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    HIV INHIBITING BICYCLIC PYRIMIDINE DERIVATIVES
    4.
    发明公开
    HIV INHIBITING BICYCLIC PYRIMIDINE DERIVATIVES 有权
    HIV抑制双环嘧啶衍生物

    公开(公告)号：EP1807430A1

    公开(公告)日：2007-07-18

    申请号：EP05801379.8

    申请日：2005-10-27

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： GUILLEMONT, Jerôme Emile Georges ,  PAUGAM, Mikaël ,  DELEST, Bruno François Marie ,  HEERES, Jan ,  LEWI, Paulus Joannes ,  JANSSEN, Paul Adriaan Jan

    IPC分类号： C07D487/04 ,  C07D473/00 ,  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.

    摘要翻译： 其中-a1 = a2-a3 = a4-是-CH = CH-CH = CH-，-N = CH- CH = CH - ， - N = CH-N = CH-，-N = CH-CH = N-，-N = N-CH = CH-; -b1 = b2-b3 = b4-是-CH = CH-CH = CH-，-N = CH-CH = CH-，-N = CH-N = CH-，-N = CH-CH = N-， -N = N-CH = CH-; n和m是0,1,2,3，在某些情况下也是4; R1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 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; 取代的氨基; 多卤代; polyhalomethylthio; -S（= O）pR6; C（= NH）R 6; R2a是CN; 氨基; 取代的氨基; 任选取代的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）-R 16; 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-X-R7; R3是CN; 氨基; C1-6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）-R 16; 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; -X-R 7; 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; 3-7环烷基; C1-6烷; CN; 硝基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; 取代的羰基; 甲酰基; 氨基; 单或二（C 1-4烷基）氨基或R 7; -A-B-是-CR 5 = N-，-N = N-，-CH 2 -CH 2 - ， - CS-NH-，-CO-NH-，-CH = CH-; 包含这些药物组合物; 制备这些化合物和组合物的方法; 这些化合物用于预防或治疗HIV感染的用途。

    HIV INHIBITING 5-HETEROCYCLYL PYRIMIDINES
    5.
    发明公开
    HIV INHIBITING 5-HETEROCYCLYL PYRIMIDINES 有权
    抑制HIV 5 HETEROCYCLYLPYRIMIDINE

    公开(公告)号：EP1797069A2

    公开(公告)日：2007-06-20

    申请号：EP05794656.8

    申请日：2005-09-29

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： GUILLEMONT, Jerôme, Emile, Georges ,  HEERES, Jan ,  LEWI, Paulus, Joannes

    IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14

    CPC分类号： C07D405/04 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

    摘要： HIV replication inhibitors of formula (I), 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-; 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 C 2-6 alkynyl; -C(=N-O-R8)-C1-4alkyl; R7 or -X3-R7; X1 is -NR1-, -O-, -C(=O)-, -CH2-, -CHOH-, -S-, -S(=O)P- 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; -X3-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; R5 is a 5- or 6-membered completely unsaturated ring system wherein 1 - 4 ring members are nitrogen, oxygen or sulfur; which ring may optionally be substituted and may optionally be annelated with a benzene ring; methods for their preparation and pharmaceutical compositions comprising them. The invention also relates to the use of these compounds for the prevention or the treatment of HIV infection.

    HIV INHIBITING 5-CARBO- OR HETEROCYCLIC SUBSTITUTED PYRIMIDINES
    6.
    发明公开
    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：EP1797048A2

    公开(公告)日：2007-06-20

    申请号：EP05803358.0

    申请日：2005-09-29

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： GUILLEMONT, Jerôme, Emile, Georges ,  HEERES, Jan ,  LEWI, Paulus Joannes

    IPC分类号： C07D239/48 ,  C07D401/12 ,  C07D417/12 ,  C07D405/12 ,  C07D409/12 ,  C07D403/12 ,  C07D413/14 ,  A61K31/505

    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 subst ituted 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; polyhalo methylt hio; -S(=O)rR6; C(=NH)R6; R2a is CN; amino; substituted amino; optionally subst ituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; 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, pharmaceut ical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.

    HIV INHIBITING 5-SUBSTITUTED PYRIMIDINES
    7.
    发明公开
    HIV INHIBITING 5-SUBSTITUTED PYRIMIDINES 有权
    HIV抑制5-取代的嘧啶

    公开(公告)号：EP1797047A1

    公开(公告)日：2007-06-20

    申请号：EP05789686.2

    申请日：2005-09-29

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： GUILLEMONT, Jerôme, Emile, Georges ,  HEERES, Jan ,  LEWI, Paulus Joannes

    IPC分类号： C07D239/48 ,  C07D239/50 ,  A61K31/505 ,  A61P31/18

    CPC分类号： C07D239/48 ,  C07D239/50

    摘要： HIV replication inhibitors of formula (I) 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.