R. Gosmini

发表

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.

Christophe Simon, P. Bamborough, R. Prinjha, 2014, Journal of medicinal chemistry.

Discovery and characterization of small molecule inhibitors of the BET family bromodomains.

P. Bamborough, R. Prinjha, R. Grimley, 2011, Journal of medicinal chemistry.

Discovery of 9-cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.

L. Nelles, G. Milligan, S. Dupont, 2020, Journal of medicinal chemistry.

Pharmacological characterization of GLPG1972/S201086, a potent and selective small molecule inhibitor of ADAMTS5.

Margaret M. Smith, C. Little, F. De Ceuninck, 2021, Osteoarthritis and cartilage.

α-t-butyl- and α-i-propyl-ortho-hydroxybenzylamines: Racemic synthesis/resolution and asymmetric synthesis

Ernst Peter Kundig, D. Fernández, G. Bernardinelli, 2000 .

From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.

E. Nicodème, J. Kirilovsky, L. Trottet, 2012, Bioorganic & medicinal chemistry letters.

Regio and enantioselective synthesis of 4-carbomethoxymethyl-1,4 dihydropyridines

A. Alexakis, R. Gosmini, P. Mangeney, 1994 .

Enantioselective synthesis of indoloquinolizidines

A. Alexakis, R. Gosmini, P. Mangeney, 1991 .

Chiral aminal templates 5. Preparation of chiral 3-carboxaldehydes-1,4-dihydropyridines

A. Alexakis, J. Normant, R. Gosmini, 1991 .

Preparation and Utilization of Chiral Dihydropyridines. Synthesis of Chiral Indoloquinolizines and Benzoquinolizines

A. Alexakis, R. Gosmini, P. Mangeney, 1994 .

Diastereoselective addition of organocuprates on 1,4-dihydropyridine-3-carboxaldehydes. Synthesis of chiral 1,4-dihydropyridyl-3-alcohols and pyridyl-3-alcohols

R. Gosmini, P. Mangeney, Sabine Raussou, 1993 .

BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

G. Ganji, R. Prinjha, C. Chung, 2013, PloS one.

Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.

P. Bamborough, R. Prinjha, C. Chung, 2013, Journal of medicinal chemistry.

Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84

B. Hudson, G. Milligan, I. Tikhonova, 2017, Scientific Reports.

Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.

N. Triballeau, E. M. van der Aar, T. Christophe, 2021, Journal of medicinal chemistry.

GLPG1972: a potent, selective, orally available adamts-5 inhibitor for the treatment of OA

C. Little, T. Christophe, P. Mollat, 2017 .

Syddansk Universitet Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR 84

B. Hudson, G. Milligan, I. Tikhonova, 2017 .