SWIDORSKI, JACOB,MEANWELL, NICHOLAS A.,REGUEIRO-REN, ALICIA,SIT, SING-YUEN,CHEN, JIE,CHEN, YAN
申请号:
PE0012792014
公开号:
PE23152014A1
申请日:
2013.02.13
申请国别(地区):
PE
年份:
2015
代理人:
摘要:
Referring to a triterpenoid Compound of formula (i), (ii), (iii) or (iv) where R1 is isopropenilo or isopropyl J and e are H or CH3 X is a cycloalkyl c4-c8, cicloalquenilo c4-c8, among others and it is coor2, nhso2nr2r2, C (o) among others, R2 is H, alkyl of C1 - C6, among others R3 is C1 - C6 alkyl option Nally replaced R4 is H, alkyl of C1 - C6, among others R5 is H, alkyl of C1 - C6, among others.Preferred compounds are: acid, 6 - ((1R, 3aS, 5aR, 5br, 7aR, 11aS, 11BR, 13ar, 13br) - 5a, 5b, 8,8,11a - 1 - (prop - 1 - - 2 (IL -) - 3 - (2 - (N - trifluoro - fenilmetilsulfonamido) ethyl) amino) - 2,3,3a, 4,5,5a, 5b, 6,7,7a, 8,11a, 11b, 12,13,13a, octadecahidro 13b - [A] - 1H - ciclopentan crisen - 9 - il) spiro [3.3] hept-3-ene - 5 - - 2.2 - dicarboxilico acid, 3 - ((1R, 3aS, 5aR, 5br, 7aR, 11aS, 11BR, 13ar, 13br) - 3 - ((2 - (1.1 - dioxidotiomorfolino) ethyl) amino) - 5a, 5b, 8,8,11a - 1 - (propo - 1 - 2 - yl) - 2,3,3a, 4,5,5a, 5b, 6,7,7a, 8,11a, 11b, 12,13,13a, octadecahidro 13b - [A] - 1H - ciclopentan crisen - 9 - il) Bicyclo [3.1.0] hex - 2 - 6 - carboxylic acid, Among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of HIV maturation and are useful in the treatment of AIDSREFERIDA A UN COMPUESTO TRITERPENOIDE DE FORMULAS (I), (II), (III) O (IV), DONDE R1 ES ISOPROPENILO O ISOPROPILO J Y E SON H O CH3 X ES UN CICLOALQUILO C4-C8, CICLOALQUENILO C4-C8, ENTRE OTROS Y ES COOR2, C(O)NHSO2NR2R2, ENTRE OTROS R2 ES H, ALQUILO C1-C6, ENTRE OTROS R3 ES ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO R4 ES H, ALQUILO C1-C6, ENTRE OTROS R5 ES H, ALQUILO C1-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 6-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-5a,5b,8,8,11a-PENTAMETIL-1-(PROP-1-EN-2-IL)-3a-((2-1,1,1-TRIFLUORO-N-FENILMETILSULFONAMIDO)ETIL)AMINO)-2,3,3a,4,5,5a,5b,6,7,7A,8,11a,11b,12,13,13a,13b-OCTADECAHIDRO-1H-CICLOPENTAN[a]CRISEN-9-IL)SPIRO[3.3]HEPT-5-EN-2,2-DICARBOXILICO, ACIDO 3-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-((2-(1,1-DIOXIDOT