The United States of America As Represented by the Department of Health

Hoffmann-la Roche Inc.

The United States of America, As Represented by the Secretary, Department of Health and Human Services

The United States of America

Sanyo-kokusaku Pulp Co., Ltd.

The Government of the United States of America, As Represented by the

University of Illinois

Hiroaki Mitsuya

Arun K Ghosh

Samuel Broder

Victor E Marquez

Robert Yarchoan

Manfred Weigele

John W Erickson

John S Driscoll

James A Kelley

Christopher K-h Tseng

Hidetoshi Yoshioka

Jiri Zemlicka

Steve Yik-Kai Tam

Sergei V Gulnik

David G Johns

Kunichika Murakami

Joseph J Barchi, Jr

Eiji Kojima

Harry Ford, Jr

Joseph E Tomaszewski

Takuma Shirasaka

Samuel Broger

Seiji Hayashi

Shashikant Phadtare

Arun K Gosh

A method for inhibiting intracellular replication of HIV in an HIV-infected individual comprising contacting the HIV reverse transcriptase in the HIV-infected cells with 2',3'-dideoxyadenosine-5'-triphosphate whose source is 2',3'-dideoxyadenosine or a pharmaceutically acceptable salt or prodrug thereof.

Method of inhibiting HIV replication with 2',3'-dideoxyadenosine

An anti-AIDS virus agent is disclosed, which is characterized in that it contains the 2',3'-dideoxypurinenucleosides represented by the chemical formula (I): ##STR1## as an effective ingredient.

Pharmaceutical composition containing

Methods of treating a human infected with human immunodeficiency virus (HIV), such as a human with AIDS, with the purina nucleotides 2',3'-dideoxy-2'-beta-fluoroadenosine (FddA) and 2',3'-dideoxy-2'-beta-fluoroinosine (FddI) are disclosed. These nucleotides are stable in an acid environment and thus can be used for oral administration. Methods of inhibiting human immunodeficiency virus replication in a human T cell using these purina nucleotides are also disclosed.

2',3'-dideoxy-2'-fluoro-purine nucleosides and methods for using same

Purine nucleosides active against human immunodeficiency virus which are substituted at the 2'-position by a strong electronegative group such as fluorine are stable in an acid environment and thus can be used for oral administration.

Acid stable purine dideoxynucleosides

The present invention relates, in general, to prodrugs. In particular, the present invention relates to lipophilic, aminohydrolase-activated, anti-viral nucleoside prodrug compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds.

Lipophilic, aminohydrolase-activated prodrugs

A preferred method and dosages for treatment of retrovirus-induced dementia by the administration of 2',3'-dideoxyinosine(ddI) is disclosed.

Treatment of retroviral induced dementia by administration of

A method for tearing retroviral infections including acquired immune deficiency syndrome (AIDS) with 2',3'-dideoxyinosine or 2',3'-dideoxyadenosine is disclosed. This antiviral effect is irreversible with 2',3'-dideoxyinosine and 2',3'-dideoxyadenosine but reversible with 2',3'-dideoxyguanosine.

Method of treating HIV with 2',3'-dideoxyinosine

A preferred method and dosages for the short and long-term treatment of human retroviral infections, or retroviral-like infections, including acquired immunodeficiency syndrome (AIDS) and other manifestations of human immunodeficiency virus (HIV) infection, with 2',3'-dideoxyinosine (ddl) are disclosed, along with a protocol for halting and restarting 2',3'-dideoxyinosine to minimize certain side effects.

Treatment of human retroviral infections with 2',3'-dideoxyinosine alone

Compounds which are active against retroviruses have the following formula

Pyrimidine and purine 1,2-butadiene-4-ols as anti-retroviral agents

Compositions containing 2',3'-dideoxycytidine and its triphosphates for use in treating retroviral infections including acquired immune deficiency syndrome (AIDS) are disclosed with preferred methods of treatment which provide protection against cytophatic effects of human immunodeficiency virus (HIV).

Antiviral compositions and methods

Compositions containing 2',3'-dideoxyadenosine, 2',3'-dideoxyinosine, and dideoxyguanosine and their triphosphates for use in treating retroviral infections including acquired immune deficiency syndrome (AIDS) are disclosed with preferred methods of treatment which provide protection against cytopathic effects of human immunodeficiency virus (HIV).

A-B-C wherein A and C are each independently 2',3' dideoxynucleosides and B is a linking group; and a method of treating or preventing a retroviral injection in a subject by administering the compounds of the invention.

Anti-retroviral compounds

This invention is an immortalized T-cell clone, designated ATH8, which is highly sensitive to the cytopathic effect of HTLV-III. The ATH8 T-cell clone is used in mass screening systems to rapidly and easily determine the in vitro capacity of new drugs or other agents to inactivate or inhibit HTLV-III or related cytopathic retroviruses.

Growing community of inventors

Rockville, MD, United States of America

Hiroaki Mitsuya