FERGUNSON, RONALD,SANDERS, JOHN M.,COLEMAN, PAUL J.,YU, TAO,STAMFORD, ANDREW,WADDELL, SHERMAN TIM,ZHANG, YONGLIAN,WAI, JOHN S.
申请号:
PE2016000401
公开号:
PE20160501A1
申请日:
2014.09.26
申请国别(地区):
PE
年份:
2016
代理人:
摘要:
It refers to compounds extracted from formula (I) or acceptable in pharmacology, where x is a simple link, pyridine, furan, smallpox, pyridine, oxazolilo, tiazolyl, pyridine, NHC (o),among others; Y is a single bond or C1-C3 alkylene; R1 is C6-C10 aryl, pyridyl, furanyl, thienyl, pyrimidinyl, oxazolyl, thiazolyl, pyrrolyl, indolyl, benzimidazolyl, quinolinyl, among others; R2 is H, C1-C6 alkyl, N (R11) 2 or OH, among others; R3 is H, C1-C6 alkyl, N (R11) 2 or OH, among others; R4 is H, C1-C6 alkyl, N (R11) 2 or OH, among others, with the proviso that R4 is different from H when at least one of R2 or R3 is N (R11) 2; R5 is H, C1-C6 alkyl, N (R11) 2 or OH, among others, with the proviso that R5 is different from H when at least one of R2 or R3 is N (R11) 2; R9 is H, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, among others; R10 is H,C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, among others; and R11 is H, C1-C6 alkyl, S (O) 2-C1-C6 alkyl, C (O) -C1-C6 alkyl, among others. It also refers to pharmaceutical compositions comprising the quinolizine-derived compounds of formula (I) or pharmaceutically acceptable salts thereof. These compounds act as inhibitors of HIV integrase, making them useful in the treatment of HIV infection.Se refiere a compuestos derivados de quinolizina de formula (I) o sales farmaceuticamente aceptables de los mismos, donde X es un enlace sencillo, piridilo, furanilo, tienilo, pirimidinilo, oxazolilo, tiazolilo, pirrolilo, NHC(O), entre otros; Y es un enlace sencillo o alquileno C1–C3; R1 es arilo C6–C10, piridilo, furanilo, tienilo, pirimidinilo, oxazolilo, tiazolilo, pirrolilo, indolilo, bencimidazolilo, quinolinilo, entre otros; R2 es H, alquilo C1–C6, N(R11)2 u OH, entre otros; R3 es H, alquilo C1–C6, N(R11)2 u OH, entre otros; R4 es H, alquilo C1–C6, N(R11)2 u OH, entre otros, con la condicion de que R4 es diferente de H cuando al menos uno de R2 o R3 es N(R11)2; R5 es H, alquilo C1–C6, N(R11)2 u OH, entre otros, con la condicion de q