Idenix Pharmaceuticals, Inc.

Other

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

Repla Chemical Ltd.

Marino Artico

Jean-Pierre Sommadossi

Paolo La Colla

Adel M Moussa

Yves Pommier

Martin L Bryant

Richard Storer

Paulo LaColla

Antonello Mai

Christophe Marchand

Paolo LaColla

Silvio Massa

Roberta Costi

Roberto Di Santo

Federico Corelli

Romano Silvestri

Enzo Tramontano

Novel quinoline inhibitors of retroviral integrase, particularly HIV-1 integrase. The quinoline inhibitors are oxoquinolines that can be used for preventing or treating AIDS or HIV infection in a subject.

Quinolin-4-ones as inhibitors of retroviral integrase for the treatment of HIV, AIDS and AIDS related complex (ARC)

This invention is in the area of phenylindoles that are useful for the treatment of HIV infection, and, in particular, phenylindoles that exhibit significant activity against resistant strains of HIV. The phenylindoles have at least two substituents other than hydrogen on the benzo ring of the indole function, preferably at the 4' and 5&#x2032;, 5&#x2032; and 6&#x2032; or the 5&#x2032; and 7&#x2032; positions, optionally in combination with disubstitution at positions 3&#x2033; and 5&#x2033; on the phenyl ring of the compound, and carboxamide containing moieties at position-2 on the indole group of the compound. Methyl is a preferred group for substitution on the phenyl ring. Preferred substituents for the benzo ring of the indole function include but are not limited to chlorine, fluorine, bromine, iodine, CF, methoxy, CN, and NO.

Substituted phenylindoles for the treatment of HIV

The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.

Phenylindoles for the treatment of HIV

The invention concerns novel substituted 6-benzyl-4-oxopyrimidines and pharmaceutically acceptable salts thereof. These compounds inhibit reverse transcriptase encoded by human immunodeficiency virus (HIV), and are useful to prevent and treat HIV infection and acquired immune deficiency syndrome (AIDS). Pharmaceutical compositions containing the compounds and a method of use of the present compounds and other agents for the treatment of AIDS and viral infection by HIV are also envisaged.

Substituted 6-benzyl-4-oxopyrimidines, process for their preparation and pharmaceutical compositions containing them

A method for inhibiting sexual transmission of HIV comprising topically applying to the skin or epithelial tissue of a human a composition comprising a non-nucleoside reverse transcriptase inhibitor (&ldquo;NNRTI&rdquo;) that is able to inhibit viral replication for periods exceeding 12, 24, or even 36 days, at concentrations below even 10 &mgr;M. In one embodiment the NNRTI is a dihydro-alkyloxy-benzyl-oxopyrimidine (DABO).

Methods for inhibiting the transmission of HIV using topically applied substituted 6-benzyl-4-oxopyrimidines

Antirhinoviral compounds having the formula ##STR1## wherein R is hetrocyclic, particularly pyrrole or pyrrolidine, X is H.sub.2 or O, n IS 3 to 7, and R.sub.1 is substituted phenyl are disclosed.

Synthetic derivatives of pyrrole and pyrrolidine suitable for the

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Rome, Italy

Marino Artico