Publications and Patents

PUBLICATIONS

INDUSTRY

2003-2007

· Synthesis of cis-fused indolocarbazole pyran derivatives as multi-kinase inhibitors.

Perron-Sierra, F.M.; Golsteyn, R.M.; Kucharczyk, N.; Boucley, C.; Théret, I.; Hickman, J.A.; Casara, P. Abstract of papers, American Chemical Society, 234^th National Meeting, Division of Medicinal Chemistry, Boston, MA, August 19^th-21^st 2007, poster 364

· Bis-imide granulatimide analogues as potent Checkpoint 1 kinase inhibitors.

Hénon, H.; Messaoudi, S ; Anizon F.; Aboab, B.; Kucharczyk, N.; Léonce, S ; Golsteyn, R.M.; Pfeiffer, B.; Prudhomme, M. Eur. J. Pharmacol. 2006, 554, 106-112

· Expedited synthesis of substituted dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraones structurally related to Granulatimide.

Hénon, H.; Anizon, F.; Kucharczyk, N.; Loynel, A.; Casara, P.; Pfeiffer, B.; Prudhomme, M. Synthesis 2006, 4, 711-715

1997-2003

· Design and synthesis of a general GPCR targeted small compound library.

Casara, P.; Loynel, A.; Kucharczyk, N.; Durand, D.; Henlin, J.M. Abstracts of papers, Gordon Research Conference “Combinatorial Chemistry”, Oxford, UK, August 20^th-25^th, 2006

· Quinazolinedione inhibitors of S-farnesyltransferase: hit optimisation by parallel solid phase synthesis.

Kucharczyk, N.; Tizot, A.; Merer, G.; Dhainaut, A.; Tucker, G.C.; Fauchère, J.L.; Goldstein, S. Abstracts of papers XIXth International Symposium on Medicinal Chemistry, Istanbul, Turkey, August 29^th-September 2^nd, 2006

· Quinazolinedione inhibitors of S-farnesyltransferase: hit optimisation by parallel solid phase synthesis.

Kucharczyk, N.; Tizot, A.; Merer, G.; Dhainaut, A.; Tucker, G.C.; Fauchère, J.L.; Goldstein, S. Abstracts of papers 4ème Colloque Franco-Roumain de Chimie Appliquée. Clermont-Ferrand, France, June 28^th – July 2^nd, 2006

· Jean-Luc Fauchère (1941-2003).

Boutin, J.A.; Henlin, J.M.; Goldstein, S.; Kucharczyk, N.; Ortuno, J.C. J. Peptide Res. 2003, 62 (4), 185

· Solid-phase synthesis of a-substituted 3-bisarylthio N-hydroxy propionamides as specific MMP inhibitors.

Chollet, A.M.; Le Diguarher, T.; Kucharczyk, N.; Loynel, A.; Bertrand, M.; Tucker, G.C.; Guilbaud, N.; Burbridge, M.; Pastoureau, P.; Fradin, A.; Sabatini, M.; Fauchère, J.L.; Casara, P. Bioorg. Med. Chem. 2002, 10 (3), 531-544

· From peptide libraries to optimized non-peptide inhibitors of S-farnesyltransferase.

Henlin, J.M.; Boutin, J.A.; Kucharczyk, N.; Desmet-Beaufort, C.; Loynel, A.; Bertrand, M.; Fouquier d’Hérouel, M.V.; Ginot, Y.M.; Genton, A.; Tucker, G.C.; Atassi, G.; Fauchère, J.L. Peptides 2000 Proceedings of the European Peptide Symposium, 26^th, Montpellier, France, September 10^th-15^th, 2000, 957-958

· From peptide libraries to optimized non-peptide inhibitors of S-farnesyltransferase.

Henlin, J.M.; Boutin, J.A.; Kucharczyk, N.; Desmet-Beaufort, C.; Loynel, A.; Bertrand, M.; Genton, A.; Tucker, G.C.; Atassi, G.; Fauchère, J.L. J. Peptide Res. 2001, 57 (2), 85-96

· Substrate specificity and inhibition studies of human serotonin N-acetyltransferase.

