Christian Hubschwerlen;Philippe Panchaud;Markus Gude
发明人:
Markus Gude,Christian Hubschwerlen,Philippe Panchaud
申请号：
US14009093
公开号：
US08889676B2
申请日:
2012.03.28
申请国别(地区):
US
年份:
2014
代理人:
摘要：
The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula IwhereinR1 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.
