1033951-07-3Relevant academic research and scientific papers
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Benzyl derivatives with broad potency against resistant mutant viruses
Kertesz, Denis J.,Brotherton-Pleiss, Christine,Yang, Minmin,Wang, Zhanguo,Lin, Xianfeng,Qiu, Zongxing,Hirschfeld, Donald R.,Gleason, Shelley,Mirzadegan, Taraneh,Dunten, Pete W.,Harris, Seth F.,Villasenor, Armando G.,Hang, Julie Qi,Heilek, Gabrielle M.,Klumpp, Klaus
scheme or table, p. 4215 - 4218 (2010/08/22)
An analysis of the binding motifs of known HIV-1 non-nucleoside reverse transcriptase inhibitors has led to discovery of novel piperidine-linked aminopyrimidine derivatives with broad activity against wild-type as well as drug-resistant mutant viruses. Notably, the series retains potency against the K103 N/Y181C and Y188L mutants, among others. Thus, the N-benzyl compound 5k has a particularly attractive profile. Synthesis and SAR are presented and discussed, as well as crystal structures relating to the binding motifs.
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 24, (2008/12/06)
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
