Chemnomics

Professional Presentations

1. Chen, Y., Cheng, D., Tomczuk, B., Bone, R., Huebert, N., “Pharmacokinetic of TDP4815 in human after single oral administration”, AAPS Annual Meeting, 96, San Diego, CA, Nov. 9-15, 2007.

2. Chen, Y., Cheng, D., Dasgupta, M., Tomczuk, B., Bone, R., Huebert, N., “Pharmacokinetic properties of TDP4815 after single intravenous and oral administrations to rat, rabbit, monkey, dog”, AAPS Annual Meeting, 95, San Diego, CA, Nov. 9-15, 2007.

3. Subasinghe, N., Yurkow, E., Crysler, C., Travins, J., Ballentine, S., Khalil, E., Hufnagel, H., Neville, M., Gaul, M., Tomczuk, B., Molloy, C., “PEGylated C1s/MASP2 Protease Inhibitors as Novel Parenteral Agents for the Treatment of Complement-Mediated Diseases”, Inflamm. Res. Supplement 2, 2006, S115.

4. Chen, Y., Cheng, D., Dasgupta, M., Tomczuk, B., Marugan, J.J., Manthey, C., Huebert, N., “In vivo biliary excretion of 3DP223206 in the rat and in vitro metabolism”, AAPS, Nov. 6-11, 2005.

5. Qiao, L., Baumann, C., Crysler, C., Ninan, N., Abad, M., Spurlino, J., DesJarlais, R., Kervinen, J., Neeper, M., Bayoumy, S., Williams, R., Deckman, I., Dasgupta, M., Reed, R., Huebert, N., Tomczuk, B., Moriarty, K., “Discovery of Dipeptidyl Peptidase IV (DPP-IV) Inhibitors by Structure-Based de novo Design”, 4th General Meeting of the International Proteolysis Society, Quebec City, Canada, PII41, October 15-19, 2005.

6. Chen, Y., Dasgupta, M., Cheng, D., Marugan, J.J., Manthey, C., Tomczuk, B., Huebert, N., “In vitro metabolism and in vivo biliary excretion of 3DP223206 in the rat”, AAPS National Meeting, Nashville, TN, November 6-10, 2005.

7. Lu, T., Grasberger, B., Schubert, C., Parks, D. J., Carver, T. E., Koblish, H. K., Cummings, M. D., LaFrance, L. V., Milkiewicz, K. L., Calvo, R. R., Maguire, D., Lattanze, J., Franks, C. F., Zhao, S-y, Ramachandren, K., Manthey, C. L., Deckman, I. C., Spurlino, J. C., Maroney, A. C., Tomczuk, B. E., Molloy, C. J., Bone, R., “Discovery, SAR, x-ray Crystal Structure and Biological Evaluation of Small Molecule HDM2 Antagonists: 1,4-Benzodiazepine-2, 5-diones”, 4^th J&JPRD Symposium on Drug Discovery, April 7-8, 2005, Antwerp, Belgium.

8. Qiao, L., Baumann, C., Crysler, C., Ninan, N., Abad, M., Spurlino, J., DesJarlais, R., Kervinen, J., Neeper, M., Bayoumy, S., Williams, R., Deckman, I., Tomczuk, B., Moriarty, K., “Discovery of dipeptidyl peptidase IV (DPP-IV) inhibitors by structure-based de novo design”, 229^th Am. Chem. Soc. National Meeting, San Diego, CA, MEDI 205, March 13-17, 2005.

9. Kreutter, K. D., Lee, L., Lu, T., Mohan, V., Patel, S., Huang, H., Xu, G., Fitzgerald, M., Crysler, C., Player, M. R., Giardino, E. C., Maryanoff, B. E., Damiano, B. P., Tomczuk, B. E., Huebert, N. D., Eisennagel, S., Dasgupta, M., Spurlino, J. C., McMillan, M., “Novel Orally Bioavailable Thrombin Inhibitors: Cyanofluorophenylacetic Acid Derivatives”, 229^th Am. Chem. Soc. National Meeting, San Diego, CA, MEDI 243, March 13-17, 2005.

10. Lee, L., Kreutter, K. D., Pan, W., Lu, T., Crysler, C., Eisennagel, S., MacMillan, M., Spurlino, J., Tomczuk, B., Player, M., Mohan, V., “Potent Small Molecule, Non-Peptidic Chlorophenyl Acetamide Thrombin Inhibitors”, 229^th Am. Chem. Soc. National Meeting, San Diego, CA, MEDI 244, March 13-17, 2005.

11. Chen, Y., Dasgupta, M., Eisennagel, S., Tomczuk, B., Marugan, J.J., Manthey, C., Huebert, N., “In vivo metabolism of 14C-3DP223206 following intravenous administration to intact and bile duct cannulated rats”, 7^th International ISSX Meeting, Vancouver, CA, #490, August 29-September 2, 2004.

