Janssen R&d Ireland

Tibotec Pharmaceuticals Ltd.

Inge Dierynck

Tim Hugo Maria Jonckers

Stefaan Julien Last

Herman Augustinus De Kock

Judith Baumeister

Gerben Albert Van 't Klooster

Sandra De Meyer

Paul Jozef Gabriel Maria Boonants

Tim Hugo Jonckers

Judith Eva Baumeister

Paul Jozef Boonants

Gerben Albert Eleutherius Van 'T Klooster

The invention concerns novel mutations or mutational profiles of HIV-1 protease cleavage sites (CS) in the Gag region correlated with a phenotype causing alterations in sensitivity to anti-HIV drugs. The present invention also relates to the use of genotypic characterization of a target population of HIV and the subsequent association, i.e., correlation, of this information to phenotypic interpretation in order to correlate virus mutational profiles with drug resistance. The invention further relates to methods of utilizing the mutational profiles of the invention in databases, drug development, i.e., drug design, and drug modification, therapy and treatment design and clinical management.

Mutational profile in HIV-1 GAG cleavage site correlated with phenotypic drug resistance

The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

Lysine related derivatives as HIV aspartyl protease inhibitors

The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors

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Berchem, Belgium

Inge Dierynck