HUBSCHWERLEN, Christian;ACTELION PHARMACEUTICALS LTD;GUDE, Markus;PANCHAUD, Philippe
发明人:
GUDE, Markus,HUBSCHWERLEN, Christian,PANCHAUD, Philippe
申请号：
IBIB2012/051473
公开号：
WO2012/131588A1
申请日:
2012.03.28
申请国别(地区):
IB
年份:
2012
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.L'invention concerne des dérivés de 3-uréidoisoquinoléin-8-yle de formule I, dans laquelle R1 est alkyle, haloalkyle ou cyclopropyle ； R2 est H, halogène, pyridazin-4-yle, pyrimidin-5-yle ou un groupe facultativement substitué de pyridin-3-yle, pyridin-4-yle ou phényle ； R3 est alkyle, alcynyle, aminoalkyle, carbamoylalkyle, méthyl-carbamoylalkyle, alcoxy, haloalcoxy, alcynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, diméthylaminoalcoxy, carbamoylalcoxy, alkylamino, cycloalkyle, cycloalkylalkyle, cycloalkylalcoxy, hydroxyalkyle, hydroxyalcoxy, alcoxyalkyle, alcoxyalcoxy, carboxyalkyle, carboxyalcoxy, alcoxycarbonylalcoxy
