ANN E WEBER, PHD
`
`PAGE 1
`
`ANN E WEBER, PHD
`103 Chestnut Street, Apt. 217, Cranford, NJ 07016 | (732) 771-4704 | weberan8@gmail.com
`
`PROFESSIONAL SUMMARY
`Accomplished independent consultant and former pharmaceutical executive with a passion for discovering innovative
`therapeutics to address unmet medical needs. Over 28 years of industrial experience focused on small molecule and
`peptide drug discovery across therapeutic areas leading to over 40 development candidates, including JANUVIA®
`(sitagliptin), a treatment for patients with Type 2 diabetes (T2DM), and MARIZEV® (omarigliptin), a once-weekly
`treatment for T2DM recently approved in Japan; vibegron for the treatment of overactive bladder is in late stage clinical
`trials. Highly collaborative scientific leader in drug discovery and early development, recognized for building strong
`teams, setting strategy and managing change. Noted for strong interpersonal skills, talent development, and
`commitment to advancing women in chemistry.
`
`EXPERIENCE
`ANN WEBER PHARMA CONSULTING
`December 2015 – present
`Independent consultant to biotech and pharma for all aspects of drug discovery including target and lead
`identification, lead optimization, and development candidate nomination
`
`
`MERCK & CO
`August 1987 – November 2015
`
`Vice President – Lead Optimization Chemistry, Kenilworth, NJ and Boston, MA
`
`November 2013 – November 2015
`Responsible for delivering the lead optimization pipeline to the clinic, particularly in the areas of cardiometabolic
`diseases, infectious diseases, neurological disorders, oncology and asthma; talent recruitment, management and
`development for department of ~100 lead optimization chemists in Kenilworth and Boston, working in small-
`molecule and peptide modalities; Cubist integration team co-lead for Discovery Research
`
`Vice President – Kenilworth Discovery Chemistry Site Head, Kenilworth, NJ
`
`September 2011 – October 2013
`Discovery of innovative therapeutic agents to treat patients with cardiovascular disease, diabetes, infectious
`diseases, and neurological disorders; leadership of chemists at Kenilworth site working in Lead Identification, Lead
`Optimization, and Automated Synthesis & Purification; Joint Steering Committee for Theravance collaboration;
`leadership and executive sponsorship of strategic initiatives; Six Sigma Executive Black Belt
`
`Vice President – Rahway Discovery Chemistry Site Head, Rahway, NJ
`February 2010 – August 2011
`Primary focus on the development of new therapies for cardiovascular disease and metabolic disorders; provided
`leadership for department of ~200 medicinal chemists during re-organization activities following Schering Plough
`merger; established Rahway Women in Chemistry Lunch, providing networking and leadership opportunities for
`emerging women leaders across the internal chemistry organization, sponsored the first Merck Women in
`Chemistry Symposium
`
`Executive Director, Medicinal Chemistry, Rahway, NJ
`
`July 2005 – January 2010
`Scientific oversight for teams that identified clinical candidates in the fields of obesity, diabetes, urinary
`incontinence, and pain; discovery of omarigliptin (approved in Japan Sept 2015), a once weekly agent for diabetes,
`and vibegron (licensed to Kyorin at Phase III) for urinary incontinence; Diabetes & Obesity Research Licensing
`Committee; Joint Research Committees for Metabasis and Neuromed collaborations; leadership of Early
`
`AstraZeneca Exhibit 2210
`Mylan v. AstraZeneca
`IPR2015-01340
`
`Page 1 of 17
`
`

`
`ANN E WEBER, PHD
`
`PAGE 2
`
`Development Teams in diabetes and pain; basic research representative on Urinary Incontinence Product
`Development Team; chair of the Lead Optimization Work Stream tasked with implementing the new Basic
`Research Global Operating Strategy in the lead optimization space; Merck Women’s Global Constituency Group
`member
`
`Senior Director, Medicinal Chemistry, Rahway, NJ
`
`March 2002 – June 2005
`Leadership of a group of 24 medicinal chemists; identification of clinical candidates in the areas of obesity,
`diabetes, and pain; co-chair of DPP-4 Back-Up Early Development Team; Diabetes & Obesity Research Licensing
`Committee
`
`
`
`
`
`Director, Medicinal Chemistry, Rahway, NJ
`
`November 1997 – February 2002
`Leadership for emerging programs in obesity and transplant therapy; initiation of chemistry effort on the DPP-4
`inhibitor program for diabetes; co-lead of program core team that identified JANUVIA® (sitagliptin), the first
`marketed DPP-4 inhibitor for the treatment of patients with type2 diabetes; basic research representative on DPP-
`4 Early Development Team
`
`Associate Director, Medicinal Chemistry, Rahway, NJ
`
`November 1994 – October 1997
`Chemistry group leader of the β3 adrenergic receptor agonist program, leading to the identification of two
`compounds that entered clinical development; medicinal chemistry representative on the Product Development
`Team
`
`Research Fellow, Medicinal Chemistry, Rahway, NJ
`
`December 1991 – October 1994
