Inhibitors of integrase of human immunodeficiency virus: pirimidinona cyclic compounds

摘要

Refers to a compound of formula I, wherein R1 is (AR1) - (C1 - C6 alkyl; R2 is H, alkyl of C1 - C6, o, o - (C1 - C6 alkyl); AR1 is; R3 is H, Halo, Hydroxy, cyano, among others; R4 is H, Halo, c1-c6 alkyl, cyano, among others; Halo R5 is H, alkyl, Hydroxy, C1 - C6, among others; X - y - Z is C (R8) CH2 (R9) CH2 C (R8), ch2ch2ch2ch2 (R9), C (R8) OCH2 (R9), among others, R8 and R9, taken together, are ch2ch2,Ch2ch2ch2, ch2ch2ch2ch2, among others.Preferred compounds are: N - [(4-fluorophenyl) methyl] - 7 ', 8' - 3 '- hydroxy Dihydro 4 oxo spiro [ciclopentan - 1.9' 6 '(H) - [4H] pirido [1,2-a] pyrimidin-2-yl] - 2 - (n' - carboxamide; phenylmethyl) - 7 ', 8' - dhidro - 3 '- hydroxy - 4' - oxo spiro [ciclobutan - 1.9 '6' (H) - [4H] pirido [1,2-a] pyrimidin-2-yl] - 2 '- carboxamide; n - [4 - [2 - (metilsulf fluoro Oil) phenyl] methyl] - 2,3,5,6,6 hexahidro ', 7' - 3 '- hydroxy - 4' - oxo spiro [4H Piran - 4.9 - (4 '' - pirimido [2, H)1 - C] [1,4] oxazin] - 2 '- carboxamide; among others. Also referred to a Pharmaceutical composition. These compounds are inhibitors of HIV integrase, useful in the treatment of AIDS