214287-75-9Relevant articles and documents
4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones useful as HIV reverse transcriptase inhibitors
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, (2008/06/13)
The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: or steroisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent, wherein: R1 is C1-3 alkyl substituted with 1-7 halogen; R2 is optionally substituted C1-5 alkyl, optionally substituted C2-5 alkenyl, or optionally substituted C2-5 alkynyl; R3, at each occurrence, is independently selected from C1-4 alkyl, OH, C1-4 alkoxy, F, Cl, Br, I, NR5R5a, NO2, CN, C(O)R6, NHC(O)R7, and NHC(O)NR5R5a; R5 and R5a are independently selected from H and C1-3 alkyl; R6 is selected from H, OH, C1-4 alkyl, C1-4 alkoxy, and NR5R5a; R7 is selected from C1-3 alkyl and C1-3 alkoxy; R8 is selected from H, C3-5 cycloalkyl, and C1-3 alkyl; and, n is selected from 0, 1, 2, 3, and 4.
Expanded-spectrum nonnucleoside reverse transcriptase inhibitors inhibit clinically relevant mutant variants of human immunodeficiency virus type 1
Corbett, Jeffrey W.,Ko, Soo S.,Rodgers, James D.,Jeffrey, Susan,Bacheler, Lee T.,Klabe, Ronald M.,Diamond, Sharon,Lai, Chii-Ming,Rabel, Shelley R.,Saye, Jo Anne,Adams, Stephen P.,Trainor, George L.,Anderson, Paul S.,Erickson-Viitanen, Susan K.
, p. 2893 - 2897 (2007/10/03)
A research program targeted toward the identification of expanded- spectrum nonnucleoside reverse transcriptase inhibitors which possess increased potency toward K103N-containing mutant human immunodeficiency virus (HIV) and which maintain pharmacokinetic
