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Featured researches published by Dieter Wiedenmayer.


Bioorganic & Medicinal Chemistry Letters | 2011

Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores

Raj Betageri; Thomas A. Gilmore; Daniel Kuzmich; Thomas M. Kirrane; Jörg Bentzien; Dieter Wiedenmayer; Younes Bekkali; John R. Regan; Angela Berry; Bachir Latli; Alison Kukulka; Tazmeen N. Fadra; Richard M. Nelson; Susan E. Goldrick; Ljiljana Zuvela-Jelaska; Don Souza; Josephine Pelletier; Roger M. Dinallo; Mark Panzenbeck; Carol Torcellini; Heewon Lee; Edward Pack; Christian Harcken; Gerald Nabozny; David S. Thomson

We report a SAR of non-steroidal glucocorticoid mimetics that utilize indoles as A-ring mimetics. Detailed SAR is discussed with a focus on improving PR and MR selectivity, GR agonism, and in vitro dissociation profile. SAR analysis led to compound (R)-33 which showed high PR and MR selectivity, potent agonist activity, and reduced transactivation activity in the MMTV and aromatase assays. The compound is equipotent to prednisolone in the LPS-TNF model of inflammation. In mouse CIA, at 30 mg/kg compound (R)-33 inhibited disease progression with an efficacy similar to the 3 mg/kg dose of prednisolone.


Bioorganic & Medicinal Chemistry Letters | 2010

SAR studies of non-zinc-chelating MMP-13 inhibitors: Improving selectivity and metabolic stability

Donghong Amy Gao; Zhaoming Xiong; Alexander Heim-Riether; Laura M Amodeo; E. Michael August; Xianhua Cao; Leonard Ciccarelli; Brandon Collins; Kyle E. Harrington; Kathleen Haverty; Melissa Hill-Drzewi; Xiang Li; Shuang Liang; Steluta Mariana Margarit; Neil Moss; Nelamangala Nagaraja; John R. Proudfoot; Rene Roman; Sabine Schlyer; Lana Louise Smith Keenan; Steven John Taylor; Bernd Wellenzohn; Dieter Wiedenmayer; Jun Li; Neil A. Farrow


Archive | 2005

Novel long-working beta-2-agonists and use thereof as medicaments

Christoph Hoenke; Klaus Rudolf; Thierry Bouyssou; Ingo Konetzki; Philipp Lustenberger; Jürgen Mack; Andreas Schnapp; Dieter Wiedenmayer


Archive | 2006

Alpha-Carbolines as CDK-1 inhibitors

Peter Sennhenn; Andreas Mantoulidis; Matthias Treu; Ulrike Tontsch-Grunt; Walter Spevak; Darryl Mcconnell; Andreas Schoop; Ralph Brueckner; Albrecht Jacobi; Ulrich Guertler; Gisela Schnapp; Christian Klein; Frank Himmelsbach; Alexander Pautsch; Bodo Betzemeier; Lars Herfurth; Juergen Mack; Dieter Wiedenmayer; Gerd Bader; Ulrich Reiser


Archive | 2005

Long acting beta-2-agonists and their use as medicaments

Thierry Bouyssou; Ingo Konetzki; Philipp Lustenberger; Juergen Mack; Andreas Schnapp; Dieter Wiedenmayer; Christoph Hoenke; Klaus Rudolf


Archive | 2011

HETEROCYCLOALKYL-CONTAINING THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS

Thorsten Lehmann-Lintz; Joerg Kley; Norbert Redemann; Achim Sauer; Leo Thomas; Dieter Wiedenmayer; Matthias Austen; John Danilewicz; Martin Schneider; Kay Schreiter; Phillip Black; Wesley Blackaby; Ian Linney


Archive | 2011

Thienopyrimidines containing a substituted alkyl group for pharmaceutical compositions

Armin Heckel; Frank Himmelsbach; Joerg Kley; Thorsten Lehmann-Lintz; Norbert Redemann; Achim Sauer; Leo Thomas; Dieter Wiedenmayer; Phillip Black; Wesley Blackaby; Ian Linney; Matthias Austen; John Danilewicz; Martin Schneider; Kay Schreiter


Archive | 2011

4 - [cycloalkyloxy (hetero) arylamino] thieno [2, 3 - d] pyrimidines having mnkl/ mnk2 inhibiting activity for pharmaceutical compositions

Thorsten Lehmann-Lintz; Armin Heckel; Joerg Kley; Elke Langkopf; Norbert Redemann; Achim Sauer; Leo Thomas; Dieter Wiedenmayer; Matthias Austen; John Danilewicz; Martin Schneider; Kay Schreiter; Phillip Black; Wesley Blackaby; Ian Linney


Archive | 2014

Sulfoximine substituted quinazolines for pharmaceutical compositions

Andreas Blum; Dirk Gottschling; Armin Heckel; Joerg P. Hehn; Bernhard Schmid; Dieter Wiedenmayer


Archive | 2011

Compounds as bradykinin B1 antagonists

Norbert Hauel; Angelo Ceci; Henri Doods; Ingo Konetzki; Juergen Mack; Henning Priepke; Annette Schuler-Metz; Rainer Walter; Dieter Wiedenmayer

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