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    HIV INHIBITING 6-SUBSTITUTED PYRIMIDINES
    1.
    发明申请
    HIV INHIBITING 6-SUBSTITUTED PYRIMIDINES 有权
    艾滋病毒抑制6-取代的吡咯烷酮

    公开(公告)号：US20100016317A1

    公开(公告)日：2010-01-21

    申请号：US12521189

    申请日：2007-12-28

    申请人： Jerôme Emile Georges Guillemont ,  Celine Isabelle Mordant

    发明人： Jerôme Emile Georges Guillemont ,  Celine Isabelle Mordant

    IPC分类号： A61K31/5377 ,  C07D239/02 ,  A61K31/505 ,  C07D413/00

    CPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/06

    摘要： 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.

    摘要翻译： 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。

    HIV inhibiting bicyclic pyrimdine derivatives
    2.
    发明授权
    HIV inhibiting bicyclic pyrimdine derivatives 有权

    公开(公告)号：US08153640B2

    公开(公告)日：2012-04-10

    申请号：US11718181

    申请日：2005-10-27

    申请人： Jerôme Emile Georges Guillemont ,  Mikaël Paugam ,  Bruno Francois Marie Delest ,  Jan Heeres ,  Paulus Joannes Lewi ,  Paul Adriaan Jan Janssen ,  Frank Xavier Jozef Herwig Arts, legal representative

    发明人： Jerôme Emile Georges Guillemont ,  Mikaël Paugam ,  Bruno Francois Marie Delest ,  Jan Heeres ,  Paulus Joannes Lewi ,  Paul Adriaan Jan Janssen

    IPC分类号： C07D473/32 ,  A61K31/52 ,  A61P31/18

    CPC分类号： C07D487/04 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/34

    摘要： HIV replication inhibitors of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0, 1, 2, 3 and in certain cases also 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; -A-B— is —CR5═N—, —N═N—, —CH2—CH2—, —CS—NH—, —CO—NH—, —CH═CH—; pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.

    HIV INHIBITING 5, 6-SUBSTITUTED PYRIMIDINES
    5.
    发明申请
    HIV INHIBITING 5, 6-SUBSTITUTED PYRIMIDINES 有权
    HIV抑制5,6-取代的吡咯烷酮

    公开(公告)号：US20100261722A1

    公开(公告)日：2010-10-14

    申请号：US12521379

    申请日：2007-12-28

    申请人： Jerôme Emile Georges Guillemont ,  Céline Isabelle Mordant ,  Benoit Antoine Schmitt

    发明人： Jerôme Emile Georges Guillemont ,  Céline Isabelle Mordant ,  Benoit Antoine Schmitt

    IPC分类号： A61K31/5377 ,  C07D401/04 ,  A61K31/506 ,  A61P31/18 ,  C07D413/12 ,  C07D239/48

    CPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/06

    摘要： HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R7 and R8 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)R10; C1-6alkyl optionally substituted with halo, cyano or —C(═O)R10; optionally substituted C1-6alkyl, C2-6alkenyl, or C2-6alkynyl; R4 and R9 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)R10; cyano; —S(═O)rR10; —NH—S(═O)2R10; —NHC(═O)H; —C(═O)NHNH2; —NHC(═O)R10; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is C2-6alkenyl or C2-6alkynyl both substituted with cyano, aminocarbonyl, mono- and di(C1-6alkyl)aminocarbonyl, aryl, pyridyl, thienyl, furanyl, or with one or two C1-6alkyloxy groups; Het; —C(═O)NR5aR5b; —CH(OR5c)R5d; X is —NR1—, —O—, —CH2—, or —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.

    摘要翻译： 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，R7和R8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 10; 任选被卤素，氰基或-C（= O）R 10取代的C 1-6烷基; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; R4和R9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）R10; 氰基; -S（= O）r R 10; -NH-S（= O）2 R 10; -NHC（= O）H; -C（= O）NHNH 2; -NHC（= O）R 10; Het; -Y-Het; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; R 5是被氰基，氨基羰基，单和二（C 1-6烷基）氨基羰基，芳基，吡啶基，噻吩基，呋喃基或与一个或两个C 1-6烷氧基取代的C 2-6烯基或C 2-6炔基; Het; -C（= O）NR5aR5b; -CH（OR 5 c）R 5d; X是-NR 1 - ， - O - ， - CH 2 - 或-S-; 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。

    HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
    9.
    发明授权
    HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines 有权
    HIV抑制5-碳环或杂环取代的嘧啶

    公开(公告)号：US07531548B2

    公开(公告)日：2009-05-12

    申请号：US11576068

    申请日：2005-09-29

    申请人： Jerôme Emile Georges Guillemont ,  Jan Heeres ,  Paulus Joannes Lewi

    发明人： Jerôme Emile Georges Guillemont ,  Jan Heeres ,  Paulus Joannes Lewi

    IPC分类号： C07D239/48 ,  C07D239/50 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  A61K31/505 ,  A61P31/18

    CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12

    摘要： HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O)rR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C2-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 is —NR1—, —O—, —C(═O)—, CH2, —CHOH—, —S—, —S(═O)r—; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X3—R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhalo C1-6alkyl; polyhalo C1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; R5 is —Y—CqH2q-L or —CqH2q—Y—CrH2r-L; L is aryl or Het; processes for the preparation of these compounds, pharmaceutical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.

    摘要翻译： 式（I）的HIV复制抑制剂N-氧化物，药学上可接受的加成盐，季胺或其立体异构形式，其中-a1 = a2-a3 = a4-是-CH-CH-CH-CH-，-N -CH-CH-CH-，-N-CH-N-CH-，-N-CH-CH-N - ，-NN-CH-CH-; -b1 = b2-b3 = b4-是-CH-CH-CH-CH-，-N-CH-CH-CH-，-N-CH-N-CH-，-N-CH-CH-N-， -NN-CH-CH-; R1是氢; 芳基; 甲酰基 C 1-6烷基羰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基; R2是OH; 光环; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; 取代的羰基; 羧基; CN; 硝基 氨基; 取代氨基; 多卤甲基 多卤甲硫基 -S（-O）r R 6; C（-NH）R 6; R2a为CN; 氨基; 取代氨基; 任选取代的C 1-6烷基; 光环; 任选取代的C 2-6烷氧基; 取代的羰基; -CH-N-NH-C（-O）-R16; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6炔基; -C（-N-O-R 8）-C 1-4烷基; R7或-X3-R7; X 1是-NR 1 - ， - O - ， - C（-O） - ，CH 2，-CHOH - ， - S - ， - S（-O） R3为CN; 氨基; C 1-6烷基; 光环; 任选取代的C 1-6烷氧基; 取代的羰基; -CH-N-NH-C（-O）-R16; 取代的C 1-6烷基; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6炔基; -C（-N-O-R 8）-C 1-4烷基; R7; -X3-R7; R4是卤素; 哦; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; C 3-7环烷基; C 1-6烷氧基; CN; 硝基 多卤代C1-6烷基; 多卤C 1-6烷氧基; 取代的羰基; 甲酰基 氨基; 单或二（C 1-4烷基）氨基或R 7; R5是-Y-CqH2q-L或-CqH2q-Y-CrH2r-L; L是芳基或Het; 制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物以及这些化合物用于预防或治疗HIV感染的用途。