Ferry, G.; Loynel, A.; Kucharczyk, N.; Bertin, S.; Rodriguez, M.; Delagrange, P.; Galizzi, J.P.; Jacoby, E.; Volland, J.P.; Lesieur, D.; Renard, P.; Canet, E.; Fauchère, J.L.; Boutin, J.A. J. Biol. Chem. 2000, 275 (12), 8794-8805

· Combinatorial chemistry for the generation of molecular diversity and the discovery of bioactive leads.

Fauchère, J.L.; Boutin, J.A.; Henlin, J.M.; Kucharczyk, N.; Ortuno, J.C. Chemometrics and Intelligent Laboratory Systems 1998, 43 (1,2), 43-68

1989-1997

· A structural rationale for the design of water soluble peptide-derived neurokinin-1 antagonists.

Jacoby, E.; Boudon, A.; Kucharczyk, N.; Michel, A.; Fauchère, J.L. J. of Receptor and Signal Transduction Res. 1997, 17 (6), 855-873

· The dipeptide neurokinin-1 receptor antagonist S 19752 is a potent and long-acting inhibitor of bronchoconstriction when administered by aerosol to the guinea pig in vivo.

Fauchère, J.L.; Kucharczyk, N.; Jacoby, E.; Longchampt, M.; Robineau, P.; Dacquet, C.; Regoli, D.; Canet, E. Bioorg. Med. Chem. Lett. 1997, 7 (2), 203-208

· Design of water soluble peptide-derived neurokinin NK1 antagonists without impairing binding affinity and pharmacological potency.

Jacoby, E.; Boudon, A.; Kucharczyk, N.; Fauchère, J.L.; Michel, A. Short Communication for the Journal of Computer-Aided Molecular Design 1996

· Solubilization of peptide-derived NK1 antagonists without impairing binding affinity and pharmacological potency: molecular modelling of the pharmacophore and the ligand-receptor interactions.

Jacoby, E.; Boudon, A.; Kucharczyk, N.; Michel, A.; Fauchère, J.L. Abstracts of papers, G-protein-Coupled receptors : Structure and Function, Beerse, Belgium, October 20-22, 1996

· Solubilization of peptide-derived neurokinin NK-1 antagonists without impairing binding affinity and pharmacological potency.

Jacoby E., Boudon A., Kucharczyk N., Michel A., Fauchère J.L. (1996) Abstract, 11^th European Symposium on Quantitative Structure-Activity Relationships : Computer-Assisted Lead Finding and Otimization, Lausanne, Switzerland, September 1-6

· Synthesis and Conformational Analysis by ¹H NMR and Restrained Molecular Dynamics Simulations of the Cyclic Decapeptide [Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly].

Buono, R.A.; Kucharczyk, N.; Neuenschwander, M.; Kemmink, J.; Hwang, L.Y.; Fauchère, J.L.; Scheek, R.M.; Venanzi, C.A. J. Comp. Aided Molecular Design 1996, 10 (3), 213-232

· A water-soluble, stable dipeptide NK1-selective neurokinin receptor antagonist with potent in vivo pharmacological effects: S18523.

Bonnet, J. ; Kucharczyk, N. ; Robineau, P. ; Lonchampt, M. ; Dacquet, C. ; Regoli, D. ; Fauchère, J.L. ; Canet, E. Eur. J. Pharmacol. 1996, 310 (1),37-46

· Effects of parathyroid hormone and agonists of the adenylyl cyclase and protein kinase C pathways on bone cell proliferation.

Sabatini, M. ; Lesur, C. ; Pacherie, M. ; Pastoureau, P. ; Kucharczyk, N. ; Fauchère, J.L. ; Bonnet, J. Bone 1996, 18 (1), 59-65

· In vitro and in vivo pharmacology of S 16474, a novel dual tachykinin NK1 and NK2 receptor antagonist.

