Remy Lemoine
Hoffmann-La Roche
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Publication
Featured researches published by Remy Lemoine.
Bioorganic & Medicinal Chemistry Letters | 2003
Constantine G. Boojamra; Remy Lemoine; Johanne Blais; Nicole G. Vernier; Karin Ann Stein; Angela Magon; Suzanne Chamberland; Scott J. Hecker; Ving J. Lee
Dihydropacidamycins having an antibacterial spectrum modified from that of the natural product pacidamycins and mureidomycins have been synthesized. Synthetic dihydropacidamycins with noteworthy antibacterial activity against wild-type and resistant Escherichia coli have been identified (MIC=4-8 microg/mL). Some dihydropacidamycins are shown to have activity against multi-resistant clinical strains of Mycobacterium tuberculosis. Compounds of this class are inhibitors of the cell wall biosynthetic enzyme, MraY.
Journal of Medicinal Chemistry | 2014
Francisco Xavier Talamas; Sarah C. Abbot; Shalini Anand; Ken A. Brameld; David S. Carter; Jun Chen; Dana E. Davis; Javier de Vicente; Amy Fung; Leyi Gong; Seth F. Harris; Petra Inbar; Sharada Shenvi Labadie; Eun Kyoung Lee; Remy Lemoine; Sophie Le Pogam; Vincent Leveque; Jim Li; Joel McIntosh; Isabel Najera; Jaehyeon Park; Aruna Railkar; Sonal Rajyaguru; Michael Sangi; Ryan Craig Schoenfeld; Leanna R. Staben; Yun-Chou Tan; Joshua Paul Gergely Taygerly; Armando G. Villaseñor; Paul Weller
In the past few years, there have been many advances in the efforts to cure patients with hepatitis C virus (HCV). The ultimate goal of these efforts is to develop a combination therapy consisting of only direct-antiviral agents (DAAs). In this paper, we discuss our efforts that led to the identification of a bicyclic template with potent activity against the NS5B polymerase, a critical enzyme on the life cycle of HCV. In continuation of our exploration to improve the stilbene series, the 3,5,6,8-tetrasubstituted quinoline core was identified as replacement of the stilbene moiety. 6-Methoxy-2(1H)-pyridone was identified among several heterocyclic headgroups to have the best potency. Solubility of the template was improved by replacing a planar aryl linker with a saturated pyrrolidine. Profiling of the most promising compounds led to the identification of quinoline 41 (RG7109), which was selected for advancement to clinical development.
Bioorganic & Medicinal Chemistry Letters | 2010
Remy Lemoine; Ann C. Petersen; Lina Setti; Jutta Wanner; Andreas Jekle; Gabrielle Heilek; André deRosier; Changhua Ji; Pamela Berry; David Mark Rotstein
Replacement of a secondary amide with an N-acyl or N-sulfonyl gem-disubstituted azacyle in a series of CCR5 antagonists led to the identification of compounds with excellent in vitro HIV antiviral activity and increased intrinsic membrane permeability.
Current Topics in Medicinal Chemistry | 2010
Remy Lemoine; Jutta Wanner
This review will focus on the discovery and clinical development of small molecule antagonists of CCR5 for the treatment of HIV-1/AIDS, as well as for the potential treatment of inflammatory diseases. In particular, we will focus on the specific medicinal chemistry problems that were faced during the discovery of the molecules. We will also describe limited data from clinical development phases focusing on specific issues that arose during the clinical trials. Finally, we will touch on the mechanism of action of CCR5 antagonists.
Bioorganic & Medicinal Chemistry Letters | 2014
Javier de Vicente; Remy Lemoine; Mark Bartlett; Johannes C. Hermann; Mohammad Hekmat-Nejad; Robert Henningsen; Sue Jin; Andreas Kuglstatter; Hongju Li; Allen John Lovey; John Menke; Linghao Niu; Vaishali Patel; Ann C. Petersen; Lina Setti; Ada Shao; Parcharee Tivitmahaisoon; Minh Diem Vu; Michael Soth
The discovery of a novel series of pyrrolopyrazines as JAK inhibitors with comparable enzyme and cellular activity to tofacitinib is described. The series was identified using a scaffold hopping approach aided by structure based drug design using principles of intramolecular hydrogen bonding for conformational restriction and targeting specific pockets for modulating kinase activity.
Bioorganic & Medicinal Chemistry Letters | 2010
Remy Lemoine; Ann C. Petersen; Lina Setti; Thomas Baldinger; Jutta Wanner; Andreas Jekle; Gabrielle Heilek; André deRosier; Changhua Ji; David Mark Rotstein
The bicyclic 5-amino-3-azabicyclo[3.3.0]octanes were shown to be effective replacements for the 3-amino-8-azabicyclo[3.2.1]octane found in the CCR5 antagonist maraviroc.
Bioorganic & Medicinal Chemistry Letters | 2010
David Mark Rotstein; Chris Richard Melville; Fernando Padilla; Dick Cournoyer; Eun Kyung Lee; Remy Lemoine; Ann C. Petersen; Lina Setti; Jutta Wanner; Lijing Chen; Lubov Filonova; David G. Loughhead; Jason Manka; Xiao-Fa Lin; Shelley K. Gleason; Surya Sankuratri; Changhua Ji; André deRosier; Marianna Dioszegi; Gabrielle Heilek; Andreas Jekle; Pamela Berry; Cheng-I. Mau; Paul Weller
Starting with a high-throughput screening lead, a novel series of CCR5 antagonists was developed utilizing an information-based approach. Improvement of pharmacokinetic properties for the series was pursued by SAR exploration of the lead template. The synthesis, SAR and biological profiles of the series are described.
Bioorganic & Medicinal Chemistry Letters | 2010
Remy Lemoine; Ann C. Petersen; Lina Setti; Lijing Chen; Jutta Wanner; Andreas Jekle; Gabrielle Heilek; André deRosier; Changhua Ji; David Mark Rotstein
The bicyclic 5-amino-3-azabicyclo[3.3.0]octanes were shown to be effective replacements for the conformationally restricted 4-aminopiperidine ring found in several series of CCR5 antagonists.
Bioorganic & Medicinal Chemistry Letters | 2010
Jutta Wanner; Lijing Chen; Remy Lemoine; Rama K. Kondru; Andreas Jekle; Gabrielle Heilek; André deRosier; Changhua Ji; Pamela Berry; David Mark Rotstein
Replacement of a secondary amide with a piperidine or azetidine moiety in a series of CCR5 antagonists led to the discovery of compounds with increased intrinsic permeability. This effort led to the identification of a potent CCR5 antagonist which exhibited an improved in vivo pharmacokinetic profile.
Bioorganic & Medicinal Chemistry Letters | 2010
Remy Lemoine; Ann C. Petersen; Lina Setti; Andreas Jekle; Gabrielle Heilek; André deRosier; Changhua Ji; Pamela Berry; David Mark Rotstein
The introduction of N-substituted pyrazoles in a new series of CCR5 antagonists was shown to substantially increase antiviral activity.