`Identification of the first human selective β3 adrenergic receptor agonists for the treatment of obesity
`
`
`
`Senior Research Chemist, Medicinal Chemistry, Rahway, NJ
`
`August 1987 – November 1991
`Design and synthesis of conformationally-restricted renin inhibitors for hypertension; initiation of the β3
`adrenergic receptor agonist program for obesity
`
`
`
`Research Assistant, Harvard University, Cambridge, MA
`
`September 1983 – July 1987
`Oxazolidinethiones, active ester analogs of oxazolidinone chiral auxiliaries in the asymmetric aldol reaction; asymmetric
`synthesis of beta-hydroxy amino acids including the total synthesis of Echinocandin D
`
`
`
`Research Assistant, California Institute of Technology, Pasadena, CA
`September 1982 – August 1987
`Initiated graduate work; assisted in laboratory move to Cambridge, MA
`
`Research Assistant / Summer Intern, Monsanto Company, St. Louis, MO
`June 1982 – August 1982
`Synthesis of novel herbicides for crop protection
`
`
`
`
`
`EDUCATION
`Harvard University
`1987 - Ph.D. in Organic Chemistry
`Thesis Advisor: David A. Evans
`
`
`
`
`
`
`
`Page 2 of 17
`
`

`
`ANN E WEBER, PHD
`
`PAGE 3
`
`University of Notre Dame
`1982 - B.S. in Chemistry, Summa cum Laude
`Research Advisor: Conrad J. Kowlaski
`
`
`
`
`
`
`
`AWARDS
`1981 Chicago Drug and Chemical Association Undergraduate Scholarship
`1981 American Chemical Society Division of Analytical Chemistry Undergraduate Award
`1981 National Science Foundation Summer Undergraduate Research Program Participant
`1982 Atlantic Richfield Academic Excellence Award
`1982 American Institute of Chemists Student Award Certificate
`1982 Phi Beta Kappa
`1982 Valedictorian, University of Notre Dame
`1982 – 1985 National Science Foundation Pre-doctoral Fellowship
`2002 American Chemical Society Women Chemists Committee, Women at the Forefront of Chemistry
`2007 Merck Directors’ Award
`2007 Thomas Alva Edison Patent Award (Research & Development Council of New Jersey)
`2007 Prix Galien USA for JANUVIA® (team member)
`2008 Outstanding Women in Science (New Jersey Association for Biomedical Research)
`2009 Award for Drug Discovery (Society for Medicines Research, London) for JANUVIA® (team member)
`2010 Robert M. Scarborough Award for Excellence in Medicinal Chemistry (Medicinal Chemistry Division
`of the American Chemical Society)
`2010 Heroes of Chemistry Award for JANUVIA® (American Chemical Society)
`2011 Discoverer's Award (Pharmaceutical Research and Manufacturers of America)
`2011 Industrial Award (Philadelphia Organic Chemists' Club)
`2011 Science and Technology Medal (Research & Development Council of NJ)
`2013 Liberty Science Center Women in STEM Honoree (LSC Women’s Leadership Council and Board of Trustees)
`2015 Gift of Mentoring Award (Metro Women Chemists Committee of the American Chemical Society)
`
`ADVISORY BOARDS
`Industrial Advisory Board, Department of Chemistry & Chemical Biology, Rutgers, The State University of NJ
`2009 – 2015
`
`Editorial Advisory Board, ACS Medicinal Chemistry Letters
`2009 – 2014
`
`
`
`PUBLICATIONS
`C. J. Kowalski, A. E. Weber, and K. W. Fields; "a-Keto Dianion Precursors via Conjugate Additions to Cyclic a-Bromo
`Enones." J. Org. Chem. 1982, 47, 5088.
`
`D. A. Evans and A. E. Weber; "Asymmetric Glycine Enolate Aldol Reactions: Synthesis of Cyclosporine's Unusual Amino
`Acid, MeBmt." J. Amer. Chem. Soc. 1986, 108, 6757.
`
`D. A. Evans, E. B. Sjogren, A. E. Weber, and R. E Conn; "Asymmetric Synthesis of Anti-b-Hydroxy a-Amino Acids."
`Tetrahedron Lett. 1987, 28, 39.
`
`D. A. Evans and A. E. Weber; "Synthesis of the Cyclic Hexapeptide Echinocandin D. New Approaches to the Asymmetric
`Synthesis of b-Hydroxy a-Amino Acids." J. Amer. Chem. Soc. 1987, 109, 7151.
`
`D. A. Evans, A. E. Weber, T. C. Britton, J. A. Ellman, and E. B. Sjogren; "Asymmetric Synthesis of Amino Acids," in
`"Peptides: Chemistry and Biology; Proceedings of the Tenth American Peptide Symposium, May 23-28,1987, St. Louis,
`Missouri", G. R. Marshall, ed., Leiden : ESCOM Science Publishers, 1988, p. 143.
`
`Page 3 of 17
`
`

`
`ANN E WEBER, PHD
`
`PAGE 4
`
`D. H. Rich, C.-Q. Sun, D. Guillaume, B. Dunlap, D. A. Evans, and A. E. Weber; "Synthesis, Biological Activity, and
`Conformational Analysis of (2S,3R,4S)-MeBmt1-cyclosporin, a Novel 1-Position Epimer of Cyclosporin A." J. Med. Chem.
`1989, 32, 1982.
`
`W. J. Greenlee and A. E. Weber; "Renin Inhibitors." Drug News & Perspectives 1991, 4, 332.
`
`A. E. Weber, T. A. Halgren, J. J. Doyle, R. J. Lynch, P. K. S. Siegl, W. H. Parsons, W. J. Greenlee, and A. A. Patchett; "Design
`and Synthesis of P2-P1' Linked Macrocyclic Human Renin Inhibitors." J. Med. Chem. 1991, 34, 2692.
`A. E. Weber, M. G. Steiner, L. Yang, D. S. Dhanoa, J. R. Tata, T. A. Halgren, P. K. S. Siegl, W. H. Parsons, W. J. Greenlee,
`and A. A. Patchett; "Highly Potent, Orally Active P2-P1' Linked Macrocyclic Human Renin Inhibitors," in "Peptides:
`Chemistry and Biology; Proceedings of the Twelfth American Peptide Symposium, June 16-21, 1991, Cambridge,
`Massachusetts" J. E. Rivier and J. A. Smith, eds., Leiden: ESCOM Science Publishers, p. 749.
