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Dr. Jacques Y. RobergeDr. Jacques Y. Roberge
Technical Specialist
McNeely, Hare & War LLP
12 Roszel Road, Suite C104
Princeton, NJ 08540
Phone: +01 (609) 865-9019
Fax: +01 202 478-1813

E-mail: jacques@miplaw.com

Dr. Roberge is an innovative pharmaceutical researcher and entrepreneur with extensive experience in drug discovery and development. He has international experience managing active pharmaceutical ingredient development to supply a clinical testing program. He is an original scientist with excellent problem-solving skills and demonstrated management experience. He is familiar with producing drugs following Quality by Design (QbD), current good manufacturing practice (cGMP) and US FDA regulations. Dr. Roberge’s work has been published in many internationally recognized journals and books and has led to completing more than fourteen patents and patent applications.

At McNeely, Hare & War, LLP, Dr. Roberge provides technical assistance and support in chemical, pharmaceutical, and nutraceutical litigations; inter partes review; and chemical and pharmaceutical opinions.

In 2014, Dr. Roberge co-founded MycoNovo Inc., an early phase innovative drug discovery company focussing on the development of small-molecule antifungal and anti-infective medications. He is currently optimizing the lead compounds and confirming the mode of action of the drug.

In 2014, Dr. Roberge also joined Rowan University in Glassboro, New Jersey as an adjunct professor teaching organic chemistry and conducting research with students.

In 2012, Dr. Roberge formed his own consulting company where he continued working with Theracos and Egret on EGT1442 development. He contributed to the chemical route selection as well as evaluating and selecting chemical manufacturing organization (CRO’s) to produce the active pharmaceutical ingredient (API) and the intermediates. He worked on the technology transfer and monitored early production on sites. EGT1442 is currently undergoing Phase 3 clinical trials in many worldwide locations.

Dr. Roberge joined Egret Pharmaceuticals Shanghai in 2008 where he rose to the position of CEO which he held until 2012. Dr. Roberge previously held the position of VP of Chemistry at Egret and then Interim CEO. At Egret Dr. Roberge led the team that developed EGT1442 trough preclinical and clinical development. He is a co-inventor of the chemical synthesis process. He is familiar with the drug development process, quality-by-design (QbD) and US FDA regulations. EGT1442 is currently being tested in human in many countries.

Prior to moving to Shanghai, Dr. Roberge spent 13 years at Bristol-Myers Squibb Pharmaceutical Research Institute in Hopewell and Princeton, New Jersey. His work was principally in the area of early phase medicinal chemistry, initially in the Combinatorial Drug Discovery Group and then in Early Discovery Chemistry.  During his tenure, his work received three PRI Star Awards and a PRI Success Award from Bristol-Myers.

Dr. Roberge was educated in Canada where he received a Ph.D. in Chemistry from the University of British Columbia and M.Sc. and B.Sc. degrees from l’Universite de Sherbrooke in Sherbrooke, Quebec. He was a Natural Sciences and Engineering Research Council of Canada Post-Doctoral Fellow at the Memorial Sloan-Kettering Cancer Centre in New York City and at Yale University in New Haven, Connecticut.

He is a member of the American Chemical Society (ACS) and the American Society for the Advancement of Science (AAAS). He is bilingual in English and French and has a basic knowledge of Mandarin Chinese.

Selected Peer-reviewed Publications

  1. Xu G, Lv B, Roberge JY, Xu B, Du J, et al. Design, synthesis, and biological evaluation of deuterated C-aryl glycoside as a potent and long-acting renal sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes. J Med Chem. 2014 Feb 27;57(4):1236-51. PubMed PMID: 24456245.
  2. Chao H, Turdi H, Herpin TF, Roberge JY, Liu Y, et al. Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists. J Med Chem. 2013 Feb 28;56(4):1704-14. PubMed PMID: 23368907.
  3. Xu B, Feng Y, Cheng H, Song Y, Lv B, et al. C-aryl glucosides substituted at the 4′-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4465-70. PubMed PMID: 21737266.
  4. Zhang W, Welihinda A, Mechanic J, Ding H, Zhu L, et al. EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. Pharmacol Res. 2011 Apr;63(4):284-93. PubMed PMID: 21215314.
  5. Roberge JY, Harikrishnan LS, Kamau MG, Ruan Z, Van Kirk K, et al. Design and synthesis of a G-protein-coupled receptor antagonist library of aryloxyalkanolamines using a polymer-supported acyclic acetal linker. J Comb Chem. 2009 Jan-Feb;11(1):72-82. PubMed PMID: 19086798.
  6. Gavai AV, Vaz RJ, Mikkilineni AB, Roberge JY, Liu Y, et al. Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5478-82. PubMed PMID: 16216508.
  7. Chen P, Norris D, Iwanowicz EJ, Spergel SH, Lin J, et al. Discovery and initial Yang W, Wang Y, Roberge JY, Ma Z, Liu Y, et al. Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1225-8. PubMed PMID: 15686947.
  8. Pitts WJ, Vaccaro W, Huynh T, Leftheris K, Roberge JY, et al. Identification of purine inhibitors of phosphodiesterase 7 (PDE7). Bioorg Med Chem Lett. 2004 Jun 7;14(11):2955-8. PubMed PMID: 15125967.
  9. Dong Y, Roberge JY, Wang Z, Wang X, Tamasi J, et al. Characterization of a new class of selective nonsteroidal progesterone receptor agonists. Steroids. 2004 Mar;69(3):201-17. PubMed PMID: 15072922.
  10. SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck). Bioorg Med Chem Lett. 2002 May 20;12(10):1361-4. PubMed PMID: 11992777.

