269055-46-1Relevant articles and documents
PRODRUGS OF HIV REPLICATION INHIBITING PYRIMIDINES
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, (2015/11/28)
The present invention concerns compounds of formula (A1)(A2)N—R1 (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula
Prodrugs of hiv replication inhibiting pyrimidines
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, (2008/06/13)
The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(=O)—R8; —S(=O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula 1
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues
Ludovici, Donald W.,De Corte, Bart L.,Kukla, Michael J.,Ye, Hong,Ho, Chih Y.,Lichtenstein, Mark A.,Kavash, Robert W.,Andries, Koen,De Bethune, Marie-Pierre,Azijn, Hilde,Pauwels, Rudi,Lewi, Paul J.,Heeres, Jan,Koymans, Lucien M.H.,De Jonge, Marc R.,Van Aken, Koen J.A.,Daeyaert, Frederik F.D.,Das, Kalyan,Arnold, Edward,Janssen, Paul A.J.
, p. 2235 - 2239 (2007/10/03)
The synthesis and anti-HIV-1 activity of a series of diarylpyrimidines (DAPYs) are described. Several members of this novel class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) are extremely potent against both wild-type and a panel of clinically significant single- and double-mutant strains of HIV-1.
