CHRISTIAN HUBSCHWERLEN,MARKUS GUDE,PHILIPPE PANCHAUD
申请号：
BR112013024899
公开号：
BR112013024899A2
申请日:
2012.03.28
申请国别(地区):
BR
年份:
2016
代理人:
摘要：
3-Ureidoisoquinolin-8-yl derivatives The present invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 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； R3 is alkyl, alkynyl, aminalkyl, carbomoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl) oxy, (4-aminabut-2-yn-1-yl) oxy , dimethylamin alkoxy, carbamoyl alkoxy, alkylamine, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxycarvoxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxyoxy, 2,3-dioxy , 4-dihydroxybutoxy, -ch ~ 2 ~ r ^ a ^, -ch ~ 2 ~ ch ~ 2 ~ r ^ b ^, - (ch ~ 2 ~) ~ n ~ -c (o) or ^ ~ d ^, - (ch ~ 2 ~) ~ n ~ -n (r ^ c ^) c (o) or ^ d ^, -o- (ch ~ 2 ~) ~ n ~ -n (r ^ c ^) c (o ) or ^ d ^, - (ch ~ 2 ~) ~ n ~ -r ^ e ^ or -o- (ch ~ 2 ~) ~ n ~ -r ^ e ^； R 4a is cyano, acetylamine or n, n-dimethylamine； R3 is cyano or carbamoyl； R 4 is H or methyl； R2 is alkyl； R ^ 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 heterioaryl； R 4 is H or methyl； and to salts of such compounds. These compounds are useful for preventing or treating bacterial infections.derivados de 3-ureidoisoquinolin-8-ila a presente invenção refere-se a derivados de 3-ureidoisoquinolin-8-ila de fórmula i em que r^ 1^ é alquila, haloalquila ou ciclopropila； r^ 2^ é h, halogênio, piridazin-4-ila, pirimidin-5-ila ou um grupo piridin-3-ila, piridin-4-ila ou fenila opcionalmente substituído； r^ 3^ é alquila, alquinila, aminalquila, carbomoilalquila, metilcarbamoilalquila, alcoxi, haloalcoxi, alquiniloxi, (4-hidroxibut-2-in-1-il)oxi, (4-aminabut-2-in-1-il)oxi, dimetilamin alcoxi, carbamoil alcoxi, alquilamina, cicloaalq
