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    HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
    34.
    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。

    Hiv Inhibiting Bicyclic Pyrimdine Derivatives
    37.
    发明申请
    Hiv Inhibiting Bicyclic Pyrimdine Derivatives 有权

    公开(公告)号：US20080085907A1

    公开(公告)日：2008-04-10

    申请号：US11718181

    申请日：2005-10-27

    申请人： Jerome Guillemont ,  Mikael Paugam ,  Bruno Delest ,  Jan Heeres ,  Paulus Lewi ,  Paul Adriaan Janssen ,  Frank Javier Arts

    发明人： Jerome Guillemont ,  Mikael Paugam ,  Bruno Delest ,  Jan Heeres ,  Paulus Lewi ,  Paul Adriaan Janssen ,  Frank Javier Arts

    IPC分类号： C07D473/36 ,  A61K31/519 ,  A61K31/52 ,  A61P31/18 ,  C07D487/04 ,  C07D239/70 ,  C07D473/32

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

    摘要： HIV replication inhibitors of formula (1) 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)—C1-4 alkyl; R7 or —X—R4; 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)—C1-4 alkyl; 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.