发明授权
- 专利标题： HIV inhibiting 5-substituted pyrimidines
- 专利标题（中）： HIV抑制5-取代嘧啶
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申请号： US11576315申请日： 2005-09-29
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公开(公告)号： US08946248B2公开(公告)日： 2015-02-03
- 发明人: Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
- 申请人： Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
- 申请人地址： IR Little Island, County Cork
- 专利权人： Janssen R&D Ireland
- 当前专利权人： Janssen R&D Ireland
- 当前专利权人地址： IR Little Island, County Cork
- 代理商 Bernard F. Plantz
- 优先权： EP04104805 20040930
- 国际申请： PCT/EP2005/054932 WO 20050929
- 国际公布： WO2006/035069 WO 20060406
- 主分类号： C07D239/48
- IPC分类号： C07D239/48 ; A61K31/505 ; 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.
公开/授权文献
- US20080262007A1 Hiv Inhibiting 5-Substituted Pyrimidines 公开/授权日：2008-10-23
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