Invention Grant
- Patent Title: HIV inhibiting 5-substituted pyrimidines
- Patent Title (中): HIV抑制5-取代嘧啶
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Application No.: US11576315Application Date: 2005-09-29
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Publication No.: US08946248B2Publication Date: 2015-02-03
- Inventor: Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
- Applicant: Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
- Applicant Address: IR Little Island, County Cork
- Assignee: Janssen R&D Ireland
- Current Assignee: Janssen R&D Ireland
- Current Assignee Address: IR Little Island, County Cork
- Agent Bernard F. Plantz
- Priority: EP04104805 20040930
- International Application: PCT/EP2005/054932 WO 20050929
- International Announcement: WO2006/035069 WO 20060406
- Main IPC: C07D239/48
- IPC: C07D239/48 ; A61K31/505 ; C07D239/50

Abstract:
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.
Public/Granted literature
- US20080262007A1 Hiv Inhibiting 5-Substituted Pyrimidines Public/Granted day:2008-10-23
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