Patents & Publications

• US 11,667,673 - Therapeutically active compounds and their methods of use
• US 11,021,515 - Therapeutically active compounds and their methods of use
• US 10,717,764 - Therapeutically active compounds and their methods of use 
• US 10,689,414 - Therapeutically active compounds and their methods of use 
• US 10,689,375 - Compounds and their methods of use 
• US 10,640,534 - Therapeutically active compositions and their methods of use 
• US 10,414,740 - Glutaminase inhibitors and method of use 
• US 10,087,172 - Compounds and their methods of use 
• US 10,011,574 - Glutaminase inhibitors and method of use 
• US 10,000,479 - Compounds and their methods of use 
• US 9,850,277 - Therapeutically active compositions and their methods of use 
• US 9,474,779 - Therapeutically active compositions and their methods of use 
• US 9,303,002 - Compounds and their methods of use 
• US 9,029,531 - Compounds and their methods of use 
• US 8,575,360 - Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amides 
• US 8,552,205 - Derivatives of 6,7-dihydro-5H-imidazo[1,2-alpha]imidazole-3-carboxylic acid amides 
• US 7,601,714 - Pyrimidine derivatives useful as inhibitors of PKC-theta 
• US 7,589,115 - Derivatives of [6,7-dihydro-5H-imidazo[1,2-.alpha.]imidazole-3-sulfonylamino]-propionamide 
• US 7,572,921 - Substituted benzylimidazoles useful for the treatment of inflammatory diseases 
• US 7,550,494 - Small molecules useful in the treatment of inflammatory disease 
• US 7,517,897 - Derivatives of 6,7-dihydro-5h -imidazo[1,2-a] imidazole-3-sulfonic acid 
• US 7,468,382 - Pyridine derivatives useful as inhibitors of PKC-theta 
• US 7,462,637 - Derivatives of [6,7-dihydro-5H-imidazo[1,2--a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide 
• US 7,345,074 - Derivatives of [6,7-dihydro-5H-imidazol[1,2-a]imidazole-3-sulfonylamino]-propionamide 
• US 7,304,067 - Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide 
• US 6,852,748 - Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide 
• US 6,846,643 - Methods and molecules useful for identifying molecules that bind LFA-1 and for determining receptor occupancy 
• US 6,844,360 - Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide 
• US 6,689,804 - Small molecules useful in the treatment of inflammatory disease 
• US 6,492,408 - Small molecules useful in the treatment of inflammatory disease 

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• Preclinical Drug Metabolism, Pharmacokinetic, and Pharmacodynamic Profiles of Ivosidenib, an Inhibitor of Mutant Isocitrate Dehydrogenase 1 for Treatment of Isocitrate Dehydrogenase 1-Mutant Malignancies. Chen Y, Nagaraja NV, Fan B, Utley L, Lemieux RM, Popovici-Muller J, Dang L, Kim H, Yan L, Su SM, Biller SA, Yand H. Drug Metab Dispos October 2021, 49 (10) 870-881
• Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers. Popovici-Muller J, Lemieux RM, Artin E, Saunders JO, Salituro FG, Travins J, Cianchetta G, Cai Z, Zhou D, Cui D, Chen P, Straley K, Tobin E, Wang F, David MD, Penard-Lacronique V, Quivoron C, Saada V, de Botton S, Gross S, Dang L, Yang H, Utley L, Chen Y, Kim H, Jin S, Gu Z, Yao G, Luo Z, Lv X, Fang C, Yan L, Olaharski A, Silverman L, Biller S, Su SM, Yen K. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305
• Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists, Joshua C. Horan,  Daniel Kuzmich, Pingrong Liu, Darren DiSalvo, John Lord, Can Mao, Tamara D. Hopkins, Hui Yu, Christian Harcken, Raj Betageri, Melissa Hill-Drzewi, Lori Patenaude, Monica Patel, Kimberly Fletcher, Donna Terenzzio, Brian Linehan, Heather Xia, Mita Patel, Debbie Studwell, Craig Miller, Eugene Hickey, Jeremy I. Levin, Dustin Smith, Raymond A. Kemper, Louise K. Modis, Lynne C. Bannen, Diva S. Chan, Morrison B. Mac, Stephanie Ng, Yong Wang, Wei Xu, René M. Lemieux, Bioorg. & Med. Chem. Letters, 2016, 26 (2), 466–471.
