HIV inhibiting bicyclic pyrimidine derivatives

• Main Authors: Guillemont, Jerôme Emile Georges, Delest, Bruno Francois Marie, Janssen, Paul Adriaan Jan, Heeres, Jan, Lewi, Paulus Joannes, Paugam, Mikaël
• Format: Patent
• Language: English
• Published: 11.09.2018
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

HIV replication inhibitors of formula 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 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; -S( O)pR6; C( NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; -CH N-NH-C( O)-R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; -C( N-O-R8)-C1-4alkyl; R7 or -X-R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; -CH N-NH-C( O)-R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; -C( N-O-R8)-C1-4alkyl; R7; -X-R7; R4 is halo; OH; 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-; and the use of these compounds for the prevention or the treatment of HIV infection.