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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.
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公开(公告)号:US20120190697A1
公开(公告)日:2012-07-26
申请号:US13410779
申请日:2012-03-02
申请人: Jerôme Emile Georges GUILLEMONT , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Frank Xavier Jozef Herwig Arts
发明人: Jerôme Emile Georges GUILLEMONT , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Frank Xavier Jozef Herwig Arts
IPC分类号: A61K31/52 , A61P31/18 , C07D473/32 , C07D487/04 , A61K31/519
CPC分类号: C07D487/04 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/34
摘要: HIV replication inhibitors of formula 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 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH═N—NH—C(═O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; 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—; and the use of these compounds for the prevention or the treatment of HIV infection.
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公开(公告)号:US20100168104A1
公开(公告)日:2010-07-01
申请号:US12294692
申请日:2007-03-30
IPC分类号: A61K31/505 , C07D413/06 , A61K31/5377 , C07D239/49 , C07D401/06 , A61K31/506 , C07D403/06 , C07D403/12 , C07D409/12 , C07D401/12 , C07D417/12 , A61P31/18
CPC分类号: C07D417/12 , C07D239/48 , C07D401/12 , C07D405/12 , C07D409/12
摘要: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.
摘要翻译: 本发明涉及具有HIV(人类免疫缺陷病毒)复制抑制性质的式的嘧啶衍生物,其制备方法和包含这些化合物的药物组合物。
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公开(公告)号:US09487518B2
公开(公告)日:2016-11-08
申请号:US13410779
申请日:2012-03-02
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
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: C07D487/04 , A61K31/519 , C07D473/00 , C07D473/34 , A61P31/18 , A61K31/52
CPC分类号: C07D487/04 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/34
摘要: HIV replication inhibitors of formula 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 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH═N—NH—C(═O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; 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—; and the use of these compounds for the prevention or the treatment of HIV infection.
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公开(公告)号:US08933089B2
公开(公告)日:2015-01-13
申请号:US12294692
申请日:2007-03-30
IPC分类号: A61K31/515 , C07D239/02 , C07D239/48 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号: C07D417/12 , C07D239/48 , C07D401/12 , C07D405/12 , C07D409/12
摘要: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.
摘要翻译: 本发明涉及具有HIV(人类免疫缺陷病毒)复制抑制性质的式的嘧啶衍生物,其制备方法和包含这些化合物的药物组合物。
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