• Optimization Of Glutaminase Inhibitors For The Treatment Of Cancer. R.M. Lemieux, M. Blake, Y. Chen, G. Cianchetta, K. Couto, V. DeJesus, B. DeLaBarre, S. Gross, E. Mandley, F. Salituro, M. Steadman, J. Travins, D. Ulanet, T.J. Unger, A. Wang, H-K. Woo, K. Yen, S. Cao, Y. Chen, S. Yan and J. Hurov, 2015 GRC Medicinal Chemistry, New London, NH; August 2-7, 2015
• From Chemistry to the Clinic: Pathways for Drug Discovery and Development, Part 4: Design of Small Molecules Targeting Tumor Metabolism (Educational Session). Optimization of Glutaminase Inhibitors for the Treatment of Cancer, Rene M. Lemieux. AACR Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA
• Piperazinyl-oxadiazoles as Selective Sphingosine-1-Phosphate Receptor Agonists. Horan JC, Sanyal S, Choi Y, Hill-Drzewi M, Patnaude L, Anderson S, Fogal S, Mao C, Cook BN, Gueneva-Boucheva K, Fisher MB, Hickey E, Pack E, Bannen LC, Chan DS, Mac MB, Ng SM, Wang Y, Xu W, Modis LK, Lemieux RM. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4807-11.
• IDH1 Mutant Inhibitor Induces Cellular Differentiation and Offers a Combination Benefit with Ara-C in a Primary Human Idh1 Mutant AML Xenograft Model. Kate Ellwood-Yen,  Yue Chen,  Fang Wang,  Rene Lemieux,  Janeta Popovici-Muller,  Hua Yang,  Kimberly Straley,  Sung Choe,  Marion Dorsch,  Sam Agresta, David Schenkein,  Scott Biller, and  Michael Su; AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA
• Optimization and Characterization of Mutant IDH Inhibitors for the Treatment of Cancer. René M. Lemieux, 2013 GRC High Throughput Chemistry & Chemical Biology, New London, NH; June 2-7, 2013
• Characterization of Mutant IDH Inhibitors for the Treatment of Cancer. Lemieux R.M., Artin E., DeLaBarre B., Driggers E., Fantin V., Gross S., Hansen E., Kunii K., Popovici-Muller J., Salituro F., Saunders J., Schalm S., Straley K., Su M., Travins J., Wang F., Yang H., Yen K. 96th Canadian Chemistry Conference and Exhibition, Québec City, QC, May 26-30, 2013
• Discovery and practical asymmetric synthesis of small molecule, nonpeptide inhibitor of LFA-1 (Part 1 of 2 - paired with C. Senanayake).  René M. Lemieux; 2010 International Chemical Congress of Pacific Basin Societies, The Science and Strategy of Process Chemistry: From Molecules to Pharmaceutical Drugs.  Honolulu, HI; December 15-20, 2010
• Keynote Speaker: Allosteric Antagonism of Protein-Protein Interaction: Lessons from the Lymphocyte Function Associated Antigen-1 (LFA-1) Experience.  René M. Lemieux; Protein-Protein Interaction Workshop, NIH Molecular Libraries Program. Bethesda, MD; October 28-29, 2010.
• Small Molecule PKC-theta Inhibitors with Oral In Vivo Activity René M. Lemieux, A.J. Barbosa, S.R. Brunette, M.L. Brown, J. Cui, S. Desai, J.-M. Kim, M.L. Lawlor, N. Li, B. McKibben, D. White, oral presentation at the 8th World Congress on Inflammation, June 16-20 2007, Copenhagen, Denmark.
• LFA-1 as a Key Regulator of Immune Function:  Approaches Toward the Development of LFA-1-Based Therapeutics. Giblin, P.A. and Lemieux, R.M.  Curr. Pharm. Design, 2006, 12, 2771-2795 (invited review).
• An orally active, primate selective antagonist of LFA-1 inhibits delayed-type hypersensitivity in a humanized-mouse model. Panzenbeck, M.J.; Jeanfavre, D.D.; Kelly, T.A.; Lemieux, R.; Nabozny, G.; Reilly, P.L.; Desai, S.  Eur. J. Pharm., 2006, 534, 233-240.
