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DÉRIVÉS DE 3-URÉIDOISOQUINOLÉIN-8-YLE
专利权人:
Actelion Pharmaceuticals Ltd.
发明人:
申请号:
EP12715438.3
公开号:
EP2691373A1
申请日:
2012.03.28
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 is alkyl, haloalkyl or cyclopropyl; R2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R3 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, —CH2Ra, —CH2CH2Rb, —(CH2)n—C(O)O—Rd, —(CH2)n—N(Rc)C(O)O—Rd, —O—(CH2)n—N(Rc)C(O)O—Rd, —(CH2)n—Re or —O—(CH2)n—Re; Ra is cyano, acetylamino or N,N-dimethylamino; Rb is cyano or carbamoyl; Rc is H or methyl; Rd is alkyl; Re 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; R4 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, alcoxyal
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