`
`A. E. Weber, M. G. Steiner, P. A. Krieter, A. E. Colletti, J. R. Tata, T. A. Halgren, R. G. Ball, J. J. Doyle, T. W. Schorn, R. A.
`Stearns, R. R. Miller, P. K. S. Siegl, W. J. Greenlee, and A. A. Patchett; "Highly Potent, Orally Active Diester Macrocyclic
`Human Renin Inhibitors." J. Med. Chem. 1992, 35, 3755.
`
`L. Yang, A. E. Weber, W. J. Greenlee, and A. A. Patchett; "Macrocyclic Renin Inhibitors: Synthesis of a Subnanomolar,
`Orally Active Cysteine Derived Inhibitor." Tetrahedron Lett. 1993, 34, 7035.
`
`A. E. Weber, R. J. Mathvink, L. Perkins, J. E. Hutchins, M. R. Candelore, L. Tota, C. D. Strader, M. J. Wyvratt, and M. H.
`Fisher; “Potent, Selective Benzenesulfonamide Agonists of the Human b3 Adrenergic Receptor.” Bioorg. Med. Chem.
`Lett. 1998, 8, 1101.
`
`E. R. Parmee, H. O. Ok, M. R. Candelore, L. Tota, L. Deng, C. D. Strader, M. J. Wyvratt, M. H. Fisher, and A. E. Weber;
`“Discovery of L-755,507: A Subnanomolar Human b3 Adrenergic Receptor Agonist.” Bioorg. Med. Chem. Lett. 1998, 8,
`1107.
`
`M. H. Fisher, A. M. Amend, T. J. Bach, J. M. Barker, E. J. Brady, M. R. Candelore, D. Carroll, M. A. Cascieri, S.-H. L. Chiu, L.
`Deng, M. J. Forrest, B. Hegarty-Friscino, X. M. Guan, G. J. Hom, J. E. Hutchins, L. J. Kelly, R. J. Mathvink, J. M. Metzger, R.
`R. Miller, H. O. Ok, E. R. Parmee, R. Saperstein, C. D. Strader, R. A. Stearns, G. M. Thompson, L. Tota, P. P. Vicario, A. E.
`Weber, J. W. Woods, M. J. Wyvratt, P. T. Zafian, and D. E. MacIntryre; “A Selective Human b3 Adrenergic Receptor
`Agonists Increases Metabolica Rate in Rhesus Monkeys.” J. Clin. Invest. 1998, 101, 2387.
`A. E. Weber; "β3 Adrenergic Receptor Agonists for the Treatment of Obesity.” Ann. Rep. Med. Chem. 1998, 33, 193.
`A. E. Weber, H. O. Ok, R. F. Alvaro, M. R. Candelore, M. A. Cascieri, S.-H. L. Chiu, L. Deng, M. J. Forrest, G. J. Hom, J. E.
`Hutchins, J. Kao, D. E. MacIntyre, R. J. Mathvink, D. McLoughlin, R. R. Miller, R. C. Newbold, T. V. Olah, E. R. Parmee, L.
`Perkins, R. A. Stearns, C. D. Strader, J. Szumiloski, Y. S. Tang, L. Tota, P. P. Vicario, M. J. Wyvratt , and M. H. Fisher; “3-
`Pyridyloxypropanolamine Agonists of the b3 Adrenergic Receptor with Improved Pharmacokinetic Properties.” Bioorg.
`Med. Chem. Lett. 1998, 8, 2111-2116.
`
`E. M. Naylor, V. J. Colandrea, M. R. Candelore, M. A. Cascieri, L. F. Colwell, Jr., L. Deng, W. P. Feeney, M. J. Forrest, G. J.
`Hom, D. E. MacIntyre, C. D. Strader, L. Tota, P.-R. Wang, M. J. Wyvratt, M. H. Fisher, and A. E. Weber; “3-
`Pyridylethanolamines: Potent and Selective Human b3 Adrenergic Receptor Agonists.” Bioorg. Med. Chem. Lett. 1998,
`8, 3087-3092.
`
`E. R. Parmee, E. M. Naylor, L. Perkins, V. J. Colandrea, H. O. Ok, M. R. Candelore, M. A. Cascieri, L. Deng, W. P. Feeney,
`M. J. Forrest, G. J. Hom, D. E. MacIntyre, R. R. Miller, R. A. Stearns, C. D. Strader, L. Tota, M. J. Wyvratt, M. H. Fisher, and
`A. E. Weber; “Human b3 Adrenergic Receptor Agonists Containing Cyclic Ureido-benzenesulfonamides.” Bioorg. Med.
`Chem. Lett. 1999, 9, 749.
`
`E. M. Naylor, E. R. Parmee, V. J. Colandrea, L. Perkins, L. Brockunier, M. R. Candelore, M. A. Cascieri, L. F. Colwell, Jr., L.
`Deng, W. P. Feeney, M. J. Forrest, G. J. Hom, D. E. MacIntyre, C. D. Strader, L. Tota, P.-R. Wang, M. J. Wyvratt, M. H.
`
`Page 4 of 17
`
`

`
`ANN E WEBER, PHD
`
`PAGE 5
`
`Fisher, and A. E. Weber; “Human b3 Adrenergic Receptor Agonists Containing Imidazolidinone and Imidazolone
`Benzenesulfonamides.” Bioorg. Med. Chem. Lett. 1999, 9, 755.
