LI, JIM,SCHOENFELD, RYAN CRAIG,TAYGERLY, JOSHUA PAUL GERGELY,DE VICENTE FIDALGO, JAVIER,TALAMAS, FRANCISCO XAVIER
申请号：
PE0020422011
公开号：
PE09372012A1
申请日:
2010.06.08
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Refers to a compound of formula (i) wherein: x1, X2, X3 and X4 are each n, CR5 r1 is pyridinyl, 1,2 Dihydro 2 - oxo - pyridin - 3 - ilo 3 - oxo - 3,4-dihydro - pirazin thiocyanatoacetate, 2 - oxo - tetrahydro - piperidin yl - 1, among others R2 is H, alkyl alkoxy C1 - C6 C1 - C6, haloalquilo C1 - C6, R3 is aryl, among others Optionally substituted heteroaryl 1-3 times by C1 - C6 Hydroxy, alkoxy, hidroxialquilo C1 - C6Among others R4 is ch2cf3 cycloalkyl, CF3, c3-5, halogen, alkoxy C1 - 6, among others R5 is H, halogen, alkoxy alkyl of C1 - C6 C1 - C6.Preferred compounds are: N - [6 - (4 - tert - butyl - 2 - methoxy - 8 - 2 - oxo - 1,2 dihydro - pyridin-3-yl) - yl] quinolin-1 - 3 - phenyl - methanesulfonamide {} n - (S) - 1 - [6 - Tert Butyl - 4 - (6 - Hydroxymethyl - 2 - oxo - 1,2 dihydro - pyridin-3-yl) - 5 - methoxy - 3 - il quinolin-1 - pyrrolidin-3-yl] - 3 - methyl - methanesulfonamide} among others. In addition to such a Pharmaceutical composition.This Compound is a useful NS5b polymerase inhibitor in the treatment of hepatitis CSE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: X1, X2, X3 Y X4 SON CADA UNO N, CR5 R1 ES PIRIDINILO, 2-OXO-1,2-DIHIDRO-PIRIDIN-3-ILO 3-OXO-3,4-DIHIDRO-PIRAZIN-2-ILO, 2-OXO-TETRAHIDRO-PIPERIDIN-1-ILO, ENTRE OTROS R2 ES H, ALCOXI C1-C6, ALQUILO C1-C6, HALOALQUILO C1-C6, ENTRE OTROS R3 ES ARILO, HETEROARILO OPCIONALMENTE SUSTITUIDO 1-3 VECES POR HIDROXI, ALCOXI C1-C6, HIDROXIALQUILO C1-C6, ENTRE OTROS R4 ES CF3, CH2CF3, CICLOALQUILO C3-5, HALOGENO, ALCOXI C1-6, ENTRE OTROS R5 ES H, HALOGENO, ALCOXI C1-C6, ALQUILO C1-C6. SON COMPUESTOS PREFERIDOS: N-{4-[6-TERT-BUTIL-2-METOXI-8-(2-OXO-1,2-DIHIDRO-PIRIDIN-3-IL)-QUINOLIN-3-IL]-FENIL}-METANOSULFONAMIDA N-{(S)-1-[6-TERT-BUTIL-8-(6-HIDROXIMETIL-2-OXO-1,2-DIHIDRO-PIRIDIN-3-IL)-5-METOXI-QUINOLIN-3-IL]-PIRROLIDIN-3-ILMETIL}-METANOSULFONAMIDA ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE LA POLIMERASA NS5b UTIL EN EL TRATAMIENTO DE HEPATITIS C
