GUILLEMONT, JEROME EMILE GEORGES,HEERES, JAN,LEWI, PAULUS JOANNES
申请号：
CA2577467
公开号：
CA2577467C
申请日:
2005.09.29
申请国别(地区):
CA
年份:
2013
代理人:
摘要：
HIV replication inhibitors of formula (I), N-oxides, pharmaceuticallyacceptable 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 C1-6alkylcarbonyloptionally substituted C1-6alkyl C1-6alkyloxycarbonyl R2 is OH halooptionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl substitutedcarbonyl carboxyl CN nitro amino substituted amino polyhalomethylpolyhalomethylthio -S(=O)PR6 C(=NH)R6 R2a is CN amino substituted aminooptionally substituted C1-6alkyl halo optionally substituted C1-6alkyloxysubstituted 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 CNamino C1-6alkyl halo optionally substituted C1-6alkyloxy substitutedcarbonyl -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- ordi(C1-4alkyl)amino or R7 R5 is a 5- or 6-membered completely unsaturated ringsystem wherein 1 - 4 ring members are nitrogen, oxygen or sulfur which ringmay optionally be substituted and may optionally be annelated with a benzenering methods for their preparation and pharmaceutical compositions comprisingthem. The invention also relates to the use of these compounds for theprevention or the treatment of HIV infection.