`
`T. L. Shih, M. R. Candelore, M. A. Cascieri, S.-H. L. Chiu, L. F. Colwell, Jr., L. Deng, W. P. Feeney, M. J. Forrest, G. J. Hom,
`D. E. MacIntyre, R. R. Miller, R. A. Stearns, C. D. Strader, L. Tota, M. J. Wyvratt, M. H. Fisher, and A. E. Weber; “L-
`770,644: A Potent and Selective Human b3 Adrenergic Receptor Agonist with Improved Oral Bioavailability.” Bioorg.
`Med. Chem. Lett. 1999, 9, 1251.
`
`R. J. Mathvink, A. M. Barritta, M. R. Candelore, M. A. Cascieri, L. Deng, L. Tota, C. D. Strader, M. J. Wyvratt, M. H. Fisher,
`and A. E. Weber; “Potent, Selective Human b3 Adrenergic Receptor Agonists Containing a Substituted Indoline-5-
`Sulfonamide Pharmacophore.” Bioorg. Med. Chem. Lett. 1999, 9, 1869.
`
`M. R. Candelore, L. Deng, L. Tota, X.-M. Guan, A. Amend, Y. Liu, R. Newbold, M. A. Cascieri, and A. E. Weber; “Potent
`and Selective Human b3-Adrenergic Receptor Antagonists.” J. Pharmacol. Exper. Ther. 1999, 290, 649.
`D. D. Feng, T. Biftu, M. R. Candelore, M. A. Cascieri, L. F. Colwell, Jr., L. Deng, W. P. Feeney, M. J. Forrest, G. J. Hom, D. E.
`MacIntyre, R. R. Miller, R. A. Stearns, C. D. Strader, L. Tota, M. J. Wyvratt, M. H. Fisher, and A. E. Weber; “Discovery of
`an Orally Bioavailable Alkyl Oxadiazole b3 Adrenergic Receptor Agonist.” Bioorg. Med. Chem. Lett. 2000, 10, 1427.
`T. Biftu, D. Feng, G.-B. Liang, H. Kuo, X. Qian, E. M. Naylor, V. J. Colandrea, M. R. Candelore, M. A. Cascieri, L. F. Colwell,
`Jr., M. J. Forrest, . J. Hom, D. Euan MacIntyre, R. A. Stearns, C. D. Strader, M. J. Wyvratt, M. H. Fisher, and A. E. Weber;
`“Synthesis and SAR of Benzyl and phenoxymethylene oxadiazole Benzenesulfonamides as Selective b3 Adrenergic
`Receptor Agonist Antiobesity Agents.” Bioorg. Med. Chem. Lett. 2000, 10, 1431.
`
`H. O. Ok, L. B. Reigle, M. R. Candelore, M. A. Cascieri, L. F. Colwell, L. Deng, W. P. Feeney, M. J. Forrest, G. J. Hom, D. E.
`MacIntyre, C. D. Strader, L. Tota, P. Wang, M. J. Wyvratt, M. H. Fisher and A. E. Weber; “Substituted Oxazole
`Benzenesulfonamides as Potent Human b3 Adrenergic Receptor Agonists.” Bioorg. Med. Chem. Lett. 2000, 10, 1531.
`R. J. Mathvink, J. S. Tolman, D. Chitty, M. R. Candelore, M. A. Cascieri, L. F. Colwell, Jr., L. Deng, W. P. Feeney, M. J.
`Forrest, G. J. Hom, D. E. MacIntyre, L. Tota, M. J. Wyvratt, M. H. Fisher and A. E. Weber; “Potent, Selective 3-
`Pyridylethanolamine b3 Adrenergic Receptor Agonists Possessing a Thiazole Benzenesulfonamide Pharmacophore.”
`Bioorg. Med. Chem. Lett. 2000, 10, 1971.
`
`L. L. Brockunier, E. R. Parmee, H. O. Ok, M. R. Candelore, . A. Cascieri, L. F. Colwell, Jr., L. Deng, W. P. Feeney, M. J.
`Forrest, G. J. Hom, D. E. MacIntyre, L. Tota, M. J. Wyvratt, M. H. Fisher and A. E. Weber; “Human b3 Adrenergic
`Receptor Agonists Containing 1,2,3-Triazole-Substituted Benzenesulfonamides.” Bioorg. Med. Chem. Lett. 2000, 10,
`2111.
`
`E. R. Parmee, L. L. Brockunier, J. He, S. B. Singh, M. R. Candelore, . A. Cascieri, L. Deng, Y. Liu, L. Tota, M. J. Wyvratt, M. H.
`Fisher and A. E. Weber; “Tetrahydroisoquinoline Derivatives Containing a Benzenesulfonamide Moiety as Potent,
`Selective Human b3 Adrenergic Receptor Agonists.” Bioorg. Med. Chem. Lett. 2000, 10, 2283.
`R. J. Mathvink, J. S. Tolman, D. Chitty, M. R. Candelore, M. A. Cascieri, L. F. Colwell, Jr., L. Deng, W. P. Feeney, M. J.
`Forrest, G. J. Hom, D. E. MacIntryre, R. R. Miller, R. A.Stearns, L. Tota, M. J. Wyvratt, M. H. Fisher, and A. E. Weber;
`“Discovery of a Potent, Orally Bioavailable b3 Adrenergic Receptor Agonist, (R)-N-[4-[2-[[2-Hydroxy-2-(3-
`pyridinyl)ethyl]amino]ethyl]phenyl]-[4-[4-(trifluoromethyl)phen-yl]thiazol-2-yl]benzenesulfonamide.” J. Med. Chem.
