Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression von Bisi, John E, Sorrentino, Jessica A, Roberts, Patrick J, Tavares, Francis X, Strum, Jay C

Volltext

Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors von Bisi, John E, Sorrentino, Jessica A, Jordan, Jamie L, Darr, David D, Roberts, Patrick J, Tavares, Francis X, Strum, Jay C

Volltext

N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as Potent and Selective Inhibitors of Glycogen Synthase Kinase 3 with Good Cellular Efficacy von Tavares, Francis X, Boucheron, Joyce A, Dickerson, Scott H, Griffin, Robert J, Preugschat, Frank, Thomson, Stephen A, Wang, Tony Y, Zhou, Hui-Qiang

Volltext

Oxidation of Oxazolines and Thiazolines to Oxazoles and Thiazoles. Application of the Kharasch−Sosnovsky Reaction von Meyers, A. I, Tavares, Francis X

Volltext

Potent, Selective, and Orally Efficacious Antagonists of Melanin-Concentrating Hormone Receptor 1 von Tavares, Francis X, Al-Barazanji, Kamal A, Bigham, Eric C, Bishop, Michael J, Britt, Christy S, Carlton, David L, Feldman, Paul L, Goetz, Aaron S, Grizzle, Mary K, Guo, Yu C, Handlon, Anthony L, Hertzog, Donald L, Ignar, Diane M, Lang, Daniel G, Ott, Ronda J, Peat, Andrew J, Zhou, Hui-Qiang

Volltext

Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo... von Thomson, Stephen A., Banker, Pierette, Bickett, D. Mark, Boucheron, Joyce A., Carter, H. Luke, Clancy, Daphne C., Cooper, Joel P., Dickerson, Scott H., Garrido, Dulce M., Nolte, Robert T., Peat, Andrew J., Sheckler, Lauren R., Sparks, Steven M., Tavares, Francis X., Wang, Liping, Wang, Tony Y., Weiel, James E.

Volltext

The discovery and optimization of pyrimidinone-containing MCH R1 antagonists von Hertzog, Donald L., Al-Barazanji, Kamal A., Bigham, Eric C., Bishop, Michael J., Britt, Christy S., Carlton, David L., Cooper, Joel P., Daniels, Alex J., Garrido, Dulce M., Goetz, Aaron S., Grizzle, Mary K., Guo, Yu C., Handlon, Anthony L., Ignar, Diane M., Morgan, Ronda O., Peat, Andrew J., Tavares, Francis X., Zhou, Huiqiang

Volltext

Ketoamide-Based Inhibitors of Cysteine Protease, Cathepsin K:  P3 Modifications von Tavares, Francis X, Deaton, David N, Miller, Larry R, Wright, Lois L

Volltext

Design of Potent, Selective, and Orally Bioavailable Inhibitors of Cysteine Protease Cathepsin K von Tavares, Francis X, Boncek, Virginia, Deaton, David N, Hassell, Anne M, Long, Stacey T, Miller, Aaron B, Payne, Alan A, Miller, Larry R, Shewchuk, Lisa M, Wells-Knecht, Kevin, Willard, Derril H, Wright, Lois L, Zhou, Hui-Qiang

Volltext

Structure-activity relationships and cellular mechanism of action of small molecules that enhance the delivery of oligonucleotides von Juliano, Rudolph L, Wang, Ling, Tavares, Francis, Brown, Edward G, James, Lindsey, Ariyarathna, Yamuna, Ming, Xin, Mao, Chengqiong, Suto, Mark

Volltext

Novel and potent cyclic cyanamide-based cathepsin K inhibitors von Deaton, David N., Hassell, Anne M., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Shewchuk, Lisa M., Tavares, Francis X., Willard, Derril H., Wright, Lois L.

Volltext

Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of Type 2 diabetes: 2. Optimization of serine and threonine ether amino acid residues von Sparks, Steven M., Banker, Pierette, Bickett, David M., Clancy, Daphne C., Dickerson, Scott H., Garrido, Dulce M., Golden, Pamela L., Peat, Andrew J., Sheckler, Lauren R., Tavares, Francis X., Thomson, Stephen A., Weiel, James E.

Volltext

6-(4-Chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-Based Melanin-Concentrating Hormone Receptor 1 Antagonist von Tavares, Francis X, Al-Barazanji, Kamal A, Bishop, Michael J, Britt, Christy S, Carlton, David L, Cooper, Joel P, Feldman, Paul L, Garrido, Dulce M, Goetz, Aaron S, Grizzle, Mary K, Hertzog, Donald L, Ignar, Diane M, Lang, Daniel G, McIntyre, Maggie S, Ott, Ronda J, Peat, Andrew J, Zhou, Hui-Qiang

Volltext

Potent and Selective Ketoamide-Based Inhibitors of Cysteine Protease, Cathepsin K von Tavares, Francis X, Deaton, David N, Miller, Aaron B, Miller, Larry R, Wright, Lois L, Zhou, Hui-Qiang

Volltext

Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes: 1. Identification of 1-amino-1-cycloalkyl carboxylic acid headgroups von Sparks, Steven M., Banker, Pierette, Bickett, David M., Carter, H. Luke, Clancy, Daphne C., Dickerson, Scott H., Dwornik, Kate A., Garrido, Dulce M., Golden, Pamela L., Nolte, Robert T., Peat, Andrew J., Sheckler, Lauren R., Tavares, Francis X., Thomson, Stephen A., Wang, Liping, Weiel, James E.

Volltext

Ketoheterocycle-based inhibitors of cathepsin K: A novel entry into the synthesis of peptidic ketoheterocycles von Tavares, Francis X., Deaton, David N., Miller, Aaron B., Miller, Larry R., Wright, Lois L.

Volltext

Acyclic, orally bioavailable ketone-based cathepsin K inhibitors von Barrett, David G., Catalano, John G., Deaton, David N., Long, Stacey T., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Samano, Vicente, Tavares, Francis X., Wells-Knecht, Kevin J., Wright, Lois L., Zhou, Hui-Qiang Q.

Volltext

Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K von Barrett, David G., Catalano, John G., Deaton, David N., Long, Stacey T., Miller, Larry R., Tavares, Francis X., Wells-Knecht, Kevin J., Wright, Lois L., Zhou, Hui-Qiang Q.

Volltext

The oxidation of 2-oxazolines to 1,3-oxazoles von Meyers, A.I., Tavares, Francis

Volltext

P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K von BARRETT, David G, BONCEK, Virginia M, PAYNE, J. Alan, RAY, John A, SAMANO, Vicente, SHEWCHUK, Lisa M, TAVARES, Francis X, WELLS-KNECHT, Kevin J, WILLARD, Derril H, WRIGHT, Lois L, ZHOU, Hui-Qiang Q, CATALANO, John G, DEATON, David N, HASSELL, Anne M, JURGENSEN, Cynthia H, LONG, Stacey T, MCFADYEN, Robert B, MILLER, Aaron B, MILLER, Larry R

Volltext