TANG, Bing-Yu,FU, Jianmin,GIRIJAVALLABHAN, Vinay M.,OLSEN, David B.,ZHANG, Zhibo
申请号：
PE0018162016
公开号：
PE01972017A1
申请日:
2015.03.26
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Describes 4 substituted nucleoside Derivatives of formula (i) as inhibitors of HIV reverse transcriptase, prophylaxis and Treatment of HIV infection, prophylaxis, Treatment and delay in the onset or progression of AIDS AIDS and \/ or more complex (ARC). Where: R is one of formula (i), (ii), etc. X is o, S, etc. and - CN, etc. r1 h, - C (o) R6, etc. R2 is H, - C (o) r6a, etc. R3 is H, F is H or Oh alkyl R4, R5 C1 - C6, etc. C1 - C6 is H, alkyl, etc. and R6 are r6a C1 - C6 h, alkyl, etc. M is 0 OR 1 R9 is H, Halo, etc.Preferred compounds are (2R, 3S, 5R) - 5 - (4 - amino - 5 - fluoro - 7h pyrrolo [2,3-d] pyrimidine 7 - il - 2 - ethinyl) - 2 - (hydroxymethyl) tetrahydrofuran-3-yl ol (2R, 3S, 5R) - 5 - (4 - amino - 2 - chlorine - 7h pyrrolo [2,3-d] pyrimidin-2-yl) - 7 - il - 2 - ethinyl - 2 - (hydroxymethyl) tetrahydrofuran-3-yl ol among othersDescribe derivados de nucleosidos 4´ sustituidos de formula (I) como inhibidores de la transcriptasa reversa de VIH, profilaxis y tratamiento de infeccion por VIH, profilaxis, tratamiento y retraso en la aparicion o progresion de SIDA y/o complejo realcionado al SIDA (ARC). Donde: R es uno de formula i), ii), etc. X es O, S, etc. Y es -CN, etc. R1 H, -C(O)R6, etc. R2 es H, -C(O)R6a, etc. R3 es H, F u OH R4 es H, alquilo C1-C6, etc. R5 es H, alquilo C1-C6, etc. R6 y R6a son H, alquilo C1-C6, etc. m es 0 o 1 R9 es H, halo, etc. Son compuestos preferidos: (2R,3S,5R)-5-(4-amino-5-fluoro-7H-pirrolo[2,3-d]pirimidin-7-il)-2-etinil-2-(hidroximetil)tetrahidrofuran-3-ol (2R,3S,5R)-5-(4-amino-2-cloro-7H-pirrolo[2,3-d]pirimidin-7-il)-2-etinil-2-(hidroximetil)tetrahidrofuran-3-ol entre otros
