Tibotec Pharmaceuticals Ltd.

Conjuchem Biotechnologies Inc.

Frontier Biotechnologies, Co., Ltd.

Frontiers Biotechnologies Col, Ltd.

Janssen R&d Ireland

Dong Xie

John W Erickson

He Jiang

Abdellah Tahri

Michael Eissenstat

Dominique P Bridon

Martin Robitaille

Kurt Hertogs

Marie-Pierre T M M G De Bethune

Grant A Krafft

Lieve Emma Jan Michiels

Sandra De Meyer

Jun Liang

Wei Cao

Rong Jian Lu

Sandra DeMeyer

Elena Afonina

Marie-Pierre TMMG De Bethune

The claimed invention is directed toward modified HIV-1 gp41 C-terminal heptad repeat fusion inhibitors. In particular, peptide derivatives of C-34 were prepared (e.g., FB006M) and modified with 3-maleimidoproionic acid (MPA), which allows rapid and irreversible conjugation to serum albumin at a 1:1 molar ratio. These polypeptides have an extended half-life in vivo and display potent antiviral activity against HIV-1.

Method of inhibiting HIV-1 replication by administering modified GP41 C34 peptide derivatives with enhanced pharmacological properties

The present invention relates to C34 peptide derivatives that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to C34 derivatives having inhibiting activity against human immunodeficiency virus (HIV), respiratory syncytial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) with long duration of action for the treatment of the respective viral infections.

Long lasting fusion peptide inhibitors for HIV infection

This invention relates to gp41 peptide derivatives that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to gp41 derivatives having inhibiting activity against human immunodeficiency virus (HIV) and simian immunodeficiency virus (SIV) with enhanced duration of action for the treatment of the respective viral infections.

Human immunodeficiency virus (HIV) gp41 peptide derivatives with enhanced solubility and antiviral activity

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

Methods for isothermal titration calorimetry analysis of the binding affinity of protease inhibitors to plasma proteins. A method that can quantitatively calculate free drug concentrations of protease inhibitors in human plasma, as well as a method to calculate therapeutic amounts and dosage regimens. Furthermore, the present invention provides a method that can calculate the effect of plasma proteins on the antiviral activity (EC50 values) of protease inhibitors from their binding affinities to plasma proteins. The present invention provides as well a method that can evaluate the in vivo anti-HIV efficacy of PIs in human plasma.

Methods for determining plasma free drug concentration by direct measurement of binding affinity of protease inhibitors to plasma proteins

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Dong Xie