Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-06-27
1998-11-10
Owens, Amelia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514252, 514397, 514459, 549214, 549292, 5483111, 544374, A61K 3135, A61K 31415
Patent
active
058345060
ABSTRACT:
This invention pertains to improved antiviral activity of 6,6-disubstituted-5,6-dihydropyran-2-ones caused by judicious placement of certain polar substituents at the 3 and/or 6 positions.
The same substituents which enhance the cellular activity also diminish cytotoxicity further enhancing the desirable properties of these agents as antivirals.
REFERENCES:
Skulnick et al., J. Med. Chem., 1997, 40:7, 1149-1164; "Structure-Based Design of Nonpeptide HIV Protease I Inhibitors: The Sulfonamide-Substituted Cyclooctylpyranones".
Romines et al, J. Med. Chem., 1996, 39:20, 4125-4130; Cycloalkylpyranones and Cycloalkylpyrones as HIV Protease Inhibitors: Exploring the Impact of Ring Size on Structure-Activity Relationships.
Thaisrivongs et al., J. Med. Chem., 1996, 39:23, 4630-4642; "Structure-Based Design of HIV Protease Inhibitors: 5,6-Dihydro-4-hydroxy-2-pyrones as Effective, Nonpeptidic Inhibitors".
Thaisrivongs et al., J. Med. Chem., 1996, 39:22, 4349-4353; "Structure-Based Design of HIV Protease Inhibitors: 5,6-Dihydro-4-hydroxy-2-pyrones as Non-Peptidic Inhibitors".
Judge et al., J. Am. Chem. Soc., 1997, 119:15, 3627-3628; "Asymmetric Syntheses and Absolute Stereochemistry of 5,6-Dihydro-.alpha.-pyrones, A New Class of Potent HIV Protease Inhibitors".
CA 127: 325973.
Boyer, Jr. Frederick Earl
Domagala John Michael
Ellsworth Edmund Lee
Gajda Christopher Andrew
Hagen Susan Elizabeth
Anderson Edizabeth M.
Owens Amelia
Warner-Lambert & Company
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