Search Results - "Stauffer, Kenneth J."

Discovery and Evaluation of Potent P1 Aryl Heterocycle-Based Thrombin Inhibitors by Young, Mary Beth, Barrow, James C, Glass, Kristen L, Lundell, George F, Newton, Christina L, Pellicore, Janetta M, Rittle, Kenneth E, Selnick, Harold G, Stauffer, Kenneth J, Vacca, Joseph P, Williams, Peter D, Bohn, Dennis, Clayton, Franklin C, Cook, Jacquelynn J, Krueger, Julie A, Kuo, Lawrence C, Lewis, S. Dale, Lucas, Bobby J, McMasters, Daniel R, Miller-Stein, Cynthia, Pietrak, Beth L, Wallace, Audrey A, White, Rebecca B, Wong, Bradley, Yan, Youwei, Nantermet, Philippe G

“…In an effort to discover potent, clinically useful thrombin inhibitors, a rapid analogue synthetic approach was used to explore the P1 region. Various…”
Get full text

Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors by Isaacs, Richard C.A., Newton, Christina L., Cutrona, Kellie J., Mercer, Swati P., Payne, Linda S., Stauffer, Kenneth J., Williams, Peter D., Cook, Jacquelynn J., Krueger, Julie A., Lewis, S. Dale, Lucas, Bobby J., Lyle, Elizabeth A., Lynch, Joseph J., McMasters, Daniel R., Naylor-Olsen, Adel M., Michener, Maria T., Wallace, Audrey A.

“…Structure based design techniques were used to exploit the putative similarity in binding mode of an aminopyridinone thrombin inhibitor 2 and a trisubstituted…”
Get full text

9-Hydroxyazafluorenes and Their Use in Thrombin Inhibitors by Stauffer, Kenneth J, Williams, Peter D, Selnick, Harold G, Nantermet, Philippe G, Newton, Christina L, Homnick, Carl F, Zrada, Matthew M, Lewis, S. Dale, Lucas, Bobby J, Krueger, Julie A, Pietrak, Beth L, Lyle, Elizabeth A, Singh, Rominder, Miller-Stein, Cynthia, White, Rebecca B, Wong, Bradley, Wallace, Audrey A, Sitko, Gary R, Cook, Jacquelyn J, Holahan, Marie A, Stranieri-Michener, Maria, Leonard, Yvonne M, Lynch, Joseph J, McMasters, Daniel R, Yan, Youwei

“…Optimization of a previously reported thrombin inhibitor, 9-hydroxy-9-fluorenylcarbonyl-l-prolyl-trans-4-aminocyclohexylmethylamide (1), by replacing the…”
Get full text

Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability by Morrissette, Matthew M, Stauffer, Kenneth J, Williams, Peter D, Lyle, Terry A, Vacca, Joseph P, Krueger, Julie A, Lewis, S.Dale, Lucas, Bobby J, Wong, Bradley K, White, Rebecca B, Miller-Stein, Cynthia, Lyle, Elizabeth A, Wallace, Audrey A, Leonard, Yvonne M, Welsh, Denise C, Lynch, Joseph J, McMasters, Daniel R

“…In order to overcome several limitations of our lead compound, which possessed a fluorenyl side chain in P3, we synthesized a series of analogs where we…”
Get full text

Discovery and Evaluation of Potent P 1 Aryl Heterocycle-Based Thrombin Inhibitors by Young, Mary Beth, Barrow, James C., Glass, Kristen L., Lundell, George F., Newton, Christina L., Pellicore, Janetta M., Rittle, Kenneth E., Selnick, Harold G., Stauffer, Kenneth J., Vacca, Joseph P., Williams, Peter D., Bohn, Dennis, Clayton, Franklin C., Cook, Jacquelynn J., Krueger, Julie A., Kuo, Lawrence C., Lewis, S. Dale, Lucas, Bobby J., McMasters, Daniel R., Miller-Stein, Cynthia, Pietrak, Beth L., Wallace, Audrey A., White, Rebecca B., Wong, Bradley, Yan, Youwei, Nantermet, Philippe G.

