Abstract: Methods for improving the cellular uptake of protease inhibitors (e.g., HIV protease inhibitor), alone or in the presence of one or more additional therapeutic agents, in protease inhibitor-based therapies, involving administration of one or more AAG-binding compounds, such as macrolide or lincosamide antibiotics, which have sufficient binding affinity for AAG to competitively bind AAG in the presence of the protease inhibitor.
Type:
Grant
Filed:
August 30, 1995
Date of Patent:
May 12, 1998
Assignees:
Raymond F. Schinazi, University of Alabama at Birmingham
Inventors:
Jean-Pierre Sommadossi, Raymond F. Schinazi
Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y H is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is H or an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2.The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
February 24, 1998
Assignees:
Mahmoud H. el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
Inventors:
Mahmoud H. el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2.The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging.
Type:
Grant
Filed:
November 2, 1993
Date of Patent:
December 19, 1995
Assignees:
Mahmoud H. el Kouni, Fardos N. M. Naguib, F. Schinazi
Inventors:
Mahmoud el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi