Tibotec Pharmaceuticals Ltd.

Janssen R&d Ireland

Sandra De Meyer

Marie-Pierre T M M G De Bethune

Hilde Azijn

Abdellah Tahri

Herman Augustinus De Kock

Michael Eissenstat

Piet Tom Bert Paul Wigerinck

Lieven Elvire Colette Baert

Kurt Hertogs

Lieve Emma Jan Michiels

Gerben Albert Van 't Klooster

Dong Xie

Inge Dierynck

Rong Jian Lu

Marie-Pierre TMMG De Bethune

The present invention is directed to the field of nucleic acid diagnostics and the identification of base variation in target nucleic acid sequences. More particularly, the present invention relates to the use of such 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 also relates to methods of utilizing the mutational profiles of the invention in drug development, i.e., drug discovery, drug design, drug modification, and therapy, treatment design, clinical management and diagnostic analysis.

Mutational profiles in HIV-1 protease correlated with phenotypic drug resistance

A method for improving the pharmacokinetics of drugs, which are metabolized by cytochrome P450 monooxygenase is disclosed. More specifically it relates to a method for improving the pharmacokinetics of retroviral protease inhibitors and in particular for improving the pharmacokinetics of human immunodeficiency virus (HIV) protease inhibitors. A pharmaceutical composition and its use in the manufacture of a medicament for the inhibition or treatment of an HIV infection or AIDS in a human being are also part of the invention.

Use of a sulfonamide compound for improving the pharmacokinetics of a drug

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 a compound having the formula (I) a N-oxide form, a stereochemical isomer, racemic mixture, salt, prodrug, ester or metabolite thereof. It further relates to processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.

Small molecule entry inhibitors

Mutational profiles in HIV-1 protease correlated with phenotypic protease inhibitor resistance

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Sandra De Meyer