Selected Patents and Patent Applications

  1. Xu, B., Lv, B., Seed, B., Jacques Y. Roberge, Process for the Preparation of Benzylbenzene SGLT2 Inhibitors. USPTO. USA, Theracos Inc. 13/889,980, 2012
  2. Y. Chen, H. Cheng, S. Li, Y. Wu, Y. Feng, B. Lv, B. Xu, B. Seed, M. J. Hadd, Y. Song, J. Du, C. Wang and J. Y. Roberge. US20120329732: Benzylbenzene Derivatives and Methods of Use. USPTO. USA, Theracos Inc. US20120329732A1, 2012
  3. Cai, M.; Liu, Q.; Xu, G.; Lv, B.; Seed, B.; Roberge, J. Preparation of crystalline form of benzylbenzene glycoside as SGLT2 inhibitor. WO2011153712A1, 2011.
  4. Salvati, M. E.; Finlay, H.; Harikrishnan, L. S.; Jiang, J.; Johnson, J. A.; Kamau, M. G.; Lawrence, R. M.; Lloyd, J.; Miller, M. M.; Pi, Z.; Qiao, J. X.; Rampulla, R. A.; Roberge, J. Y.; Wang, T. C.; Wang, Y.; Yang, W. Preparation of heterocyclic and aromatic ureas and amides as CEPT inhibitors. WO2007062308A2, 2007; US7790770B2, 2010.
  5. Song, Y.; Chen, Y.; Cheng, H.; Li, S.; Wu, Y.; Feng, Y.; Lv, B.; Xu, B.; Seed, B.; Hadd, M. J.; Du, J.; Wang, C.; Roberge, J. Y. Preparation of benzylbenzene glycoside derivatives as antidiabetic agents. WO2009026537A1, 2009.
  6. Seed, B.; Lv, B.; Roberge, J. Y.; Chen, Y.; Peng, K.; Dong, J.; Xu, B.; Du, J.; Zhang, L.; Tang, X.; Xu, G.; Feng, Y.; Xu, M. Preparation of deuterated benzyl-benzene glycosides having an inhibitory effect on sodium-dependent glucose co-transporter. WO2010009243A1, 2008.
  7. Herpin, T. F.; Morton, G. C.; Rehfuss, R. P.; Lawrence, R. M.; Poss, M. A.; Roberge, J. Y.; Gungor, T. Preparation of aminobenzazoles and analogs as P2Y1 receptor inhibitors for treating thromboembolic disorders. WO2005070920A1, 2005.
  8. Chao, H. J.; Tuerdi, H.; Herpin, T.; Roberge, J. Y.; Liu, Y.; Lawrence, R. M.; Rehfuss, R. P.; Clark, C. G.; Qiao, J. X.; Gungor, T.; Lam, P. Y. S.; Wang, T. C.; Ruel, R.; L’Heureux, A. L.; Thibeault, C.; Bouthillier, G.; Schnur, D. M. Preparation of phenyl or pyridinyl ureas as antagonists of P2Y1 receptors for the treatment of thromboembolic disorders. WO2005113511A1, 2005.
  9. Dickson, J. K.; Lawrence, R. M.; Roberge, J. Y.; Rotella, D. P.; Yang, W. Preparation of substituted piperidines and pyrrolidines as calcium sensing receptor modulators. WO2004106295A2, 2004.
  10. Gavai, A. V.; Vaz, R. J.; Dickson, J. K., Jr.; Roberge, J. Y.; Wang, W.; Gungor, T.; Corte, J. R.; Rotella, D. P.; Wang, Y.; Wu, Y. Preparation of pyrrolidinylhydroxyethylarylethylamines and related compounds as calcium sensing receptor modulators. WO2004069793A2, 2004.
  11. Salvati, M. E.; Balog, J. A.; Pickering, D. A.; Giese, S.; Fura, A.; Li, W.; Patel, R. N.; Hanson, R. L.; Mitt, T.; Roberge, J.; Corte, J. R.; Spergel, S. H.; Rampulla, R. A.; Misra, R.; Xiao, H.-y. Preparation of fused succinimides as modulators of nuclear hormone receptor function. US20040077605A1, 2004; WO2003062241A1, 2003.
  12. Vaccaro, W.; Roberge, J. Y.; Leftheris, K.; Pitts, W. J.; Barbosa, J. Preparation of purines as inhibitors of phosphodiesterase VII (PDE7) for therapeutic use in treating T-cell mediated diseases. WO2002102314A2, 2002.
  13. J. Barrish, P. Chen, J. Das, E. Iwanowicz, D. Norris, R. Padmanabha, J.Y. Roberge, G. Schieven, Preparation of Imidazoquinoxaline Protein Tyrosine Kinase Inhibitors, PCT Int. Appl. (1999), 315 pp. WO 9909845 A1 19990304; US6235740B1.
  14. Danishefsky, S. J.; Roberge, J.; Beebe, X. Synthesis of asparagine-linked glycopeptides on a polymeric solid support. WO9640198A1, 1996: US5679769A, 1997.