Discovery of a Novel, Selective, and Orally Bioavailable Class of Thrombin Inhibitors Incorporating Aminopyridyl Moieties at the P1 Position
Feng, Dong-Mei, Gardell, Stephen J, Lewis, S. Dale, Bock, Mark G, Chen, Zhongguo, Freidinger, Roger M, Naylor-Olsen, Adel M, Ramjit, Harri G, Woltmann, Richard, Baskin, Elizabeth P, Lynch, Joseph J, Lucas, Robert, Shafer, Jules A, Dancheck, Kimberley B, Chen, I-Wu, Mao, Shi-Shan, Krueger, Julie A, Hare, Timothy R, Mulichak, Anne M, Vacca, Joseph P
Published in Journal of medicinal chemistry (07.11.1997)
Published in Journal of medicinal chemistry (07.11.1997)
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Pharmacokinetics and biodistribution of novel aptamer compositions
Healy, Judith M, Lewis, Scott D, Kurz, Markus, Boomer, Ryan M, Thompson, Kristin M, Wilson, Charles, McCauley, Thomas G
Published in Pharmaceutical research (01.12.2004)
Published in Pharmaceutical research (01.12.2004)
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Discovery and evaluation of potent P-1 aryl heterocycle-based thrombin inhibitors
Young, MB, Barrow, JC, Glass, KL, Lundell, GF, Newton, CL, Pellicore, JM, Rittle, KE, Selnick, HG, Stauffer, KJ, Vacca, JP, Williams, PD, Bohn, D, Clayton, FC, Cook, JJ, Krueger, JA, Kuo, LC, Lewis, SD, Lucas, BJ, McMasters, DR, Miller-Stein, C, Pietrak, BL, Wallace, AA, White, RB, Wong, B, Yan, YW, Nantermet, PG
Published in Journal of medicinal chemistry (03.06.2004)
Published in Journal of medicinal chemistry (03.06.2004)
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Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B-1 receptor antagonists
Wood, MR, Schirripa, KM, Kim, JJ, Wan, BL, Murphy, KL, Ransom, RW, Chang, RSL, Tang, CY, Prueksaritanont, T, Detwiler, TJ, Hettrick, LA, Landis, ER, Leonard, YM, Krueger, JA, Lewis, SD, Pettibone, DJ, Freidinger, RM, Bock, MG
Published in Journal of medicinal chemistry (23.02.2006)
Published in Journal of medicinal chemistry (23.02.2006)
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Pharmacologic and Pharmacokinetic Assessment of Anti-TGF beta 2 Aptamers in Rabbit Plasma and Aqueous Humor
McCauley, Thomas G, Kurz, Jeffrey C, Merlino, Patricia G, Lewis, Scott D, Gilbert, Madaline, Epstein, David M, Marsh, HNicholas
Published in Pharmaceutical research (01.02.2006)
Published in Pharmaceutical research (01.02.2006)
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Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization
Deng, James Z., McMasters, Daniel R., Rabbat, Philippe M.A., Williams, Peter D., Coburn, Craig A., Yan, Youwei, Kuo, Lawrence C., Lewis, S. Dale, Lucas, Bobby J., Krueger, Julie A., Strulovici, Berta, Vacca, Joseph P., Lyle, Terry A., Burgey, Christopher S.
Published in Bioorganic & medicinal chemistry letters (15.10.2005)
Published in Bioorganic & medicinal chemistry letters (15.10.2005)
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9-Hydroxyazafluorenes and Their Use in Thrombin Inhibitors
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
Published in Journal of medicinal chemistry (07.04.2005)
Published in Journal of medicinal chemistry (07.04.2005)
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Journal Article
Design and Synthesis of a Series of Potent and Orally Bioavailable Noncovalent Thrombin Inhibitors That Utilize Nonbasic Groups in the P1 Position
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
Published in Journal of medicinal chemistry (13.08.1998)
Published in Journal of medicinal chemistry (13.08.1998)
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Journal Article
Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 1: Weakly basic azoles
Isaacs, Richard C.A., Solinsky, Mark G., Cutrona, Kellie J., Newton, Christina L., Naylor-Olsen, Adel M., Krueger, Julie A., Lewis, S. Dale, Lucas, Bobby J.
