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    HIV inhibiting bicyclic pyrimdine derivatives
    1.
    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 replication inhibiting pyrimidines
    7.
    发明授权
    HIV replication inhibiting pyrimidines 有权
    HIV复制抑制嘧啶

    公开(公告)号：US08003789B2

    公开(公告)日：2011-08-23

    申请号：US11930835

    申请日：2007-10-31

    申请人： Bart De Corte ,  Marc René de Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Frank Xavier Jozef Herwig Arts, legal representative ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici ,  Koen Jeanne Alfons Van Aken ,  Koenraad Jozef Lodewijk Marcel Andries

    发明人： Bart De Corte ,  Marc René de Jonge ,  Jan Heeres ,  Chih Yung Ho ,  Paul Adriaan Jan Janssen ,  Robert W. Kavash ,  Lucien Maria Henricus Koymans ,  Michael Joseph Kukla ,  Donald William Ludovici ,  Koen Jeanne Alfons Van Aken ,  Koenraad Jozef Lodewijk Marcel Andries

    IPC分类号： C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61P31/18

    CPC分类号： A61K31/505 ,  A61K31/5513

    摘要： This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, 13 NHC(═O)R6,—C(═NH)R6, aryl; for the treatment of subjects suffering from HIV infection.

    摘要翻译： 本发明涉及式I化合物的N-氧化物，药学上可接受的加成盐，季胺，其立体化学异构体形式的用途，其中-a1 = a2-a3 = a4形成苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基， 乙烯基; n为0〜5; R 1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，取代的C 1-6烷基，取代的C 1-6烷氧基C 1-6烷基羰基; R2是羟基，卤素，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，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单或二（C 1-6烷基）氨基 ，多卤代甲基，多卤代甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6，-NHC（= O）H，-C（= O）NHNH 2， NHC（= O）R 6，-C（= NH）R 6，5元杂环; L是任选取代的C 1-10烷基，C 2-10烯基，C 2-10炔基或C 3-7环烷基; 或-X-R 3; Q是氢，C 1-6烷基，卤素，多卤代-C 1-6烷基，任选取代的氨基; Y表示羟基，卤素，C 3-7环烷基，任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单 - 或二（C 1-6烷基）氨基 ，多卤甲基，多卤代甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6，-NHC（= O）H，-C（= O）NHNH 2， NHC（= O）R 6，-C（= NH）R 6，芳基; 用于治疗患有艾滋病毒感染的受试者。

    HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
    8.
    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 5-substituted pyrimidines
    10.
    发明授权
    HIV inhibiting 5-substituted pyrimidines 有权
    HIV抑制5-取代嘧啶

    公开(公告)号：US08946248B2

    公开(公告)日：2015-02-03

    申请号：US11576315

    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 ,  A61K31/505 ,  C07D239/50

    CPC分类号： C07D239/48 ,  C07D239/50

    摘要： 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.

    摘要翻译： 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。