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    • 5. 发明申请
    • BENZO [E] [1, 3 ] OXAZIN-4-ONE DERIVATIVES AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS
    • 苯并[E] [1,3]氧嗪-4-酮衍生物作为磷酸三磷酸酶抑制剂
    • WO2011012883A1
    • 2011-02-03
    • PCT/GB2010/051221
    • 2010-07-23
    • KARUS THERAPEUTICS LIMITEDSHUTTLEWORTH, Stephen JosephSILVA, Franck AlexandreCECIL, Alexander Richard LiamHILL, Thomas James
    • SHUTTLEWORTH, Stephen JosephSILVA, Franck AlexandreCECIL, Alexander Richard LiamHILL, Thomas James
    • C07D265/24A61K31/536A61P35/00A61P9/00A61P37/00A61P29/00A61P5/00
    • C07D265/24
    • Compounds of formula (I): wherein: W is O, N-H, N-alky!, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R 1 is formula (b) or R 3 is H, alkyl, NH 2 , OH, =0 or halogen; each A and B are independently CH or N; D is NHR 4 ; R 4 is H, alkyl, -C(O)- alkyl. -C(O)-NH 2 , -C(O)-NH- alkyl, -SO 2 - alky!, -SO 2 -NH 2 or -SO 2 -NH- alkyl; R 2 is aryl substituted with at least one nitrogen-containing group or R 2 is a nitrogen-containing heteroaryl, cycloalkyl substituted with a nitrogen-containing group, nitrogen-containing cycloalkyl, C 1 -C 6 mono alkylamino, C 1 C 6 bis alkylamino, C 1 C 6 acylamino, C 1 -C 6 aminoalkyl, mono (C 1 C 6 alkyl) amino C 1 -C 6 alkyl, bis (C 1 C 6 alkyl) amino C 1 C 6 alkyl, C 1 -C 6 -acylamino or C 1 C 6 alkynyl-NR 11 ; R 11 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, halogen, O-alkyl, NH-alkyl, N-dialkyl, -C(O)-R 7 , -C(O)-NH 2 , -C(O)-NH-R 7 , -SO 2 -R 7 , -SO 2 -NH 2 , -SO 2 -NH- R 7 , NH-acyl, NH-sulfonyl, NR 7 -acyl, NR 7 -suIfonyl, N-C(O)-NH-R 7 , N-SO 2 -NH-R 7 , N-C(O)-NR 7 R 7 or N-SO 2 -NR 7 R 7 ; and R 7 is alkyl, aryl or heteroaryl, are useful as PI3K inhibitors and are useful in therapy.
    • 式(I)化合物:其中:W为O,N-H,N-烷基,N-烯基,N-炔基,N-芳基,N-杂芳基或S; 每个X独立地是CH或N; R1是式(b)或R3是H,烷基,NH2,OH,= 0或卤素; 每个A和B独立地是CH或N; D是NHR4; R4是H,烷基,-C(O) - 烷基。 -C(O)-NH 2,-C(O)-NH-烷基,-SO 2 - 烷基,-SO 2 -NH 2或-SO 2 -NH-烷基; R2是被至少一个含氮基取代的芳基,或R2是含氮杂芳基,被含氮基取代的环烷基,含氮环烷基,C1-C6单烷基氨基,C1C6双烷基氨基,C1C6酰基氨基,C1- (C 1 -C 6烷基)氨基C 1 -C 6烷基,双(C 1 -C 6烷基)氨基C 1 -C 6烷基,C 1 -C 6酰基氨基或C 1 -C 6炔基-NR 11; R 11是H,烷基,烯基,炔基,芳基,杂芳基,卤素,O-烷基,NH-烷基,N-二烷基,-C(O)-R 7,-C(O)-NH 2,-C(O) NH-R7,-SO2-R7,-SO2-NH2,-SO2-NH-R7,NH-酰基,NH-磺酰基,NR7-酰基,NR7-磺酰基,NC(O) NH-R7,NC(O)-NR7R7或N-SO2-NR7R7; 和R7是烷基,芳基或杂芳基,可用作PI3K抑制剂,并且可用于治疗。