Get full text

Design and Synthesis of a Series of Potent and Orally Bioavailable Noncovalent Thrombin Inhibitors That Utilize Nonbasic Groups in the P1 Position by Tucker, Thomas J, Brady, Stephen F, Lumma, William C, Lewis, S. Dale, Gardell, Stephen J, Naylor-Olsen, Adel M, Yan, Youwei, Sisko, Jack T, Stauffer, Kenneth J, Lucas, Bobby J, Lynch, Joseph J, Cook, Jacquelynn J, Stranieri, Maria T, Holahan, Marie A, Lyle, Elizabeth A, Baskin, Elizabeth P, Chen, I-Wu, Dancheck, Kimberly B, Krueger, Julie A, Cooper, Carolyn M, Vacca, Joseph P

“…As part of an ongoing effort to prepare therapeutically useful orally active thrombin inhibitors, we have synthesized a series of compounds that utilize…”
Get full text

Discovery and Development of the Novel Potent Orally Active Thrombin Inhibitor N-(9-Hydroxy-9-fluorenecarboxy)prolyl trans-4-Aminocyclohexylmethyl Amide (L-372,460):  Coapplication of Structure-Based Design and Rapid Multiple Analogue Synthesis on Solid Support by Brady, Stephen F, Stauffer, Kenneth J, Lumma, William C, Smith, Graham M, Ramjit, Harri G, Lewis, S. Dale, Lucas, Bobby J, Gardell, Steven J, Lyle, Elizabeth A, Appleby, Sandra D, Cook, Jacquelynn J, Holahan, Marie A, Stranieri, Maria T, Lynch, Joseph J, Lin, Jiunn H, Chen, I.-Wu, Vastag, Kari, Naylor-Olsen, Adel M, Vacca, Joseph P

“…Early studies in these laboratories of peptidomimetic structures containing a basic P1 moiety led to the highly potent and selective thrombin inhibitors 2 (K i…”
Get full text

Nonpeptide oxytocin antagonists: Analogs of L-371,257 with improved potency by Williams, Peter D., Bock, Mark G., Evans, Ben E., Freidinger, Roger M., Gallicchio, Steven N., Guidotti, Maribeth T., Jacobson, Marlene A., Kuo, Michelle S., Levy, Michelle R., Lis, Edward V., Michelson, Stuart R., Pawluczyk, Joseph M., Perlow, Debra S., Pettibone, Douglas J., Quigley, Amy G., Reiss, Duane R., Salvatore, Christopher, Stauffer, Kenneth J., Woyden, Carla J.

“…Structure-activity studies on the oxytocin antagonist 1 (L-371,257; K i = 9.3 nM) have led to the identification of a related series of compounds containing an…”
Get full text

Amide and α-keto carbonyl inhibitors of thrombin based on arginine and lysine: Synthesis, stability and biological characterization by Brady, Stephen F., Sisko, John T., Stauffer, Kenneth J., Colton, Christiana D., Qiu, Howard, Lewis, Sidney D., Ng, Assunta S., Shafer, Jules A., Bogusky, Michael J., Veber, Daniel F., Nutt, Ruth F.

“…We report structure-activity investigations in a series of tripeptide amide inhibitors of thrombin, and the development of a series of highly potent active…”
Get full text

Inhibition of thrombin by peptides containing Lysyl-alpha-keto carbonyl derivatives by Lewis, S D, Ng, A S, Lyle, E A, Mellott, M J, Appleby, S D, Brady, S F, Stauffer, K J, Sisko, J T, Mao, S S, Veber, D F

“…Several H-N-Me-D-Phe-Pro-Lysyl-alpha-keto carbonyl derivatives were shown to be potent thrombin inhibitors (Ki 0.2 to 27 nM). The inhibitory potencies of these…”
Get more information

Specific N-methylations of HPV-16 E7 peptides alter binding to the retinoblastoma suppressor protein by Jones, R E, Heimbrook, D C, Huber, H E, Wegrzyn, R J, Rotberg, N S, Stauffer, K J, Lumma, P K, Garsky, V M, Oliff, A

“…Complex formation between the human papilloma virus type 16 E7 protein (HPV-16 E7) and the retinoblastoma growth suppressor protein (RB) is believed to…”
Get full text