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N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol-3-kinase inhibitors
专利权人:
INC.;EXELIXIS
发明人:
BAJJALIEH, WILLIAM,CANNE BANNEN, LYNNE,BROWN, S. DAVID,KEARNEY, PATRICK,MAC, MORRISON B.,MARLOWE, CHARLES K.,NUSS, JOHN M.,TESFAI, ZEROM,WANG, YONG,XU, WEI
申请号:
ES06836252
公开号:
ES2513165T3
申请日:
2006.10.09
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of Formula Ia: ** Formula ** or a tautomer, simple stereoisomer, racemate, mixture of enantiomers and diastereomers, or geometric isomer thereof and optionally as a salt acceptable for pharmaceutical or solvate use thereof; where W1, W2, W3, and W4 are -C (R1)>; =; or one or two of W1, W2, W3, and W4 are independently -N>; = and the rest are -C (R1)>; =; and where each R1 is independently hydrogen, alkyl, haloalkyl, nitro, alkoxy, haloalkoxy, halo, hydroxy, cyano, amino, alkylamino, or dialkylamino; R51 is methyl; R50, R52, and R53 are hydrogen and R54 is halo or alkoxy; or R50, R52, and R54 are hydrogen and R53 is alkoxy; R3 is not present or R3 is methyl, methoxy or halo; and R3a is -N (R7) C (O) -C1-C6-N alkylene (R7a) (R7b) where R7 is hydrogen and R7a and R7b are independently hydrogen, alkyl, aminoalkyl, alkylaminoalkyl, or dialkylaminoalkyl.Un compuesto de Fórmula Ia:**Fórmula** o un tautómero, estereoisómero simple, racemato, mezcla de enantiómeros y diastereómeros, o isómero geométrico del mismo y opcionalmente como una sal aceptable para uso farmacéutico o solvato del mismo; en el que W1, W2, W3, y W4 son -C(R1)>;=; o uno o dos de W1, W2, W3, y W4 son independientemente -N>;= y el resto son -C(R1)>;=; y donde cada R1 es independientemente hidrógeno, alquilo, haloalquilo, nitro, alcoxi, haloalcoxi, halo, hidroxi, ciano, amino, alquilamino, o dialquilamino; R51 es metilo; R50, R52, y R53 son hidrógeno y R54 es halo o alcoxi; o R50, R52, y R54 son hidrógeno y R53 es alcoxi; R3 no está presente o R3 es metilo, metoxi o halo; y R3a es -N(R7)C(O)-alquileno C1-C6-N(R7a)(R7b) donde R7 es hidrógeno y R7a y R7b son independientemente hidrógeno, alquilo, aminoalquilo, alquilaminoalquilo, o dialquilaminoalquilo.
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