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    • 10. 发明授权
    • Derivatives of 1-phenyl-benzofuro[3,2]pyridin-2(1H)-one
    • 1-苯基 - 苯并呋喃并[3,2]吡啶-2(1H) - 酮的衍生物
    • US07622582B2
    • 2009-11-24
    • US11569108
    • 2005-05-17
    • Bart Rudolf Romanie KesteleynWim Van De VrekenDominique Louis Nestor Ghislain SurlerauxSandrine Marie Helene VendevillePierre Jean-Marie Bernard RaboissonPiet Tom Bert Paul WigerinckAnnick Ann Peeters
    • Bart Rudolf Romanie KesteleynWim Van De VrekenDominique Louis Nestor Ghislain SurlerauxSandrine Marie Helene VendevillePierre Jean-Marie Bernard RaboissonPiet Tom Bert Paul WigerinckAnnick Ann Peeters
    • C07D491/00
    • C07D471/04C07D491/04C07D491/14
    • 4-substituted 1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; X is NR2, O, S, SO, SO2; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, which are optionally substituted; R2 is aryl substituted with —COOR4; or R2 is: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b (b-5); -a1=a2-a3=a4- is —CH═CH—CH═CH—; —N═CH—CH═CH—; —CH═N—CH═CH—; —CH═CH—N═CH—; —CH═CH—CH═N—; wherein hydrogen atoms in (c-1)-(c-5) may be replaced by certain radicals; R3 is optionally substituted phenyl or a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted; R21 is halo, hydroxy, amino, carboxyl, C1-6alkyl, C3-7cycloalkyl, arylC1-6alkyl, formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy, —C(═O)—NR13R14; C1-6alkyloxy, arylC1-6alkyloxy, polyhaloC1-6alkyloxy, amino, mono or di(C1-6alkyl)amino, formylamino, C1-6alkylcarbonylamino, C1-6alkylsulfonylamino, mercapto, C1-6alkylthio, arylthio, aryloxy, arylC1-6alkylthio, C1-6alkylsulfynyl, C1-6alkylsulfonyl, aryl, arylamino, Het1, Het2.
    • 式(I)的4-取代的1,5-二氢吡啶并[3,2-b]吲哚-2-酮:N-氧化物,盐,立体异构形式,外消旋混合物,前药,酯和代谢物,其中n 是1,2或3; R 1是氢,氰基,卤素,取代的羰基,甲酰亚胺基,N-羟基 - 甲酰亚胺基,单或二(C 1-4烷基)甲酰亚胺基,Het1或Het2; X是NR2,O,S,SO,SO2; R 2是氢,C 1-10烷基,C 2-10烯基,C 3-7环烷基,其任选被取代; R2是被-COOR4取代的芳基; 或R2是:-CpH2p-CH(OR14)-CqH2q-R15(b-3); -CH 2 -CH 2 - (O-CH 2 -CH 2)m -OR 14(b-4); -CH 2 -CH 2 - (O-CH 2 -CH 2)m -NR 5 a R 5b(b-5); -a1 = a2-a3 = a4-是-CH-CH-CH-CH-; -N-CH-CH-CH-; -CH-N-CH-CH-; -CH-CH-N-CH-; -CH-CH-CH-N-; 其中(c-1) - (c-5)中的氢原子可被某些基团取代; R3是任选取代的苯基或可被取代的单环或双环芳族杂环体系; R 21是卤素,羟基,氨基,羧基,C 1-6烷基,C 3-7环烷基,芳基C 1-6烷基,甲酰基,C 1-6烷基羰基,C 1-6烷氧基羰基,C 1-6烷基羰氧基,-C(-O)-NR 13 R 14; C 1-6烷氧基,芳基C 1-6烷氧基,多卤代C 1-6烷氧基,氨基,一或二(C 1-6烷基)氨基,甲酰氨基,C 1-6烷基羰基氨基,C 1-6烷基磺酰基氨基,巯基,C 1-6烷硫基,芳硫基,芳氧基,芳基C 1-6烷硫基, C 1-6烷基磺酰基,芳基,芳基氨基,Het1,Het2。