4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinthiones useful as

Details 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinthiones useful as 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinthiones useful as

1999-03-26

2000-10-03

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544284, 544286, A61K 31517, C07D23978

Patent

active

061273759

ABSTRACT:
The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinthiones of formula I: ##STR1## or stereoisomeric 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.

REFERENCES:
patent: 3660322 (1972-05-01), Bernardi et al.
patent: 5519021 (1996-05-01), Young et al.
Huffman et al., J. Org. Chem, 1995, 60, 1590-1594, "Lithium Alkoxides of Cinchona Alkaloids as Chiral Controllers for Enantioselective Acetylide Addition to Cyclic N-Acyl Ketimines".
Tucker et al., J. Med. Chem, 1994, 37, 2437-2444, "Synthesis of a Series of 4-(Arylethynyl)-6-chloro-4-cyclopropyl-3, 4-dihydroquinazolin-2 (1H)-ones as Novel Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors".
Houpis et al., Tetrahedron Letters, 1994, 35, 6811-6814, "Synthesis of a New Generation Reverse Transcriptase Inhibitor via the BC1.sub.3 /GaCl.sub.3 -induced Condensation of Anilines with Nitriles (Sugasawa Reaction)".
Yamamoto et al., Chemical & Pharmaceutical Bulletin, 1981, 29, 8, 2135-2156, "Synthetic studies on quinazolinone derivatives. The reactions of 2-trichloro-and 2-trifluoroacetamidobenzophenones with primary amines".

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