Jerôme Emile Georges Guillemont,Mikaël Paugam,Bruno Francois Marie Delest,Jan Heeres,Paulus Joannes Lewi,Paul Adriaan Jan Janssen
申请号：
US15241615
公开号：
US09802943B2
申请日:
2016.08.19
申请国别(地区):
US
年份:
2017
代理人:
摘要：
HIV replication inhibitors of formulaN-oxides, pharmaceutically acceptable 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 4R1 is hydrogen aryl formyl C1-6alkylcarbonyl optionally substituted C1-6alkyl C1-6alkyloxycarbonylR2 is OH halo optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl substituted carbonyl carboxyl CN nitro amino substituted amino polyhalomethyl polyhalomethylthio —S(═O)pR6 C(═NH)R6R2a 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)—C1-4alkyl R7 or —X—R7R3 is CN amino C1-6alkyl 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—R7R4 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- or di(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 the preparation of these compounds and compositions the use of these compounds for the prevention or the treatment of HIV infection.
