Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Piet Wigerinck"'
Autor:
Fred Stappers, Alfons Wouters, Koen Iterbeke, Francois Marc Karel Jozef, Guenter Kraus, Piet Wigerinck, Laurent Schueller, Lieven Baert, Pieter Van Remoortere, Esther Dina Guido Basstanie, Gerben Albert Eleutherius Van 'T Klooster, Willy Maria Albert Carlo Dries, Jan Rosier, Paul Stevens
Publikováno v:
European Journal of Pharmaceutics and Biopharmaceutics. 72:502-508
Long-acting parenteral formulations of antiretrovirals could facilitate maintenance and prophylactic treatment in HIV. Using the poorly water- and oil-soluble non-nucleoside reverse transcriptase inhibitor (NNRTI) TMC278 (rilpivirine) as base or hydr
Autor:
Pierre Raboisson, Tse-I Lin, Bertil Samuelsson, Frederic Delouvroy, Katrien Vermeiren, Lotta Vrang, Oliver Lenz, Kenneth Simmen, Piet Wigerinck, Michael Edlund, Annick Scholliers, Thierry Verbinnen, Herman de Kock, Åsa Rosenquist, Gregory Fanning
Publikováno v:
Antimicrobial Agents and Chemotherapy. 53:1377-1385
The hepatitis C virus (HCV) NS3/4A serine protease has been explored as a target for the inhibition of viral replication in preclinical models and in HCV-infected patients. TMC435350 is a highly specific and potent inhibitor of NS3/4A protease select
Autor:
Michael Edlund, Oliver Lenz, Pia Cecilia Kahnberg, Stefan Lindström, Frederic Delouvroy, Dominique Louis Nestor Ghislain Surleraux, Magnus Nilsson, Dmitry Antonov, Anders Eneroth, Wim Van De Vreken, Kristina Wikström, Tse-I Lin, Piet Wigerinck, Kenneth Simmen, Vladimir Ivanov, Marleen Van Dooren, Susana Ayesa, Hu Lili, Abdellah Tahri, Åsa Rosenquist, Lotta Vrang, Per-Ola Johansson, Vendeville Sandrine Marie Hele, Herman de Kock, Pierre Raboisson, Bertil Samuelsson, Björn Classon, Natalie Maria Francisca Kindermans, David McGowan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:6189-6193
A novel series of P3-truncated macrocyclic HCV NS3/4A protease inhibitors containing a P2 proline-urea or carbamate scaffold was synthesized. Very potent inhibitors were obtained through the optimization of the macrocycle size, urea and proline subst
Autor:
Frederic Delouvroy, Dominique Louis Nestor Ghislain Surleraux, Herman de Kock, Oliver Lenz, David McGowan, Pierre Raboisson, Magnus Nilsson, Åsa Rosenquist, Wim Van De Vreken, Hu Lili, Piet Wigerinck, Tse-I Lin, Bertil Samuelsson, Abdellah Tahri, Vendeville Sandrine Marie Hele, Kenneth Simmen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5095-5100
Starting from the previously reported HCV NS3/4A protease inhibitor BILN 2061, we have used a fast-follower approach to identify a novel series of HCV NS3/4A protease inhibitors in which (i) the P3 amino moiety and its capping group have been truncat
Autor:
Jan Rosier, Lieven Baert, Doug Macbride, Herman Borghys, Yanik Tardy, Gerben Albert Eleutherius Van 'T Klooster, Laurent Schueller, Ellen Clessens, Elke Van Gyseghem, Pieter Van Remoortere, Guy Van den Mooter, Piet Wigerinck
Publikováno v:
International Journal of Pharmaceutics. 355:38-44
Factors such as insufficient drug potency, non-compliance and restricted tissue penetration contribute to incomplete suppression of Human Immunodeficiency Virus (HIV) and the difficulty to control this infection. Infusion via standard catheters can b
Autor:
Sophie Lachau-Durand, Piet Wigerinck, Laurent Schueller, Ellen Clessens, Guy Van den Mooter, Lieven Baert, Herman Borghys, Jan Rosier, Tim Hugo Maria Jonckers, Elke Van Gyseghem, Pieter Van Remoortere
Publikováno v:
International Journal of Pharmaceutics. 355:45-52
A dog model was developed to test the capacity of boosters for antiretroviral medication. Two dogs were implanted with a modified constant-flow Codman 3000® infusion pump, adapted to release viscous solutions of darunavir (TMC114) at a constant rate
Autor:
Piet Wigerinck, Maryam Ehteshami, Jerome Deval, Bertrand Van Schoubroeck, Tania Ivens, Marcia Van Ginderen, Eva Bettens, Dirk Jochmans, Matthias Götte, Inky De Baere, Pascale Dehertogh, Kurt Hertogs, Bart Rudolf Romanie Kesteleyn, Herwig Van Marck
Publikováno v:
Journal of Virology. 80:12283-12292
We have discovered a novel class of human immunodeficiency virus (HIV) reverse transcriptase (RT) inhibitors that block the polymerization reaction in a mode distinct from those of the nucleoside or nucleotide RT inhibitors (NRTIs) and nonnucleoside
Autor:
Bart De Spiegeleer, Christian Burvenich, Lieven Van Vooren, Filip Dumont, Piet Wigerinck, Kathelijne Peremans, Lieven Baert, Jan Rosier, Guido Slegers
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 49:683-686
[77Br]TMC125-R165335 (etravirine) was synthesized for imaging studies by SPECT. Labelling was performed with bromine-77 by electrophilic substitution of the desbromo-precursor 4-{6-amino-2-[(4-cyanophenyl)amino]pyrimidin-4-yloxy}-3,5-dimethylbenzenec
Autor:
Dominique Louis Nestor Ghislain Surleraux, Anik Peeters, Sandra De Meyer, Rudi Wilfried Jan Pauwels, Moses Prabu-Jeyabalan, Piet Wigerinck, Celia A. Schiffer, Geert M. E. Pille, Hilde Azijn, Louis J. R. Maes, Herman Augustinus De Kock, Sandrine Marie Helene Vendeville, Wim Gaston Verschueren, Marie-Pierre de Béthune, Nancy M. King
Publikováno v:
Journal of medicinal chemistry
On the basis of structural data gathered during our ongoing HIV-1 protease inhibitors program, from which our clinical candidate TMC114 9 was selected, we have discovered new series of fused heteroaromatic sulfonamides. The further extension into the
Autor:
Celia A. Schiffer, Moses Prabu-Jeyabalan, Piet Wigerinck, Ellen A. Nalivaika, Marie-Pierre de Béthune, Nancy M. King
Publikováno v:
Journal of Virology. 78:12012-12021
TMC114, a newly designed human immunodeficiency virus type 1 (HIV-1) protease inhibitor, is extremely potent against both wild-type (wt) and multidrug-resistant (MDR) viruses in vitro as well as in vivo. Although chemically similar to amprenavir (APV