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Gilles Doerflinger

Aventis Pharma

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Publication

Featured researches published by Gilles Doerflinger.

Bioorganic & Medicinal Chemistry Letters | 2012

Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kβ inhibitors.

Victor Certal; Frank Halley; Angela Virone-Oddos; Fabienne Thompson; Bruno Filoche-Romme; Youssef El-Ahmad; Jean Christophe Carry; Cécile Delorme; Andreas Karlsson; Pierre Yves Abecassis; Loic Vincent; Hélène Bonnevaux; Jean Paul Nicolas; Renaud Morales; Nadine Michot; Isabelle Vade; Audrey Louboutin; Sébastien Perron; Gilles Doerflinger; Bernadette Tric; Sylvie Monget; Christoph Lengauer; Laurent Schio

From a HTS campaign, a new series of pyrimidone anilides exemplified by compound 1 has been identified with good inhibitory activity for the PI3Kβ isoform. The structure of compound 1 in PI3Kγ was solved revealing a binding mode in agreement with the SAR observed on PI3Kβ. These compounds displayed inhibition in the nanomolar range in the biochemical assay and were also potent p-Akt inhibitors in a PTEN-deficient PC3 prostate cancer cell line. Optimization of in vitro pharmocokinetic properties led to compound 25 exhibiting 52% bioavailability in mice and target engagement in an acute PK/PD study.

Archive | 2004

Substituted thieno [2,3-c] pyrazoles and their use as medicinal products

Antony Bigot; François Clerc; Gilles Doerflinger; Serge Mignani; Hervé Minoux

Archive | 2004

Substituted 1H-pyrrolo[3,2-b, 3,2-c, and 2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase lepsilon

William A. Metz; Frank Halley; Gilles Dutruc-Rosset; Yong Mi Choi-Sledeski; Gregory Bernard Poli; David Marc Fink; Gilles Doerflinger; Bao-Guo Huang; Ann Marie Gelormini; Juan Antonio Gamboa; Andrew Giovanni; Joachim E. Roehr; Joseph Tsay; Fernando Camacho; William Joseph Hurst; Stephen Wayne Harnish; Yulin Chiang

Archive | 2004

Chemical derivatives and their application as antitelomerase agents

Patrick Mailliet; Abdelazize Laoui; Jean-François Riou; Gilles Doerflinger; Jean-Louis Mergny; Francois Hamy; Thomas Caulfield

Archive | 2004

Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them

Arielle Genevois-Borella; Jean-Luc Malleron; Jean Bouquerel; Gilles Doerflinger; Andrees Bohme; Gaetan Touyer; Jean-Francois Sabuco; Corrine Terrier; Serge Mignani; Michel Evers; Youssef El-Ahmad

Archive | 1999

Streptogramin derivatives, preparation method and compositions containing same

Pascal Desmazeau; Gilles Doerflinger; Yves Ribeill; Eric Bacque; Jean-Claude Barriere; Gilles Dutruc-Rosset; Gérard Puchault

Archive | 2002

Chemical derivatives and their use as anti-telomerase agent

Patrick Mailliet; Abdelazize Laoui; Jean-François Riou; Gilles Doerflinger; Jean-Louis Mergny; Francois Hamy; Thomas Caulfield

Archive | 2007

Hydrazinocarbonyl-thieno[2,3-C]pyrazoles, Process for Preparing Them, Compositions Containing Them and Use Thereof

Claude Barberis; Jean-Christophe Carry; Gilles Doerflinger; Dominique Barbalat-Damour; François Clerc; Hervé Minoux

Archive | 2004

Pyrazolyl derivatives in the form of drugs for treating acute or chronic neuronal regressions

Arielle Genevois-Borella; Jean-Luc Malleron; Jean Bouquerel; Gilles Doerflinger; Andrees Bohme; Gaetan Touyer; Jean-Francois Sabuco; Corinne Terrier; Serge Mignani; Michel Evers; Youssef El-Ahmad

Archive | 2002

Triazine derivatives and their application as antitelomerase agents

Patrick Mailliet; Abdelazize Laoui; Jean-François Riou; Gilles Doerflinger; Jean-Louis Mergny; Francois Hamy; Thomas Caulfield

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Collaboration

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Gilles Dutruc-Rosset

Aventis Pharma

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Eric Bacque

Rhône-Poulenc

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Jean-Claude Barriere

Institut de Chimie des Substances Naturelles

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Pascal Desmazeau

Rhône-Poulenc

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Arielle Genevois-Borella

Aventis Pharma

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Hervé Minoux

Aventis Pharma

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Jean-Christophe Carry

Aventis Pharma

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Yves Ribeill

Rhône-Poulenc

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Abdelazize Laoui

Rhône-Poulenc

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Claude Barberis

Aventis Pharma

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