GUILLEMONT, JEROME EMILE GEORGES,HEERES, JAN,LEWI, PAULUS JOANNES
申请号：
CA2573976
公开号：
CA2573976C
申请日:
2005.09.29
申请国别(地区):
CA
年份:
2014
代理人:
摘要：
HIV replication inhibitors of formula (I) N-oxides, a pharmaceuticallyacceptable addition salts, a quaternary amines or a stereoisomeric formsthereof, 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 subst ituted C1-6alkyl C1-6alkyloxycarbonyl R2 isOH halo optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynylsubstituted carbonyl carboxyl CN nitro amino substituted aminopolyhalomethyl polyhalo methylt hio -S(=O)rR6 C(=NH)R6 R2a is CN aminosubstituted amino optionally subst ituted C1-6alkyl halo optionallysubstituted C1-6alkyloxy substituted carbonyl -CH=N-NH-C(=O)-R16 optionallysubstituted 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 C1-6alkyloptionally substituted C1-6alkyloxy C1-6alkyl substituted C2-6alkenyl or C2-6alkynyl -C(=N-O-R8)-C1-4alkyl R7 -X3-R7 R4 is halo OH optionallysubstituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl C3-7cycloalkyl C1-6alkyloxy CN nitro polyhalo C1-6alkyl polyhalo C1-6alkyloxy substitutedcarbonyl 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 thesecompounds, pharmaceut ical compositions comprising these compounds as activeingredient and the use of these compounds for the prevention or the treatmentof HIV infection.
