN HUBSCHWERLEN,MARKUS GUDE,PHILIPPE PANCHAUD
申请号:
MX2013011253
公开号:
MX2013011253A
申请日:
2012.03.28
申请国别(地区):
MX
年份:
2013
代理人:
摘要:
The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I I wherein R is alkyl, haloalkyl or cyclopropyl; R 2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R 3 is alkyl, alkynyl, aminoalkyl, carbamoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, dimethylaminoalkoxy, carbamoylalkoxy, alkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxy, carboxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxy, 2-cyanoethoxy, 2,3-dihydroxypropoxy, 3,4-dihydroxybutoxy, -CH 2 R a, -CH 2 CH 2 R b, -(CH 2 ) n -C(O)O-R d, -(CH 2 ) n -N(R c )C(O)O-R d, -O-(CH 2 ) n -N(R c )C(O)O-R d, -(CH 2 ) n -R e or -O-(CH 2 ) n -R e; R a is cyano, acetylamino or N,N-dimethylamino; R b is cyano or carbamoyl; R c is H or methyl; R d is alkyl; R e is pyrrolidin-1-yl, piperidin-1-yl, piperidin-3-yl, morpholin-1-yl, 2-oxopyrrolidin-1-yl, 5-oxopyrrolidin-2-yl, 2,5-dioxopyrrolidin-1-yl, 2-oxoimidazolidin-1-yl, 4-(tert-butoxycarbonyl)piperazin-1-yl, 4-(aminomethyl)cyclohexyl or heteroaryl; R 4 is H or methyl; and to the salts of such compounds. These compounds are useful for the prevention or the treatment of bacterial infections.La invención se refiere a derivados de 3-ureidoisoquinolin-8-ilo de la fórmula I; (Ver Formula) en donde R1 es alquilo, haloalquilo o ciclopropilo; R2 es H, halógeno, piridazin-4-ilo, pirimidin-5-ilo o un grupo piridin-3-ilo, piridin-4-ilo o fenilo opcionalmente sustituido; R3 es alquilo, alquinilo, aminoalquilo, carbamoiloalquilo, metilcarbamoiloalquilo, alcoxi, haloalcoxi, alquiniloxi, (4-hidroxibut-2-in-1-iI)oxi, (4-aminobut-2-in-1-il)ox i, dimetilaminoalcoxi, carbamoiloalcoxi, alquilamino, cicloalquilo, cicloalquilalquilo, cicloalquilalcoxi, hidroxialquilo, hiroxialcoxi, alcoxialquilo, alcoxialcoxi, carboxialquilo, carboxialcoxi, alco
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