12. Gushue, J., Leonard, K., Pan, W., Anaclerio, B., Guo, Z., DesJarlais, R., Lattanze, J., Crysler, C., Marugan, J. J., Manthey, C., Tomczuk, B., Lu, T., Markotan, T., Chaikin, M., Donatelli, R., Hubert, N., Eissenagwel, S., Dasgupta, M., Fries, H., “Non-peptidic avb3 antagonist containing indol-1-yl propionic acids”, 228^th Am. Chem. Soc. National Meeting, Philadelphia, PA, MEDI 281, August 22-26, 2004.

13. Marugan, J. J., Anaclerio, B., LaFrance, L., Lu, T., Markotan, T., Gushue, J., Leonard, K., Guo, Z., Pan, W., Raboisson, P., Tomczuk, B., Manthey, C., “N-substituted Indoles as Potent, Selective, and Bioavailable alphavbeta3/alphavbeta5 Inhibitors”, 227^th Am. Chem. Soc. National Meeting, Anaheim, CA, MEDI 347, March 28-April 1, 2004.

14. Anaclerio, B., LaFrance, L., Lu, T., Markotan, T., Marugan, J. J., Gushue, J., Leonard, K., Guo, Z., Pan, W., Manthey, C., Chaikin, M., Donatelli, R., Crysler, C., Kirkpatrick, J., Huebert, N., Eisennagel, S., Dasgupta, M., Fries, H., Tomczuk, B., “Indole Propionic Acids as Potent, Bioavailable a_vb₃/a_vb₅ Inhibitors”, New Advances in Drug Discovery, Keystone, CO, March 21-26, 2004.

15. Giardino, E.C., Haertlein, B., de Garavilla, L., Kauffman, J., Costanzo, M., Maryanoff, B., Damiano, B., Lu, T., Tomczuk, B., Bone, R., Andrade-Gordon, P., “In Vitro Characteristics, Anticoagulant Effects and Antithrombotic Efficacy of JNJ-6368661, a Potent, Orally Active and Selective Direct Thrombin Inhibitor”, American Soc. Hematology, December 5-9, 2003.

16. Markotan, T., Lu, T., Coppo, F., Tomczuk, B., Crysler, C., Eisennagel, S., Spurlino, J., Soll, R., Bone, R. “Oxyguanidines: Discovery of a Novel Orally Active Thrombin Inhibitor through Structure-Based Drug Design and Parallel Synthesis”, 226^th Am. Chem. Soc. National Meeting, New York, New York, MEDI-087, September 7-11, 2003.

17. Chaikin, M., Marugan, J. J., Tomczuk, B., Eisennagel, S., Gushue, J., Lee, Y.K., Manthey, C., “A Plasma-Echistatin Model Useful for Characterizing the Pharmacodynamic, Pharmacokinetic, and Plasma Protein Binding Properties of avb3-Integrin Inhibitors”, Proc. Am. Assoc. Cancer Res., 44, #107124, April, 2003.

18. Lu, T., Tomczuk, B., Soll, R.M., Fedde, C., Wang, A., Murphy, L., Crysler, C., Dasgupta, M., Eisennagel, S., Spurlino, J., Bone, R., “Oxyguanidines: Application to nonpeptidic phenyl-based thrombin inhibitors”, 224^th Am. Chem. Soc. National Meeting, Boston, MA, MEDI-287, August 18-22, 2002.

19. Manthey, C.L., Lee, Y., Wang, A., Crysler, C., Zhao, S., Bone, R.F., Soll, R.M., Tomczuk, B.E., “Characterization of O-Guanidines as novel alpha-v-beta-3 Inhibitors”, Proc. Am. Assoc. Cancer Res., 42, March 24-28, 2001, 368.

20. Dasgupta, M., Ott, H., Eisennagel, S., Tomczuk, B., “Accelerated Method for In Vitro Permeability Measurement: Application for Preclinical Screening of Thrombin Inhibitors”, 10^th North American ISSX, Indianapolis, IN, October 24-28, 2000.

21. Pan, W., Lu, T., Soll, R. M., Tomczuk, B. E., Bone, R., Spurlino, J., Green, D. W., “Heteroaryl keto thrombin inhibitors:Design and Synthesis”, 220^th Am. Chem. Soc. National Meeting, Washington, DC, MEDI 285, August 20-24, 2000.

22. Markotan, T. P., Lu, T., Soll, R. M., Tomczuk, B. E., Spurlino, J., Murphy, L. G., “Amino acid alkoxyguanidines as thrombin inhibitors”, 220^th Am. Chem. Soc. National Meeting, Washington, DC, MEDI 287, August 20-24, 2000.

