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    • 9. 发明申请
    • Hiv Inhibiting 1,2,4-Triazin-6-One Derivatives
    • HIF抑制1,2,4-三嗪-6-酮衍生物
    • US20090012092A1
    • 2009-01-08
    • US11573224
    • 2005-08-10
    • Georges Joseph Cornelius HoornaertAmuri KilondaJan HeeresPaulus Joannes LewiMarc Rene de JongeFrederik Frans Desire DaeyaertHendrik Maarten VinkersLucien Maria Henricus KoymansPaul Adriaan Jan JanssenFrank Xavier Jozef Herwig Arts
    • Georges Joseph Cornelius HoornaertAmuri KilondaJan HeeresPaulus Joannes LewiMarc Rene de JongeFrederik Frans Desire DaeyaertHendrik Maarten VinkersLucien Maria Henricus KoymansPaul Adriaan Jan JanssenFrank Xavier Jozef Herwig Arts
    • A61K31/53C07D253/06A61P31/18
    • C07D253/075
    • The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(═O)pR6; —NH—S(═O)pR6; —C(═O)R6; —NHC(═O)H; —C(═O)NHNH2; NHC(═O)R6; C(═NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14 —C(═O)—NHR13; —C(═O)—NR13 R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 or X2 represents —NR1—; —NH—NH—; —N═N—; —O—; —C(═O)—; —C1-4alkanediyl-; —CHOH—; —S—; —S(═O)p—; —X4—C1-4alkanediyl-; —C1-4alkanediyl-X4—; or —C1-4alkanediyl-X4—C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.
    • 本发明涉及式N-氧化物的HIV复制抑制剂,其药学上可接受的加成盐,季胺或其立体化学异构形式,其中环A和环B表示苯基,吡啶基,哒嗪基,嘧啶基或吡嗪基; n和m为1〜4; R1表示氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷氧基羰基; 任选取代的C 1-6烷基; 被C 1-6烷氧基羰基取代的C 1-6烷氧基C 1-6烷基羰基; R2或R4代表氢; 羟基; 光环; 任选取代的C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的C 2-6炔基; C 3-7环烷基; C 1-6烷氧基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 羧基; 氰基; 硝基 氨基; 单或二(C 1-6烷基)氨基; 多卤代C 1-4烷基; 多卤代1-4烷基氧基; 多卤代 -S(-O)p R 6; -NH-S(-O)p R 6; -C(-O)R 6; -NHC(-O)H; -C(-O)NHNH 2; NHC(-O)R 6; C(-NH)R 6; 或R7; R2a或R3表示氰基; 氨基羰基; 氨基; 光环; NHR13; NR 13 R 14 -C(-O)-NHR 13; -C( - ) - NR 13 R 14; -C(-O)-R 15; -CH-N-NH-C(-O)-R16; 任选取代的C 1-6烷基; 任选取代的C 1-6烷氧基; 任选取代的C 1-6烷氧基C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的C 2-6炔基; -C(-N-O-R 8)-C 1-4烷基; R7或-X3-R7; X1或X2表示-NR1-; -NH-NH-; -N-N- -O-; -C(-O) - ; -C 1-4烷二基 -CHOH-; -S-; -S(-O)p - ; -X4-C1-4烷二基 -C 1-4烷二基-X4-; 或-C1-4烷二基-X4-C1-4烷二基; 它们作为药物的用途,它们用于制备用于治疗或预防HIV感染的药物的用途; 其制备方法和包含它们的药物组合物。