Robineau, P.; Lonchampt, M.; Kucharczyk, N.; Krause, J.E.; Regoli, D.; Fauchère, J.L.; Prost, J.F.; Canet, E. Eur. J. Pharmacol. 1995, 294, 677-684

· Tachykinin antagonists in development.

Kucharczyk, N. Exp. Opin. Invest. Drugs 1995, 4 (4), 299-311

· A new somatostatin analog with optimized ring size inhibits neointima formation induced by balloon injury in rats without altering growth hormone release.

Thurieau, C.; Janiak, P.; Krantic, S.; Guyard, C.; Pillon, A.; Kucharczyk, N.; Vilaine, J.P.; Fauchère, J.L. Eur. J. Med Chem. 1995, 30 (2),115-122

· A new somatostatin analog inhibits neointima formation induced by balloon injury in rats without altering growth hormone release.

Thurieau, C.; Janiak, P.; Krantic, S.; Guyard, C.; Carsalade, H.; Kucharczyk, N.; Pilon, A.; Vilaine, J.P.; Fauchère, J.L. Peptides 1994 Proceedings of the European Peptide Symposium, 23^rd, Braga, Portugal, Sept. 4-10, 1994, 640-641

· Estimation de la stabilité à la protéolyse et de l’absorption orale comme outils dans la conception de peptides-médicaments.

Kucharczyk, N. ; Paladino, J. ; Thurieau, C. ; Fauchère, J.L. Abstracts of papers, 9ème Réunion Peptides et Protéines. Aussois. France, Juanuary 8-13, 1995. Oral presentation.

· Estimation of blood levels of endothelin and neurokinin receptor antagonists at the rat portal and jugular veins after oral administration as a tool in peptide drug design.

Paladino, J.; Kucharczyk, N.; Morris, A.; Thibault-Naze, M.; Mahieu, J.P.; Serkiz, B.; Volland, J.P.; Autissier, C.; Fauchère, J.L. Drug Design and Discovery 1994, 12 (2),121-128

· Improved pharmacological properties of a tetrapeptide tachykinin antagonist when incorporated into phosphatidylcholine liposomes.

Rault, I.; Bonnet, J.; Kucharczyk, N.; Cuiné, A.; De Jong, H.; Fauchère, J.L. J. Controlled Release 1994, 29 (3),397

· Synthesis and biological activity of R820, a NK-3A-selective dipeptide neurokinin receptor antagonist.

Regoli, D.; Kucharczyk, N.; Brebbia, A.M.; Jukic, D.; Fauchère, J.L. Abstracts of papers, Satellite symposia of the XII ^th IUPHAR Congress. « Peptides and their antagonists in tissue injury », Montréal, July 31^st- August 3^rd, 1994

· Synthesis and in vitro activities of new tryptophan-modified and thiomethylene-containing pseudopeptide antagonists of the neurokinins.

Paladino, J.; Thurieau, C.; Morris, A.; Kucharczyk, N.; Rouissi, N.; Regoli, D.; Fauchère, J.L. Int. J. Peptide Protein Res. 1993, 42 (3), 284-293

· Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs.

Kucharczyk, N.; Thurieau, C.; Paladino, J.; Morris, A.D.; Bonnet, J.; Canet, E.; Krause, J.E.; Regoli, D.; Couture, R.; Fauchère, J.L. J. Med. Chem. 1993, 36 (11),1654-1661

ACADEMIA

· Thèse de doctorat de l’université Paris VI. N. Kucharczyk, 19 juin 1989 :

Synthèse de dérivés de l’acide N³-fumaroyl diaminopropionique-2,3, inhibiteurs de la glucosamine-6-phosphate synthase. Détermination du mécanisme d’inactivation à l’aide de réactions modèles. Etude du pouvoir antifongique de dérivés peptidiques de ces inhibiteurs.

· Synthesis and evaluation of inhibitors for Escherichia coli glucosamine-6-phosphate synthase.