`2000, 43, 3832.
`
`M. J. Forrest, G. Hom, T. Bach, M. R. Candelore, M. A Cascieri, C. Strader, L. Tota, M. H. Fisher, J. Szumiloski, H. O. Ok, A.
`E. Weber, M. Wyvratt P. Vicario, O. Marko, L. Deng, C. Cioffe, B. Hegarty-Friscino and E. MacIntyre; “L-750355, a human
`b3 adrenergic receptor agonist; in vitro pharmacology and profile of activity in vivo in the rhesus monkey.” Eur. J.
`Pharmacol. 2000, 407, 175.
`
`Page 5 of 17
`
`

`
`ANN E WEBER, PHD
`
`PAGE 6
`
`L. L. Brockunier, M. R. Candelore, M. A. Cascieri, Y. Liu, L. Tota, M. J. Wyvratt, M. H. Fisher, A. E. Weber, and E. R.
`Parmee; “Human b3 Adrenergic Receptor Agonists Containing Cyanoguanidine and Nitroethylenediamine Moieties.”
`Bioorg. Med. Chem. Lett. 2001, 11, 379.
`
`L. Chu, J. E. Hutchins, A. E. Weber, J.-L. Lo, Y.-T. Yang, K. Chen, R. G. Smith, M. H. Fisher, M. J. Wyvratt, M. T. Goulet;
`“Initial Structure-Activity Relationship of a Novel Class of Nonpeptidyl GnRH Receptor Antagonists: 2-Arylindoles.”
`Bioorg. Med. Chem. Lett. 2001, 11, 509.
`
`G. J. Hom, T. J. Bach, E. Brady, M. R. Candelore, M. A Cascieri, D. J. Fletcher, M. H. Fisher, M. J. Forrest, S. Iliff, R.
`Mathvink, J. Metzger, V. Pecore, R. Saperstein, T. Shih, A. E. Weber, M. Wyvratt, P. Zafian and D. E. MacIntyre; “Beta-3
`adrenoceptor agonist induced increases in lipolysis, metabolic rate, facial flushing and reflex tachycardia in anesthetized
`rhesus monkeys.” J. Pharmacol. Exper. Ther. 2001, 297, 299.
`
`W. Tang, R. A. Stearns, R. R. Miller, J. S. Ngui, R. J. Mathvink, A. E. Weber, G. Y. Kwei, J. R. Strauss, C. A. Keohane, G. A.
`Doss, S.-H. L. Chiu, T. A. Baillie; “Metabolism of a thiazole benzenesulfonamide derivative, a potent and selective agonist
`of the human β3-adrenergic receptor, in rats: identification of a novel isethionic acid conjugate.” Drug Metab. Dispos.
`2002, 30, 778.
`
`S. D. Edmondson, A. Mastracchio, J. He, C. C. Chung, M. J. Forrest, S. Hofsess, E. MacIntyre, J. Metzger, N. O’Connor, K.
`Patel, X. Tong, M. R. Tota, L. H. T. Van der Ploeg, J. P. Varnerin, M. H. Fisher, M. J. Wyvratt, A. E. Weber, E. R. Parmee;
`“Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective
`PDE3B inhibitors.” Bioorg. Med. Chem. Lett. 2003,13, 3983.
`
`E. R. Parmee, J. He, A. Mastracchio, S. D. Edmondson, L. Colwell, G. Eiermann, W. P. Feeney, B. Habulihaz, H. He, R.
`Kilburn, B. Leiting, K. Lyons, F. Marsilio, R. Patel, A. Petrov, J. di Salvo, J. K. Wu, N. A. Thornberry, A. E. Weber; “4-Amino
`cyclohexylglycine analogs as potent dipeptidyl peptidase IV inhibitors.” Bioorg. Med. Chem. Lett. 2004, 14, 43.
`
`A. Mastracchio, E. R. Parmee, B. Leiting, F. Marsilio, R. Patel, N. A. Thornberry, A. E. Weber, and S. D. Edmondson;
`“Heterocycle fused cyclohexylglycine derivatives as novel dipeptidyl peptidase-IV inhibitors.” Heterocycles 2004, 62,
`203.
`
`W. T. Ashton, H. Dong, R. M. Sisco, G. A. Doss, B. Leiting, R. A. Patel, J. K. Wu, F. Marsilio, N. A. Thornberry, and A. E.
`Weber; “Diastereoselective Synthesis and Configuration-Dependent Activity of (3-Substituted-cycloalkyl)glycine
`Pyrrolidides and Thiazolidides as Dipeptidyl Peptidase IV Inhibitors.” Bioorg. Med. Chem. Lett. 2004, 14, 859.
`
`C. G. Caldwell, P. Chen, J. He, E. R. Parmee, B. Leiting, F. Marsilio, R. A. Patel, J. K. Wu, G. J. Eiermann, A. Petrov, H. He, K.
`A. Lyons, N. A. Thornberry, and A. E. Weber; “Fluoropyrrolidine Amides as Dipeptidyl Peptidase IV Inhibitors.” Bioorg.
`Med. Chem. Lett. 2004, 14, 1265.
`
`A. Weber; “Dipeptidyl Peptidase IV Inhibitors for the Treatment of Diabetes.” J. Med. Chem. 2004, 47, 4135.
`J. Xu, H. O. Ok, E. J. Gonzalez, L. F. Colwell Jr., B. Habulihaz, H. He, B. Leiting, K. A. Lyons, F. Marsilio, R. A. Patel, J. K. Wu,
`N. A. Thornberry, A. E. Weber, E. R. Parmee; “Discovery of Potent and Selective β-Homophenylalanine Based Dipeptidyl
`Peptidase IV Inhibitors.” Bioorg. Med. Chem. Lett. 2004, 14, 4759.
