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Christos Tsaklakidis

Merck & Co.

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Publication

Featured researches published by Christos Tsaklakidis.

Bioorganic & Medicinal Chemistry Letters | 2014

Structure-based optimization of non-peptidic Cathepsin D inhibitors.

Ulrich Grädler; Paul Czodrowski; Christos Tsaklakidis; Markus Klein; Daniela Werkmann; Sven Lindemann; Klaus Maskos; Birgitta Leuthner

We discovered a novel series of non-peptidic acylguanidine inhibitors of Cathepsin D as target for osteoarthritis. The initial HTS-hits were optimized by structure-based design using CatD X-ray structures resulting in single digit nanomolar potency in the biochemical CatD assay. However, the most potent analogues showed only micromolar activities in an ex vivo glycosaminoglycan (GAG) release assay in bovine cartilage together with low cellular permeability and suboptimal microsomal stability. This new scaffold can serve as a starting point for further optimization towards in vivo efficacy.

Archive | 2001

Substituted biphenyl derivatives

Horst Juraszyk; Dieter Dorsch; Werner Mederski; Christos Tsaklakidis; Christopher Bames; Johannes Gleitz

Archive | 2004

Pyrrolidino-1,2-dicarboxy-1-(phenylamide)-2-(4-(3-oxo-morpholino-4-yl)-phenylamide) derivatives and related compounds for use as inhibitors of coagulation factor xa in the treatment of thrombo-embolic diseases

Christos Tsaklakidis; Dieter Dorsch; Werner Mederski; Bertram Cezanne; Johannes Gleitz

Archive | 2000

Pyrazole-3-on-derivative as factor xa inhibitors

Dieter Dorsch; Horst Juraszyk; Werner Mederski; Christos Tsaklakidis; Hanns Wurziger; Sabine Bernotat-Danielowski; Guido Melzer

Archive | 1999

Imidazo[4,5-c]-pyridine-4-on-derivatives

Werner Mederski; Horst Juraszyk; Hanns Wurziger; Christos Tsaklakidis; Dieter Dorsch; Sabine Bernotat-Danielowski; Guido Melzer; Soheila Anzali

Archive | 2004

Method for the production of pyrrolidine-1,2-dicarboxylic acid-1-(phenyl(-amide))-2(phenyl(-amide)) derivatives and 1-(phenylcarbamoyl)-pyrrolidine-2-carboxylic acid derivatives as intermediate products

Werner Mederski; Christos Tsaklakidis; Dieter Dorsch; Bertram Cezanne; Johannes Gleitz

Archive | 2001

Aza-amino acid derivatives (factor Xa inhibitors 15)

Werner Mederski; Horst Juraszyk; Dieter Dorsch; Christos Tsaklakidis; Johannes Gleitz; Christopher Barnes

Archive | 2007

3-AMINOIMIDAZO 1,2-A PYRIDINE DERIVATIVES HAVING AN SGLT1- AND SGLT2-INHIBITING ACTION FOR THE TREATMENT OF TYPE 1 AND TYPE 2 DIABETES

Markus Klein; Rolf Gericke; Norbert Beier; Bertram Cezanne; Christos Tsaklakidis; Werner Mederski

Archive | 2007

3 -amino-imidazo[1, 2-a]pyridine derivatives as sglt inhibitors

Werner Mederski; Norbert Beier; Bertram Cezanne; Rolf Gericke; Markus Klein; Christos Tsaklakidis

Archive | 2005

Carbonyl compound-containing drug and the use thereof

Bertram Cezanne; Dieter Dorsch; Werner Mederski; Christos Tsaklakidis; Johannes Gleitz

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Werner Mederski

Merck

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Dieter Dorsch

Merck

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Bertram Cezanne

Merck

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Johannes Gleitz

Merck

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Markus Klein

Merck

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Christopher Barnes

Merck

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Norbert Beier

Merck

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Horst Juraszyk

Merck

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Birgitta Leuthner

Merck

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Wolfgang Staehle

Merck

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