23. Green, D., Manthey, C. L., Crysler, C. S., Zhou, Z., Lee, Y-K., Molloy, C. J., Tomczuk, B. E., Dhanoa, D. S., Soll, R. M., Bone, R. F., “Identification of novel small molecule vitronectin receptor (v3integrin) antagonists”, American Association for Cancer Research, Washington, DC, #0738, November 16-19, 1999.

24. Lu, T., Soll, R., Tomczuk, B., Illig, C., Subasinghe, N., Bone, R., Locke, K., Harrison, R., Spurlino, J. “A Novel Series of Potent, Non-peptide Active-site Thrombin Inhibitors”, 217^th Am. Chem. Soc. National Meeting, Anaheim, CA, MEDI-079, March 21-25, 1999.

25. Lu, T., Soll, R., Tomczuk, B., Illig, C., Fedde, C., Murphy, L., Spurlino, J., Bone, R., “Amidinohydrazones as Guanidine Bioisosteres: Application to a New Class of Potent, Selective, and Orally Bioavailable, Non-amide Based Small Molecular Thrombin Inhibitors”, 217^th Am. Chem. Soc. National Meeting, Anaheim, CA, MEDI-078, March 21-25, 1999.

26. Tomczuk,B.E.,”Recent Developments in the Search for Orally Bioavailable Small Molecule Inhibitors of Proteases Involved in the Coagulation Cascade”, IBC’s 9th Annual Advances in Anticoagulant, Antithrombotic, and Thrombolytic Drugs, Cambridge, MA, September 10-12, 1998.

27. Lu, T., Soll, R., Tomczuk, B., Illig, C., Subasinghe, N., Bone, R., Locke, K., Harrison, R., Spurlino, J., “A Novel Series of Potent, Non-peptide Active-site Thrombin Inhibitors”, 212^th Am. Chem. Soc. National Meeting, Orlando, FL, MEDI-185, August 25-29, 1996.

28. Lu, T., Soll, R., Illig, C., Tomczuk, B., Subasinghe, N., Bone, R., Locke, K., Harrison, R., Spurlino, J., “Active-site Thrombin Inhibitors Based on a Phenyl Template”, 212^th Am. Chem. Soc. National Meeting, Orlando, FL, MEDI-200, August 25-29, 1996.

29. Tomczuk, B. E., Gowravaram, M. R., Johnson, J. S., Delecki, D., Cook, E. R., Ghose, A., Mathiowetz, A. M., Spurlino, J. C., Rubin, B., Smith, D. L., Pulvino, T., Wahl, R. C.,“P1' Heteroatom-Based Modifications of Hydroxamate Inhibitors of Collagenases and Stromelysin”, National Meeting of the American Chemical Society, Anaheim, CA, MEDI 172, April 2-6, 1995.

30. Ghose, A. K., Treasurywala, A. M., Logan, M. E., Wahl, R., Tomczuk, B., Goswami, R., Jaeger, E. P., "A Few Critical Aspects of Molecular Superimposition of Flexible Organic Molecules", 11th Annual Mol. Graphics Society, Univ. of Bath, U. K., April 13-16, 1992.

31. Venepalli, B. R., Lawrence, K. B., Tomczuk, B. E., "Nine-membered Lactams containing Phenyl and Benzyl Substituents as NK-2 Ligands", Gordon Research Conference on Org. Reactions and Processes, July 13-17, 1992.

32. Venepalli, B. R., Appell, K. C., Bell, M. R., Dority, J. A., Goswami, R., Hall, P. L., Kumar, V., Lawrence, K. B., Logan, M. E., Lussier, B. B., Scensny, P. M., Seelye, J. A., Tomczuk, B. E., Yanni, J. M., "Synthesis and Substance P Receptor Binding Activity of a Series of Heterosteroids", Fourth Chemical Congress of North America, New York, MEDI 158, August, 1991.

33. Tomczuk, B. E., Taylor, C. R., Jr., Moses, L. M., Sutherland, D. B., Johnson, D. N., Kinnier, W. B., and Kilpatrick, B. F.,"2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anxiolytics and anticonvulsants", American Chemical Society National Meeting, Boston, MEDI 112, April,1990.

34. Kilpatrick, B. F., Tabor, R. D., Young, R., Tomczuk, B. E., Taylor, C. R., and Johnson, D. N.,"AHR-14749: A New BZ-1 Benzodiazepine receptor selective anxiolytic/anticonvulsant", Society for Neuroscience, Phoenix, AZ, 1989.

35. Tomczuk, B., Kumar, A., and Hite, G.,"Synthons for the elaboration of cyclobutanone analogs of penicillins", American Pharmaceutical Society, 36th National, p.82, 1984.

36. Tomczuk, B., Kumar, A., and Hite, G., Kelly, J.A., Moews, P.C., Knox, J.R., Tilton, R.C., Frere, J.M., Ghuysen, J.M., "Cyclobutanone analogs of penicillin", American Pharmaceutical Society, 35th National, p.172, 1983.