• Discovery of Novel LFA-1 Antagonists Lemieux, René M, invited speaker at the 1st AMRI Frontiers in Drug Discovery Symposium, October 2004, Albany, NY.
• Opening of Tartrate Acetals Using Dialkylboron Bromide: Evidence for Stereoselective Downstream from Ring Fission. Guindon, Y.; Ogilvie, W.W.; Bordeleau, J.; Cui, W.L.; Durkin, K.; Gorys, V.; Juteau, H.; Lemieux, R.; Liotta, D.; Simoneau, B.; and Yoakim, C. J. Am. Chem. Soc., 2003, 125, 428-426.
• Novel Antagonists of LFA-1 Function R. Lemieux, P. Giblin, S. Desai, J, Emeigh, S. Fogal, D. Goldberg, D. Jeanfavre, S. Kerr, T. Kishimoto, E. Mainolfi, G. Nabozny, M. Panzenbeck, P. Reilly, R. Rothlein, D. Tweedie, J. Woska, J.-P. Wu, T. Kelly, poster presented at the 6th World Congress on Inflammation, August 2003, Vancouver, Canada.
• An Asymetric Route to Novel Chiral Cyclohexenones with Spiro-Connected Cyclopentenes.  Further Utility of Chiral Bicyclic Thiolactams and the [3,3] Thio-Claisen Products. Lemieux, R.M.; Devine, P.N.; Mechelke, M.F. and Meyers, A.I. J. Org. Chem., 1999, 64, 3585-3591.
• Novel (Trimethylgermyl)copper(I) Reagents: Preparation and Addition to -Unsaturated Ketones and -Alkynic esters. Piers, E. and Lemieux, R.M. Organometallics, 1998, 17, 4213-4217.
• Asymmetric Synthesis of (-)-Trichodiene.  Generation of Vicinal Stereogenic Quaternary Centers via the Thio-Claisen Rearrangement. Lemieux, R.M. and Meyers, A.I. J. Am. Chem. Soc., 1998, 120, 5453-5457.
• Reaction of (Trimethylgermyl)copper(I)–Dimethyl Sulfide with Acyl Chlorides: Efficient Syntheses of Functionalized Acyltrimethylgermanes Piers, E. and Lemieux, R. Organometallics, 1995, 14, 5011-2.
• Platinum-catalysed Addition of Trimethylgermane to 1-Trimethylsilylalk-1-ynes: a Convenient Synthesis of Functionalised 2-Trimethylgermylalk-1-enes Piers, E. and Lemieux, R. J. Chem. Soc., Perkin Trans. 1, 1995, 3-5.
• Synthesis of 2-(Trimethylgermyl)-1-Alkenes and Related Compounds.  New Bifunctional Reagents R. Lemieux and E Piers; seminar presented at the 77th Canadian Society for Chemistry Conference and Exhibition, Winnipeg, Canada, June 1994.
• Stereoselective Opening of Acetals Derived from Dimethyl Tartrate Guindon, Y.; Simoneau, B.; Yoakim, C.; Gorys, V.; Lemieux, R. and Ogilvie, W. Tetrahedron Lett., 1991, 32, 5453-6.
• Stereoselective Radical-mediated Reduction and Alkylation of -Halo Esters Guindon, Y.; Lavallée, J.-F.; Boisvert, L.; Chabot, C.; Delorme, D.; Yoakim, C.; Hall, D.; Lemieux, R. and Simoneau, B. Tetrahedron Lett., 1991, 32, 27-30.
• Stereoselective Reduction of Acyclic -Bromo Esters Guindon, Y.; Yoakim, C.; Lemieux, R.; Boisvert, L.; Delorme, D. and Lavallée, J.-F. Tetrahedron Lett., 1990, 31, 2845-8.
• The Electrocatalytic Hydrogenation of Fused Polycyclic Aromatic Compounds at Raney Nickel Electrodes: the Influence of Catalyst Activation and Electrolysis Conditions Robin, D.; Comtois, M.; Martel, A.; Lemieux, R.; Cheong, A.K.; Belot, G. and Lessard, J. Can. J. Chem., 1990, 68, 1218-27.
• Dialkyl and Diaryl Boron Halides: Reductive Opening of Benzylidene Acetals Guindon, Y.; Girard, Y.; Berthiaume, S.; Gorys, V.; Lemieux, R. and Yoakim, C. Can. J. Chem., 1990, 68, 897-902.