0350287-A2 is referenced by 132 patents and cites 8 patents.

Compounds are disclosed for treating AIDS, herpes, and other viral infections by means of lipid derivatives of antiviral agents. The compounds consist of nucleoside analogues having antiviral activity which are linked, commonly through a phosphate group at the 5 min position of the pentose residue, to one of a selected group of lipids. The lipophilic nature of these compounds provide advantages over the use of the nucleoside analogue alone. It also makes it possible to incorporate them into the lamellar structure of liposomes, either alone or combined with similar molecules. In the form of liposomes, these antiviral agents are preferentially taken up by macrophages and monocytes, cells which have been found to harbor the target HIV virus. Additional site specificity may be incorporated into the liposomes with the addition of ligands, such as monoclonal antibodies or other peptides or proteins which bind to viral proteins. Effective nucleoside analogues are dideoxynucleosides, azidothymine (AZT), and acyclovir; lipid groups may be glycolipids, sphingolipids, phospholipids or fatty acids. The compounds persist, after intracellular hydrolysis, as phosphorylated or non-phosphorylated antiviral nucleosides. The compounds are effective in improving the efficacy of antiviral nucleoside analogues by prolonging the antiviral activity after the administration of the drug has ended, and in preventing retroviral replication in HIV infections which have become resistant to therapy with conventional forms of the antiretroviral agents.

Lipid derivatives of antiviral nucleosides, liposomal incorporation and method of use.
Application Number
EP19890306815 19890705
Publication Number
0350287 (A2)
Application Date
July 5, 1989
Publication Date
January 10, 1990
Stuhmiller Louise M
Kumar Raj
Hostetler Karl Y
C07H 19/173
C07H 19/073
C07F 09/6561
C07F 09/656
C07F 09/6558
C07F 09/655
A61K 31/70
A61K 09/127
C07H 19/00
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A61P 31/00
A61K 31/7042
A61K 31/70
A61K 09/127
C07H 19/207
C07H 19/16
C07H 19/06
C07H 19/04
C07H 15/04
A61P 31/12
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A61K 31/7052
A61K 31/7042
A61K 31/70
A61K 09/127
C07H 19/10
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