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11 条记录 (耗时 0.042 秒)

    HIV INHIBITING 5-CARBO- OR HETEROCYCLYL SUBSTITUTED PYRIMIDINES
    8.
    发明申请
    HIV INHIBITING 5-CARBO- OR HETEROCYCLYL SUBSTITUTED PYRIMIDINES 有权

    公开(公告)号：US20070208022A1

    公开(公告)日：2007-09-06

    申请号：US11576068

    申请日：2005-09-29

    申请人： Jerome Guillemont ,  Jan Heeres ,  Paulus Lewi

    发明人： Jerome Guillemont ,  Jan Heeres ,  Paulus Lewi

    IPC分类号： A61K31/5377 ,  A61K31/53 ,  A61K31/506 ,  C07D403/02 ,  C07D413/02

    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; polyhalo methylthio; —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.

    Hiv Inhibiting Bicyclic Pyrimdine Derivatives
    9.
    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.

    Stereotypy test apparatus and methods
    10.
    发明申请
    Stereotypy test apparatus and methods 审中-公开
    定型检验仪器及方法

    公开(公告)号：US20050084832A1

    公开(公告)日：2005-04-21

    申请号：US10499385

    申请日：2002-12-19

    申请人： Paul Janssen ,  Paulus Lewi ,  Roger Rosiers

    发明人： Paul Janssen ,  Paulus Lewi ,  Roger Rosiers

    IPC分类号： A61B5/16 ,  G06F19/00 ,  G09B19/00

    CPC分类号： A61B5/16 ,  A61B5/168

    摘要： A stereotypy test apparatus 10 is disclosed, which is suitable for interactive use in the diagnosis of a psychiatric disorder. The apparatus comprises an input means in the form of a keypad 14 adapted for physical entry of input signals to the apparatus 10 and a control means 28 which is adapted to prompt a candidate to enter during a test session a succession of said input signals. The control means 28 analyses entered said input signals in order to derive and output from said analysis one or more output signals indicative of at least one value RC, RS which is used in the diagnosis of the presence or absence in said candidate of at least one predetermined psychiatric disorder or of the candidate's predisposition theretowards. The input signals comprise a succession of choices (1-9) selected freely by said candidate from a plurality of mutually independent choices (1-9) and a said output signal RC, RS is indicative of repetitive patterns among said candidate choices.

    摘要翻译： 公开了一种定型测试装置10，其适用于精神障碍诊断中的互动使用。 该装置包括适于将输入信号物理地输入到装置10的小键盘14形式的输入装置和控制装置28，该控制装置28适于提示候选者在测试会话期间输入一系列所述输入信号。 控制装置28分析输入的所述输入信号，以便从所述分析中导出和输出表示至少一个值RC，RS的一个或多个输出信号，所述值用于诊断所述候选者是否存在至少一个 预期的精神障碍或候选人的倾向。 所述输入信号包括由多个相互独立的选择（1-9）中所述候选者自由选择的一系列选择（1-9），并且所述输出信号RC，RS表示所述候选选择中的重复模式。