`
`L. L. Brockunier, J. He, L. F. Colwell Jr., B. Habulihaz, H. He, B. Leiting, K. A. Lyons, F. Marsilio, R. A. Patel, Y. Teffera, J. K.
`Wu, N. A. Thornberry, A. E. Weber, E. R. Parmee; “Substituted Piperazines as Novel Dipeptidyl Peptidase IV Inhibitors.”
`Bioorg. Med. Chem. Lett. 2004, 14, 4763.
`
`S. D. Edmondson, A. Mastracchio, M. Beconi, L. F. Colwell Jr., B. Habulihaz, H., He, S. Kumar, B. Leiting, K. A. Lyons, A.
`Mao, F. Marsilio, R. A. Patel, J. K. Wu, L. Zhu, N. A. Thornberry, A. E. Weber and E. R. Parmee; “Potent and Selective
`Proline Derived Dipeptidyl Peptidase IV Inhibitors.” Bioorg. Med. Chem. Lett. 2004, 14, 5151.
`
`D. Kim, L. Wang, M. Beconi, G. J. Eiermann, M. H. Fisher, H. He, G. J. Hickey, J. E. Kowalchick, B. Leiting, K. Lyons, F.
`Marsilio, M. E. McCann, R. A. Patel, A. Petrov, G. Scapin, S. B. Patel, R. Sinha Roy, J. K. Wu, M. J. Wyvratt, B. Zhang, L.
`Zhu, N. A. Thornberry, and A. E. Weber; “(2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-
`
`Page 6 of 17
`
`

`
`ANN E WEBER, PHD
`
`PAGE 7
`
`7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the
`Treatment of Type 2 Diabetes.” J. Med. Chem. 2005, 48, 141.
`
`W. T. Ashton, R. M. Sisco, H. Dong, K. A. Lyons, H. He, G. A. Doss, B. Leiting, R. A. Patel, J. K. Wu, F. Marsilio, N. A.
`Thornberry and A. E. Weber; “Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused
`thiazole, oxazole, isoxazole, or pyrazole.” Bioorg. Med. Chem. Lett. 2005, 15, 2253.
`
`J. Xu, L. Wei, R. Mathvink, J. He, Y.-J. Park, H. He, B. Leiting, K. A. Lyons, F. Marsilio, R. A. Patel, J. K. Wu, N. A. Thornberry,
`and A. E. Weber; “Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.” Bioorg.
`Med. Chem. Lett. 2005, 15, 2533.
`
`S. D. Edmondson, A. Mastracchio, J. L. Duffy, G. J. Eiermann, H. He, I. Ita, B. Leiting, J. F. Leone, K. A. Lyons, A. M.
`Makarewicz, R. A. Patel, A. Petrov, J. K. Wu, N. A. Thornberry and A. E. Weber; “Discovery of potent and selective orally
`bioavailable β-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.” Bioorg. Med. Chem. Lett. 2005, 15,
`3048.
`
`G. R. Lankas, B. Leiting, R. Sinha Roy, G. J. Eiermann, M. G. Beconi, T. Biftu, C.–C. Chan, S. Edmondson, W. P. Feeney, H.
`He, D. E. Ippolito, D. Kim, K. A. Lyons, H. O. Ok, R. A. Patel, A. N. Petrov, K. A. Pryor, X. Qian, L. Reigle, A. Woods, J. K. Wu,
`D. Zaller, X. Zhang, L. Zhu, A. E. Weber, and N. A. Thornberry; “Dipeptidyl Peptidase IV Inhibition for the Treatment of
`Type 2 Diabetes: Potential Importance of Selectivity Over Dipeptidyl Peptidases 8 and 9.” Diabetes 2005, 54, 2988.
`
`J. Xu, L. Wei, R. Mathvink, S. D. Edmondson, A. Mastracchio, G. J. Eiermann, H. He, J. F. Leone, B. Leiting, K. A. Lyons, F.
`Marsilio, R. A. Patel, A. Petrov, J. K. Wu, N. A. Thornberry, and A. E. Weber; “Discovery of Potent, Selective and Orally
`Bioavailable Pyridone Based Dipeptidyl Peptidase-4 Inhibitors.” Bioorg. Med. Chem. Lett. 2006, 16, 1346.
`
`S. D. Edmondson, A. Mastracchio, R. J. Mathvink, J. He, B. Harper, Y.-J. Park, M. Beconi, J. Di Salvo, G. J. Eiermann, H. He,
`B. Leiting, J. F. Leone, D. A. Levorse, K. Lyons, R. A. Patel, S. B. Patel, A. Petrov, G. Scapin, J. Shang, R. Sinha Roy, A. Smith,
`J. K. Wu, S. Xu, B. Zhu, N. A. Thornberry, and A. E. Weber; “(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-
`4-oxo-2-(4-[1,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)butanamide: A Selective α-Amino Amide Dipeptidyl Peptidase IV
`Inhibitor for the Treatment of Type 2 Diabetes.” J. Med. Chem. 2006, 49, 3614.
`
`J. Xu, L. Wei, R. J. Mathvink, S. D. Edmondson, G. J. Eiermann, H. He, J. F. Leone, B. Leiting, K. A. Lyons, F. Marsilio, R. A.
`Patel, S. B. Patel, A. Petrov, G. Scapin, J. K. Wu, N. A. Thornberry and A. E. Weber; “Discovery of potent, selective, and
`orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.” Bioorg. Med. Chem. Lett. 2006, 16, 5373.
