FERGUNSON, RONALD,SANDERS, JOHN M.,COLEMAN, PAUL J.,YU, TAO,STAMFORD, ANDREW,WADDELL, SHERMAN TIM,ZHANG, YONGLIAN,WAI, JOHN S.
申请号:
PE0004012016
公开号:
PE05012016A1
申请日:
2014.09.26
申请国别(地区):
PE
年份:
2016
代理人:
摘要:
Quinolizina refers to compounds of formula (i), or pharmaceutically acceptable salts of the same, where X is a single link, piridilo, furanilo, tienilo, pirimidinilo, oxazolilo, thiazolyl pirrolilo NHC (,, OR), among others and it is a simple link or alquileno c1\u2013c3 R1 is aril Or c6\u2013c10, piridilo, furanilo, tienilo, pirimidinilo, oxazolilo thiazolyl pirrolilo indolilo,,,,Bencimidazolilo, quinolinilo, among others c1\u2013c6 R2 is H, alkyl, N or o 2 (R11), among others c1\u2013c6 R3 is H, alkyl, N or o 2 (R11), among others c1\u2013c6 R4 is H, alkyl, N or o 2 (R11), among others, with the condition R4 H that is different from at least one of R2 and R3 is N (R11) 2 R5 is H, C1\u2013c6 alkyl, N or o 2 (R11), among others.Under the condition that R5 H is different from at least one of R2 and R3 is N (2 R9 R11) is H, alkyl c1\u2013c6, haloalquilo c1\u2013c6, hidroxialquilo c1\u2013c6, among others c1\u2013c6 R10 is H, alkyl, haloalquilo c1\u2013c6, hidroxialquilo c1\u2013c6, among others and R11 is H, alkyl c1\u2013c6 2\u2013alqui, S (o) The c1\u2013c6, C (o) \u2013alquilo c1\u2013c6, among others.It also relates to pharmaceutical compositions comprising compounds of formula (i) quinolizina or pharmaceutically acceptable salts of the same. These compounds act as inhibitors of HIV integrase, which are 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 cua