Published in Bioorganic & medicinal chemistry letters (15.01.2006)
Published in Bioorganic & medicinal chemistry letters (15.01.2006)
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Journal Article
Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the ‘Distal binding pocket’
Sanderson, Philip E.J., Cutrona, Kellie J., Dyer, Dona L., Krueger, Julie A., Kuo, Lawrence C., Lewis, S.Dale, Lucas, Bobby J., Yan, Youwei
Published in Bioorganic & medicinal chemistry letters (20.01.2003)
Published in Bioorganic & medicinal chemistry letters (20.01.2003)
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Journal Article
Design of Novel, Potent, Noncovalent Inhibitors of Thrombin with Nonbasic P-1 Substructures: Rapid Structure−Activity Studies by Solid-Phase Synthesis
Lumma, William C, Witherup, Keith M, Tucker, Thomas J, Brady, Steven F, Sisko, John T, Naylor-Olsen, Adel M, Lewis, S. Dale, Lucas, Bobby J, Vacca, Joseph P
Published in Journal of medicinal chemistry (26.03.1998)
Published in Journal of medicinal chemistry (26.03.1998)
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Journal Article
P 2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold
Nantermet, Philippe G., Burgey, Christopher S., Robinson, Kyle A., Pellicore, Janetta M., Newton, Christina L., Deng, James Z., Selnick, Harold G., Lewis, S. Dale, Lucas, Bobby J., Krueger, Julie A., Miller-Stein, Cynthia, White, Rebecca B., Wong, Bradley, McMasters, Daniel R., Wallace, Audrey A., Lynch, Joseph J., Yan, Youwei, Chen, Zhongguo, Kuo, Lawrence, Gardell, Stephen J., Shafer, Jules A., Vacca, Joseph P., Lyle, Terry A.
Published in Bioorganic & medicinal chemistry letters (02.06.2005)
Published in Bioorganic & medicinal chemistry letters (02.06.2005)
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Journal Article
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position
RITTLE, Kenneth E, BARROW, James C, NANTERMET, Philippe G, NEWTON, Christina L, SANDERS, William M, YOUWEI YAN, VACCA, Joseph P, SELNICK, Harold G, CUTRONA, Kellie J, GLASS, Kristen L, KRUEGER, Julie A, KUO, Lawrence C, LEWIS, S. Dale, LUCAS, Bobby J, MCMASTERS, Daniel R, MORRISSETTE, Matthew M
Published in Bioorganic & medicinal chemistry letters (20.10.2003)
Published in Bioorganic & medicinal chemistry letters (20.10.2003)
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Journal Article
Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors
Sanderson, Philip E.J., Stanton, Matthew G., Dorsey, Bruce D., Lyle, Terry A., McDonough, Colleen, Sanders, William M., Savage, Kelly L., Naylor-Olsen, Adel M., Krueger, Julie A., Lewis, S.Dale, Lucas, Bobby J., Lynch, Joseph J., Yan, Youwei
Published in Bioorganic & medicinal chemistry letters (10.03.2003)
Published in Bioorganic & medicinal chemistry letters (10.03.2003)
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Journal Article
Design and synthesis of potent and selective macrocyclic thrombin inhibitors
Nantermet, Philippe G., Barrow, James C., Newton, Christina L., Pellicore, Janetta M., Young, MaryBeth, Lewis, S.Dale, Lucas, Bobby J., Krueger, Julie A., McMasters, Daniel R., Yan, Youwei, Kuo, Lawrence C., Vacca, Joseph P., Selnick, Harold G.
Published in Bioorganic & medicinal chemistry letters (18.08.2003)
Published in Bioorganic & medicinal chemistry letters (18.08.2003)
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Journal Article
Design of Highly Potent Noncovalent Thrombin Inhibitors That Utilize a Novel Lipophilic Binding Pocket in the Thrombin Active Site
Tucker, Thomas J, Lumma, William C, Mulichak, Anne M, Chen, Zhongguo, Naylor-Olsen, Adel M, Lewis, S. Dale, Lucas, Robert, Freidinger, Roger M, Kuo, Lawrence C
Published in Journal of medicinal chemistry (14.03.1997)
Published in Journal of medicinal chemistry (14.03.1997)
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