`
`T. Biftu, D. Feng, X. Qian, G.-B. Liang, G. Kieczykowski, G. Eiermann, H. He, B. Leiting, K. Lyons, A. Petrov, R. Sinha Roy, B.
`Zhang, G. Scapin, S. Patel, Y.-D. Gao, S. Singh, J. Wu, X. Zhang, N. A. Thornberry and A. E. Weber; “(3R)-4-[(3R)-3-Amino-
`4-(2,4,5-trifluorophenyl)-butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a Selective Dipeptidyl Peptidase IV
`Inhibitor for the Treatment of Type 2 Diabetes.” Bioorg. Med. Chem. Lett. 2007, 17, 49.
`
`N. A. Thornberry and A. E. Weber; “Discovery of JANUVIA™ (Sitagliptin), a Selective Dipeptidyl Peptidase IV Inhibitor for
`the Treatment of Type2 Diabetes.” Curr. Topics Med. Chem. 2007, 14, 557.
`
`G.-B. Liang, X. Qian; D. Feng; T. Biftu; G. Eiermann; H. He; B. Leiting; K. Lyons; A. Petrov; Ra. Sinha Roy; B. Zhang; J. Wu;
`X. Zhang; N. Thornberry; A. E. Weber; “Optimization of 1,4-Diazepan-2-one Containing Dipeptidyl Peptidase IV Inhibitors
`for the Treatment of Type 2 Diabetes.” Bioorg. Med. Chem. Lett. 2007, 17, 1903.
`
`J. L. Duffy, B. A. Kirk, L. Wang, G. J. Eiermann, H. He, B. Leiting, K. A. Lyons, R. A. Patel, S. B. Patel, A. Petrov, G. Scapin, J.
`K. Wu, N. A. Thornberry and A. E. Weber; “4-Aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent,
`selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.” Bioorg. Med. Chem. Lett. 2007, 17, 2879.
`
`KIM, D., KOWALCHICK, J.E., EDMONDSON, S.D., MASTRACCHIO, A., XU, J., EIERMANN, G.J., LEITING, B., WU, J.K., PRYOR,
`K.D., PATEL, R.A., HE, H., LYONS, K.A., THORNBERRY, N.A., WEBER, A.E. “Triazolopiperazine-amides as dipeptidyl
`peptidase iv inhibitors: close analogs of JANUVIA™ (sitagliptin phosphate).” Bioorg. Med. Chem. Lett. 2007, 17, 3373.
`
`BIFTU, T., SCAPIN, G., SINGH, S.B., FENG, D.D., BECKER, J.W., EIERMANN, G.J., HE, H., LYONS, K.A., PATEL, S.B., PETROV,
`A., SINHA ROY, R., ZHANG, B.B., WU, J.K., ZHANG, X., DOSS, G.A., THORNBERRY, N.A., WEBER, A.E. “Rational design of a
`
`Page 7 of 17
`
`

`
`ANN E WEBER, PHD
`
`PAGE 8
`
`novel, potent and orally bioavailable cyclohexylamine dpp-4 inhibitor by application of molecular modeling and x-ray
`crystallography of sitagliptin.” Bioorg. Med. Chem. Lett. 2007, 17, 3384.
`
`GAO, Y., FENG, D.D., SHERIDAN, R.P., SCAPIN, G., PATEL, S.B., WU, J.K., ZHANG, X., SINHA ROY, R., THORNBERRY, N.A.,
`WEBER, A.E., BIFTU, T. “Modeling assisted rational design of novel, potent and selective pyrrolopyrimidine dpp-4
`inhibitors.” Bioorg. Med. Chem. Lett. 2007, 17, 3877.
`
`COX, J.M., HARPER, B., MASTRACCHIO, A., LEITING, B., SINHA ROY, R., PATEL, R.A., WU, J.K., LYONS, K.A., HE, H., XU, S.S.,
`ZHU, B., THORNBERRY, N.A., WEBER, A.E., EDMONDSON, S.D. “Discovery of 3-aminopiperidines as potent, selective, and
`orally bioavailable dipeptidyl peptidase IV inhibitors.” Bioorg. Med. Chem. Lett. 2007, 17, 4579.
`
`KAELIN, D.E., SMENTON, A.L., EIERMANN, G.J., HE, H., LEITING, B., LYONS, K.A., PATEL, R.A., PATEL, S.B., PETROV, A.,
`SCAPIN, G., WU, J.K., THORNBERRY, N.A., WEBER, A.E., DUFFY, J.L. 4-arylcyclohexylalanine analogs as potent, selective,
`and orally active inhibitors of dipeptidyl peptidase IV. Bioorg. Med. Chem. Lett. 2007, 17, 5806.
`
`CHEN, P., CALDWELL, C.G., MATHVINK, R.J., LEITING, B., MARSILIO, F., PATEL, R.A., WU, J.K., HE, H., LYONS, K.A.,
`THORNBERRY, N.A., WEBER, A.E. Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of
`diabetes. Bioorg. Med. Chem. Lett. 2007, 17, 5853.
`
`KOWALCHICK, J.E., LEITING, B., PRYOR, K.D., MARSILIO, F., WU, J.K., HE, H., LYONS, K.A., EIERMANN, G.J., PETROV, A.,
`SCAPIN, G., PATEL, R.A., THORNBERRY, N.A., WEBER, A.E., KIM, D.* Design, synthesis, and biological evaluation of
`triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. Bioorg.
`Med. Chem. Lett. 2007, 17, 5934.
