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C-3 modified betulinic acid derivatives as inhibitors of HIV maturation
专利权人:
VIIV Healthcare UK (No.5) Limited
发明人:
REGUEIRO-REN, Alicia,SWIDORSKI, Jacob,LIU, Zheng,MEANWELL, Nicholas A.,SIT, Sing-Yuen,CHEN, Jie
申请号:
ES11726563
公开号:
ES2612452T3
申请日:
2011.06.02
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound, including pharmaceutically acceptable salts and prodrug esters and prodrug ethers thereof, a compound selected from the group of: a compound of formula I ** Formula ** a compound of formula II ** Formula ** a compound of formula III ** Formula ** in which R1 is isopropenyl or isopropyl; J and E are -H or -CH3; E is absent when double bond is present; X is a phenyl or heteroaryl ring substituted with A, in which A is at least one member selected from the group of -H, -halo, -hydroxy, -C 1-6 alkyl, -C 1-6 alkoxy, -C 1-6 alkyl 6, -NR2R2, -COOR2, -C (O) NR2R2, -C (O) NR2SO2R3, -SO2NR2R2, -NR2SO2R2, -cycloalkyl C1-6-COOR2, -alkenyl C1-6-COOR2, -alkyl C1-6- COOR2, -C1-6 alkyl-COOR2, -NHC (O) (CH2) n-COOR2, -SO2NR2C (O) R2, -tetrazol, and -cyclic heteroaryl-COOR2, in which R2 is H, -C1 alkyl 6 or -C1-6 substituted alkyl and in which R3 is C1-6 alkyl and additionally in which n>; = 1-6; Y is selected from the group of -COOR2, -C (O) NR2R2, -C (O) NR2SO2R3, C {O) NR2SO2NR2R2, -NR2SO2R2, -SO2NR2R2, -C1-6-COOR2 alkyl, -C1-6 alkenyl , -C 1-6 alkyl-COOR2, -C 1-6 alkyl-COOR2, -NHC (O) (CH2) n-COOR2, -SO2NR2C (O) R2, -tetrazol, -CONHOH, -cyclic heteroaryl-COOR2 and -B (OH) 2, in which n>; = 1-6; and Z is selected from the group of -COOH, -COOR4 and -CH2OH, wherein R4 is C1-6 alkyl or C1-6 alkylphenyl.Un compuesto, incluyendo sales farmacéuticamente aceptables y ésteres de profármacos y éteres de profármacos del mismo, compuesto que se selecciona del grupo de: un compuesto de fórmula I**Fórmula** un compuesto de fórmula II**Fórmula** un compuesto de fórmula III**Fórmula** en las que R1 es isopropenilo o isopropilo; J y E son -H o -CH3; E está ausente cuando está presente el doble enlace; X es un anillo de fenilo o heteroarilo sustituido con A, en los que A es al menos un miembro seleccionado del grupo de -H, -halo, -hidroxilo, -alquilo C1-6, -alcoxi C1-6, -haloalquilo C1-6, -NR2R2,-COOR2, -C(O)NR2R2, -C(O)NR2SO2R3, -SO2NR2R2, -NR2SO2R2, -cicloalquil C1-6-COOR2, -alq
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