GUDE, MARKUS,HUBSCHWERLEN, CHRISTIAN,PANCHAUD, PHILIPPE
申请号：
TW101110929
公开号：
TW201249801A
申请日:
2012.03.28
申请国别(地区):
TW
年份:
2012
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.
