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    • 6. 发明授权
    • HIV inhibiting 6-substituted pyrimidines
    • HIV抑制6-取代嘧啶
    • US09006243B2
    • 2015-04-14
    • US12521189
    • 2007-12-28
    • Jerôme Emile Georges GuillemontCéline Isabelle Mordant
    • Jerôme Emile Georges GuillemontCéline Isabelle Mordant
    • C07D239/48A61K31/506C07D401/04C07D401/12C07D403/06C07D405/12C07D409/12C07D417/06
    • C07D239/48C07D401/04C07D401/12C07D403/06C07D405/12C07D409/12C07D417/06
    • HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(═O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(═O)R9; cyano; —S(═O)rR9; —NH—S(═O)2R9; —NHC(═O)H; —C(═O)NHNH2; —NHC(═O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(═O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH═NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(═O)(OR5g)2; —CH2—O—C(═O)—NH2; —C(═O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.
    • 式R1的HIV复制抑制剂是氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷基; C 1-6烷氧基羰基; R2,R3,R6和R7是氢; 羟基; 光环; C 3-7环烷基; C 1-6烷氧基; 羧基; C 1-6烷氧基羰基; 氰基; 硝基 氨基; 单或二(C 1-6烷基)氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; -C(= O)R 9; 任选取代的C 1-6烷基,C 2-6烯基或C 2-6炔基; R4和R5是羟基; 光环; C 3-7环烷基; C 1-6烷氧基; 羧基; C 1-6烷氧基羰基; 甲酰基 氰基; 硝基 氨基; 单或二(C 1-6烷基)氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; -C(= O)R 9; 氰基; -S(= O)r R 9; -NH-S(= O)2 R 9; -NHC(= O)H; -C(= O)NHNH 2; -NHC(= O)R 9; Het; -Y-Het; 任选取代的C 1-6烷基,C 2-6烯基或C 2-6炔基; R5是吡啶基,-C(= O)NR5aR5b; -CH(OR 5 c)R 5d; -CH2-NR5eR5f; -CH=NOR5a; -CH 2 -O-C 2-6烯基; -CH 2 -O-P(= O)(OR 5 g)2; -CH 2 -O-C(= O)-NH 2; -C(= O)-R5d; X是-NR 1 - , - O - , - CH 2 - , - S- 含有这些化合物作为活性成分的药物组合物和制备所述化合物和组合物的方法。
    • 7. 发明授权
    • HIV inhibiting 5-substituted pyrimidines
    • HIV抑制5-取代嘧啶
    • US08946248B2
    • 2015-02-03
    • US11576315
    • 2005-09-29
    • Jerôme Emile Georges GuillemontJan HeeresPaulus Joannes Lewi
    • Jerôme Emile Georges GuillemontJan HeeresPaulus Joannes Lewi
    • C07D239/48A61K31/505C07D239/50
    • C07D239/48C07D239/50
    • HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH═CH—, —C≡C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(═O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(═O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(═O)H, —NH—C(═O)R6, —CH═N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.
    • 其中A是-CH 2 -CH 2 - , - CH = CH - , - C≡C-;其中A是-CH 2 -CH 2 - , - CH = CH - , - C≡C-; R1是氢,芳基,甲酰基,C1-6烷基羰基,C1-6烷基,C1-6烷氧基羰基,R2羟基,卤素,C1-6烷基,羧基,氰基,-C(= O)R6,硝基,氨基,单或二 C 1-6烷基)氨基,多卤甲基; X 1是-NR 1 - , - O - , - S - , - S(= O)p - ; R 3是H,C 1-6烷基,卤素; R4是H,C1-6烷基,卤素; R 5是硝基,氨基,单和二C 1-4烷基氨基,芳基,卤素,-CHO,-CO-R 6,-COOR 7,-NH-C(= O)H,-NH-C(= = N-O-R8; R 6是C 1-4烷基,氨基,单或二(C 1-4烷基)氨基或多卤代C 1-4烷基; R 7是氢,C 1-6烷基,芳基C 1-6烷基; R8是氢,C1-6烷基,芳基; p为1或2; 芳基是任选取代的苯基; 含有这些化合物作为活性成分的药物组合物及其制备方法。