Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-04-08
2000-09-26
Ford, John M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5142358, 5142521, 51425202, 514241, 5142225, 544284, 544286, 544 5, 544116, 544257, 544264, 544238, 544 8, 544180, C07D40106, C07D40306, A61K 31517
Patent
active
061243027
ABSTRACT:
The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: ##STR1## 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:
R.sup.1 is C.sub.1-3 alkyl substituted with 1-7 halogen;
R.sup.2 is optionally substituted C.sub.1-5 alkyl, optionally substituted C.sub.2-5 alkenyl, or optionally substituted C.sub.2-5 alkynyl;
R.sup.3, at each occurrence, is independently selected from C.sub.1-4 alkyl, OH, C.sub.1-4 alkoxy, F, Cl, Br, I, NR.sup.5 R.sup.5a, NO.sub.2, CN, C(O)R.sup.6, NHC(O)R.sup.7, and NHC(O)NR.sup.5 R.sup.5a ;
R.sup.5 and R.sup.5a are independently selected from H and C.sub.1-3 alkyl;
R.sup.6 is selected from H, OH, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, and NR.sup.5 R.sup.5a ;
R.sup.7 is selected from C.sub.1-3 alkyl and C.sub.1-3 alkoxy;
R.sup.8 is selected from H, C.sub.3-5 cycloalkyl, and C.sub.1-3 alkyl; and,
n is selected from 0, 1, 2, 3, and 4.
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Corbett Jeffrey W.
Ko Soo S.
Dupont Pharmaceuticals
Ford John M.
VanAtten Mary K.
Vance David H.
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