Auvin, S.; Cochet, O.; Kucharczyk, N.; Le Goffic, F.; Badet, B. Bioorg. Chem. 1991, 19 (2),143-151

· Glucosamine-6-phosphate synthase from Escherichia coli: determination of the mechanism of inactivation by N³-fumaroyl-L-2,3-diaminopropionic derivatives.

Kucharczyk, N.; Denisot, M.A.; Le Goffic, F.; Badet, B. Biochemistry 1990, 29 (15), 3668-3676

· Inhibiteurs de la glucosamine phosphate synthase.

Kucharczyk, N. ; Le Goffic, F. ; Badet, B. Abstracts of papers, Journées de Chimie Organique, Palaiseau, France, September 19^th-21^st, 1989

· Quantitative synthesis of L or D-N²-(tertbutoxycarbonyl)-2,3-diaminopropanoic acid from L- or D-serine b-lactone.

Kucharczyk, N. ; Badet, B.; Le Goffic, F. Synthetic Comm. 1989, 19 (9-10),1603-1609

· Synthesis of N³-fumaroyl-L-2,3-diaminopropionic acid derivatives. Study of their behavior towards the pure bacterial glucosamine-6-phosphate synthetase.

Kucharczyk, N. ; Vermoote, P. ; Le Goffic, F. ; Badet, B. Abstracts of papers, Second forum on peptides. Colloque INSERM/John Libbey Eurotext Ltd, Nancy, France, 1989, 174, 325-331. Oral presentation

· Glucosamine-6-phosphate synthetase from Escherichia coli: kinetic mechanism and inhibition by N³-fumaroyl-L-2,3-diaminopropionic derivatives.

Badet, B. ; Vermoote, P. ; Le Goffic, F. Biochemistry 1988, 27, 2282-2287

· Discotic liquid crystals of transition metal complexes. X. Phtalocyanine derivatives substituted with n-alkyloxyphenyl side chains.

Ohta, K.; Watanabe, T.; Tanaka, S.; Fujimoto, T.; Yamamoto, I.; Bassoul, P.; Kucharczyk, N.; Simon, J. Liquid Crystals 991, 10 (3),357-368

PATENTS

· Nouveaux composés dérivés de la quinazoline, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.

Goldstein, S. ; Dhainaut, A. ; Tizot, A. ; Fauchère, J.L. ; Kucharczyk, N. ; Hickman, J. ; Pierré, A. ; Tucker, G.C. ; Kraus-Berthier, L.

2003 : FR 2837201, EP 1346992 A1, US 20030199530 A1

· Pseudopeptides dérivés de neurokinines, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. (S 19752)

Fauchère, J.L. ; Kucharczyk-Gentric, N. ; Canet, E. ; Lonchampt, M.

1997: EP 0790254, US 5708016

· Nouveaux pseudopeptides dérivés de neurokinines, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. (S 18523)

Fauchère, J.L. ; Kucharczyk-Gentric, N. ; Paladino, J. ; Bonnet, J. ; Canet E. ; Birrell, G.

1995: FR 2719312, EP 0684257

· Nouveaux dérivés pseudopeptidiques à activité antagoniste de la bradykinine, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. (S 16118)

Fauchère, J.L. ; Thurieau, C. ; Paladino, J. ; Kucharczyk, N. ; Canet, E.

1993: FR 2692581, EP 0578521

· Nouveaux peptides et pseudopeptides dérivés de tachykinines, leur procédé de fabrication et les compositions pharmaceutiques qui les contiennent. (S 16474)

Fauchère, J.L. ; Kucharczyk, N. ; Morris, A.D. ; Paladino, J. ; Bonnet, J. ; Thurieau, C.

1992: FR 2677361, EP 0517589

· Peptides et pseudopeptides dérivés de tachykinines, leur procédé de fabrication et les compositions pharmaceutiques qui les contiennent. (analogues FR113680 : S 15313 et analogues FK888)

Fauchère, J.L. ; Kucharczyk, N. ; Morris, A.D. ; Paladino, J. ; Bonnet, J. ; Thurieau, C.

1991: FR 2677361, EP 0676411