Publication


Featured researches published by Alexandros Vakalopoulos.


Bioorganic & Medicinal Chemistry Letters | 2011

Chromanol derivatives--a novel class of CETP inhibitors.

Alexandros Vakalopoulos; Carsten Schmeck; Michael Thutewohl; Volkhart Min-Jian Li; Hilmar Bischoff; Klemens Lustig; Olaf Weber; Holger Paulsen; Harry Elias

Based on our former development candidate BAY 38-1315, optimization efforts led to the discovery of a novel chemical class of orally active cholesteryl ester transfer protein (CETP) inhibitors. The chromanol derivative 19b is a highly potent CETP inhibitor with favorable pharmacokinetic properties suitable for clinical studies. Chemical process optimization furnished a robust synthesis for a kilogram-scale process.


Bioorganic & Medicinal Chemistry Letters | 2010

Novel tetrahydrochinoline derived CETP inhibitors

Carsten Schmeck; Heike Gielen-Haertwig; Alexandros Vakalopoulos; Hilmar Bischoff; Volkhart Min-Jian Li; Gabriele Wirtz; Olaf Weber

In the course of our efforts to identify orally active cholesteryl ester transfer protein (CETP) inhibitors, we have continued to explore tetrahydrochinoline derivatives. Based on BAY 19-4789 structural modifications led to the discovery of novel cycloalkyl substituted compounds. Thus, example 11b is a highly potent CETP inhibitor both in vitro and in vivo in transgenic mice with favourable pharmacokinetic properties for clinical development.


British Journal of Clinical Pharmacology | 2012

Prediction of a potentially effective dose in humans for BAY 60–5521, a potent inhibitor of cholesteryl ester transfer protein (CETP) by allometric species scaling and combined pharmacodynamic and physiologically-based pharmacokinetic modelling

Olaf Weber; Stefan Willmann; Hilmar Bischoff; Volkhart Min-Jian Li; Alexandros Vakalopoulos; Klemens Lustig; Frank-Thorsten Hafner; Roland Heinig; Carsten Schmeck; Klaus Buehner

AIMS The purpose of this work was to support the prediction of a potentially effective dose for the CETP-inhibitor, BAY 60-5521, in humans. METHODS A combination of allometric scaling of the pharmacokinetics of the CETP-inhibitor BAY 60-5521 with pharmacodynamic studies in CETP-transgenic mice and in human plasma with physiologically-based pharmacokinetic (PBPK) modelling was used to support the selection of the first-in-man dose. RESULTS The PBPK approach predicts a greater extent of distribution for BAY 60-5521 in humans compared with the allometric scaling method as reflected by a larger predicted volume of distribution and longer elimination half-life. The combined approach led to an estimate of a potentially effective dose for BAY 60-5521 of 51 mg in humans. CONCLUSION The approach described in this paper supported the prediction of a potentially effective dose for the CETP-inhibitor BAY 60-5521 in humans. Confirmation of the dose estimate was obtained in a first-in-man study.


Archive | 2012

Substituted annellated pyrimidine and the use thereof

Markus Follmann; Johannes-Peter Stasch; Gorden Redlich; Nils Griebenow; Dieter Lang; Frank Wunder; Walter Hübsch; Niels Lindner; Alexandros Vakalopoulos; Adrian Tersteegen


Archive | 2013

Substituted annulated pyrimidines and triazines, and use thereof

Markus Follmann; Johannes-Peter Stasch; Gorden Redlich; Nils Griebenow; Dieter Lang; Frank Wunder; Walter Hübsch; Alexandros Vakalopoulos; Adrian Tersteegen


Archive | 2012

Substituted annellated pyrimidines and use thereof

Markus Follmann; Johannes-Peter Stasch; Gorden Redlich; Nils Griebenow; Dieter Lang; Frank Wunder; Walter Hübsch; Niels Lindner; Alexandros Vakalopoulos; Adrian Tersteegen


Archive | 2013

Hydroxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use

Alexandros Vakalopoulos; Ingo Hartung; Markus Follmann; Rolf Jautelat; Alexander Straub; Jorma Haβfeld; Niels Lindner; Dirk Schneider; Frank Wunder; Johannes-Peter Stasch; Gorden Redlich; Volkhart Min-Jian Li; Eva-Maria Becker; Andreas Knorr


Archive | 2009

AMINO ACID ESTER PRODRUGS AND THE USE THEREOF

Daniel Meibom; Hans-Georg Lerchen; Alexandros Vakalopoulos; Barbara Albrech-Küpper; Peter Nell; Jörg Keldenich; Katja Zimmermann; Ursula Krenz


Archive | 2008

Substituted aryloxazoles and the use thereof

Peter Nell; Walter Hübsch; Barbara Albrecht-Küpper; Jörg Keldenich; Alexandros Vakalopoulos; Frank Süssmeier; Katja Zimmermann; Dieter Lang; Daniel Meibom


Archive | 2014

BENZYL-SUBSTITUTED PYRAZOLOPYRIDINES AND USE THEREOF

Markus Follmann; Johannes-Peter Stasch; Gorden Redlich; Dieter Lang; Alexandros Vakalopoulos; Frank Wunder; Adrian Tersteegen

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