GUILLEMONT, JEROME EMILE GEORGES,PAUGAM, MIKAEL,DELEST, BRUNO FRANCOIS MARIE,HEERES, JAN,LEWI, PAULUS JOANNES,JANSSEN, PAUL ADRIAAN JAN (DECEASED)
申请号:
CA2577588
公开号:
CA2577588C
申请日:
2005.10.27
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- n and m is 0, 1, 2, 3 and in certain cases also 4 R1is 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 nitroamino 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-R7 R3 is CN aminoC1-6alkyl 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- ordi(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 thepreparation of these compounds and compositions the use of these compoundsfor the prevention or the treatment of HIV infection.