`
`HOYT, S.B.* , LONDON, C., OK, H.O., GONZALEZ, E.J., DUFFY, J.L., WEBER, A.E., ABBADIE, C., DEAN, B.J., FELIX, J.P.,
`GARCIA, M.L., JOCHNOWITZ, N., KARANAM, B.V., LI, X., LYONS, K.A., MCGOWAN, E.M., MACINTYRE, D.E., MARTIN, W.J.,
`SMITH, M.M., TSCHIRRET-GUTH, R.A., WARREN, V.A., WILLIAMS, B.S., KACZOROWSKI, G.J., PARSONS, W.H.
`“Benzazepinone Nav1.7 Blockers: Potential Treatments for Neuropathic Pain", Bioorg. Med. Chem. Lett. 2007 17, 6172.
`
`WEBER, A.E., THORNBERRY, N.A. “Case history: JANUVIA™ (sitagliptin), a selective dipeptidyl peptidase IV inhibitor for
`the treatment of type 2 diabetes.” Ann. Rep. Med. Chem. 2007, 42, 95.
`
`KIM, D., KOWALCHICK, J.E., BROCKUNIER, L.L., PARMEE, E.R., BECONI, M.G., EIERMANN, G.J., FISHER, M.H., HE, H.,
`LEITING, B., LYONS, K.A., SCAPIN, G., PATEL, S.B., PETROV, A., PRYOR, K.D., SINHA ROY, R., WU, J.K., ZHANG, X.,
`WYVRATT, M.J., ZHANG, B.B., ZHU, L., THORNBERRY, N.A., WEBER, A.E. “Discovery of potent and selective DPP-4
`inhibitors derived from β-aminoamides bearing subsituted triazolopiperazines.” J. Med. Chem. 2008, 51, 589.
`
`EDMONDSON, S.D., WEI, L., XU, J., SHANG, J., XU, S.S., PANG, J., CHAUDHARY, A.G., DEAN, D.C., HE, H., LEITING, B.,
`LYONS, K.A., PATEL, R.A., PATEL, S.B., SCAPIN, G., WU, J.K., BECONI, M.G., THORNBERRY, N.A., WEBER, A.E.
`“Fluoroolefins as amide bond mimics in dipeptidyl peptidase four inhibitors.” Bioorg. Med. Chem. Lett. 2008, 18, 2409.
`
`LIANG, G., QIAN, X., BIFTU, T., SINGH, S., GAO, Y., SCAPIN, G., PATEL, S.B., LEITING, B., PATEL, R.A., WU, J.K., ZHANG, X.,
`LYONS, K.A., HE, H., THORNBERRY, N.A., WEBER, A.E. "Discovery of new binding elements in DPP-4 inhibition and their
`applications in novel DPP-4 inhibitor design." Bioorg. Med. Chem. Lett. 2008, 18, 3706.
`
`ZHU, C., HANSEN, A.R., BATEMAN, T.J., CHEN, Z., HOLT, T.G., HUBERT, J.A., KARANAM, B.V., LEE, S.J., PAN, J., QIAN, S.,
`REDDY, V.B.G., REITMAN, M.L., STRACK, A.M., TONG, V.W., WEINGARTH, D.T., WOLFF, M.S., MACNEIL, D.J., WEBER, A.E.,
`DUFFY, J.L., EDMONDSON, S.D. "Discovery of imidazole carboxamides as potent and selective CCK1R agonists." Bioorg.
`Med. Chem. Lett. 2008, 18, 4393.
`
`BERGER, R., ZHU, C., HANSEN, A.R., HARPER, B., CHEN, Z., HOLT, T.G., HUBERT, J.A., LEE, S.J., PAN, J., QIAN, S., REITMAN,
`M.L., STRACK, A.M., WEINGARTH, D.T., WOLFF, M.S., MACNEIL, D.J., WEBER, A.E., EDMONDSON, S.D. "2-Substituted
`piperazine derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity."
`Bioorg. Med. Chem. Lett. 2008, 18, 4833.
`
`Page 8 of 17
`
`

`
`ANN E WEBER, PHD
`
`PAGE 9
`
`Edmondson, S.D., Mastracchio, A., Cox, J.M., Eiermann, G.J., He, H., Lyons, K.A., Patel, R.A., Patel, S.B., Petrov, A., Scapin,
`G., Wu, J.K., Xu, S., Zhu, B., Thornberry, N.A., SinhaRoy, R., Weber, A.E., "Aminopiperidine Fused Imidazoles as Dipeptidyl
`Peptidase IV Inhibitors." Bioorg. Med. Chem. Lett. 2009, 19, 4097.
`
`SHAO, P.P.* , YE, F., WEBER, A.E., LI, X., GARCIA, M.L., PRIEST, B.T., FELIX, J.P., WILLIAMS, B.S., KACZOROWSKI, G.J.,
`MCGOWAN, E.M., ABBADIE, C., MCMASTERS, D.R., GAO, Y., LYONS, K.A., PARSONS, W.H., SMITH, M.M., MARTIN, W.J.
`"Discovery of isoxazole Nav1.7 sodium channel blockers for treatment of chronic pain." Bioorg. Med. Chem. Lett. 2009,
`19, 5334.
`
`SHAO, P.P., YE, F., WEBER, A.E., LI, X., GARCIA, M.L., PRIEST, B.T., FELIX, J.P., WILLIAMS, B.S., KACZOROWSKI, G.J.,
`MCGOWAN, E.M., ABBADIE, C., MCMASTERS, D.R., GAO, Y., PARSONS, W.H., LYONS, K.A., SMITH, M.M., MARTIN, W.J.
`"Discovery of a novel class of isoxazoline Nav1.7 sodium channel blockers." Bio