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' 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.

Os compostos são divulgados tratando o AIDS, o herpes, e outras infecções viral por meio dos derivatives do lipid de agentes antiviral. Os compostos consistem nos analogues do nucleoside que têm a atividade antiviral que são ligados, geralmente através de um grupo do phosphate na posição 5' do resíduo do pentose, a um de um grupo selecionado dos lipids. A natureza lipophilic destes compostos fornece vantagens sobre o uso do sozinho análogo do nucleoside. Ele também makes ele possível incorporá-los sozinho na estrutura lamellar dos liposomes, ou combinado com as moléculas similares. No formulário dos liposomes, estes agentes antiviral são feitos exame preferentially acima por macrophages e por monocytes, as pilhas que foram encontradas para abrigar o vírus do HIV do alvo. O specificity adicional do local pode ser incorporado nos liposomes com a adição dos ligands, tais como os antibodies monoclonal ou os outros peptides ou proteínas que ligam às proteínas viral. Os analogues eficazes do nucleoside são dideoxynucleosides, azidothymine (AZT), e acyclovir; os grupos do lipid podem ser glycolipids, sphingolipids, phospholipids ou ácidos fatty. Os compostos persistem, após o hydrolysis intracellular, como nucleosides antiviral phosphorylated ou non-non-phosphorylated. Os compostos são eficazes em melhorar o efficacy de analogues antiviral do nucleoside prolongando a atividade antiviral depois que a administração da droga terminou, e em impedir o replication retroviral nas infecções de HIV que se tornaram resistentes à terapia com formulários convencionais dos agentes antiretroviral.