Search Results - "MCFADYEN, Robert B"

Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064 by Akwabi-Ameyaw, Adwoa, Bass, Jonathan Y., Caldwell, Richard D., Caravella, Justin A., Chen, Lihong, Creech, Katrina L., Deaton, David N., Jones, Stacey A., Kaldor, Istvan, Liu, Yaping, Madauss, Kevin P., Marr, Harry B., McFadyen, Robert B., Miller, Aaron B., III, Frank Navas, Parks, Derek J., Spearing, Paul K., Todd, Dan, Williams, Shawn P., Wisely, G. Bruce

“…Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR…”
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Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene by Bass, Jonathan Y., Caravella, Justin A., Chen, Lihong, Creech, Katrina L., Deaton, David N., Madauss, Kevin P., Marr, Harry B., McFadyen, Robert B., Miller, Aaron B., Mills, Wendy Y., Navas, Frank, Parks, Derek J., Smalley, Terrence L., Spearing, Paul K., Todd, Dan, Williams, Shawn P., Wisely, G. Bruce

“…To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR…”
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FXR agonist activity of conformationally constrained analogs of GW 4064 by Akwabi-Ameyaw, Adwoa, Bass, Jonathan Y., Caldwell, Richard D., Caravella, Justin A., Chen, Lihong, Creech, Katrina L., Deaton, David N., Madauss, Kevin P., Marr, Harry B., McFadyen, Robert B., Miller, Aaron B., Navas, Frank, Parks, Derek J., Spearing, Paul K., Todd, Dan, Williams, Shawn P., Bruce Wisely, G.

“…Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either…”
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Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064 by Bass, Jonathan Y., Caldwell, Richard D., Caravella, Justin A., Chen, Lihong, Creech, Katrina L., Deaton, David N., Madauss, Kevin P., Marr, Harry B., McFadyen, Robert B., Miller, Aaron B., Parks, Derek J., Todd, Dan, Williams, Shawn P., Wisely, G. Bruce

“…Starting from the known FXR agonist GW 4064 1a, a series of alternately 3,5-substituted isoxazoles was prepared. Several of these analogs were potent full FXR…”
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Novel and potent cyclic cyanamide-based cathepsin K inhibitors by 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.

“…Starting from a PDE IV inhibitor hit derived from high throughput screening of the compound collection, a key pyrrolidine cyanamide pharmacophore was…”
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Acyclic cyanamide-based inhibitors of cathepsin K by Barrett, David G., Deaton, David N., Hassell, Anne M., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Payne, J. Alan, Shewchuk, Lisa M., Willard, Derril H., Wright, Lois L.

“…Conversion of the proline-derived cyanamide lead into an acyclic cyanamide capable of forming an additional hydrogen bond with cathepsin K resulted in a large…”
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Acyclic, orally bioavailable ketone-based cathepsin K inhibitors by 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.

“…Starting from a potent ketone-based inhibitor with poor drug properties, incorporation of P 2–P 3 elements from a ketoamide-based inhibitor led to the…”
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Design of small molecule ketoamide-based inhibitors of cathepsin K by Catalano, John G., Deaton, David N., Long, Stacey T., McFadyen, Robert B., Miller, Larry R., Payne, J.Alan, Wells-Knecht, Kevin J., Wright, Lois L.

“…A novel series of ketoamide-based inhibitors of cathepsin K has been identified. Modifications to P 2 and P 3 elements were crucial to enhancing inhibitory…”
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A structural screening approach to ketoamide-based inhibitors of cathepsin K by Barrett, David G., Catalano, John G., Deaton, David N., Long, Stacey T., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Wells-Knecht, Kevin J., Wright, Lois L.

“…Several novel ketoamide-based inhibitors of cathepsin K have been identified. Starting from a modestly potent inhibitor, structural screening of P 2 elements…”
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Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors? by Adkison, Kim K., Barrett, David G., Deaton, David N., Gampe, Robert T., Hassell, Anne M., Long, Stacey T., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Payne, J. Alan, Shewchuk, Lisa M., Wells-Knecht, Kevin J., Willard, Derril H., Wright, Lois L.

“…Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of…”
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P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K by 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

“…An orally bioavailable series of ketoamide-based cathepsin K inhibitors with good pharmacokinetic properties has been identified. Starting from a potent…”
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Exploration of the P1 SAR of aldehyde cathepsin K inhibitors by CATALANO, John G, DEATON, David N, FURFINE, Eric S, HASSELL, Annie M, MCFADYEN, Robert B, MILLER, Aaron B, MILLER, Larry R, SHEWCHUK, Lisa M, WILLARD, Derril H, WRIGHT, Lois L

“…The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a…”
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P 2–P 3 conformationally constrained ketoamide-based inhibitors of cathepsin K by Barrett, David G., Boncek, Virginia M., Catalano, John G., Deaton, David N., Hassell, Anne M., Jurgensen, Cynthia H., Long, Stacey T., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., 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.

“…An orally bioavailable series of ketoamide-based cathepsin K inhibitors with good pharmacokinetic properties has been identified. Starting from a potent…”
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Exploration of the P2–P3 SAR of aldehyde cathepsin K inhibitors by Boros, Eric E., Deaton, David N., Hassell, Anne M., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Paulick, Margot G., Shewchuk, Lisa M., Thompson, James B., Willard, Derril H., Wright, Lois L.

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Exploration of the P 1 SAR of aldehyde cathepsin K inhibitors by Catalano, John G., Deaton, David N., Furfine, Eric S., Hassell, Annie M., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Shewchuk, Lisa M., Willard, Derril H., Wright, Lois L.

“…The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S 1 subsite with a…”
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Exploration of the P 2–P 3 SAR of aldehyde cathepsin K inhibitors by Boros, Eric E., Deaton, David N., Hassell, Anne M., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Paulick, Margot G., Shewchuk, Lisa M., Thompson, James B., Willard, Derril H., Wright, Lois L.

“…The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S 2 and S 3 subsites…”
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Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors by BORES, Eric E, DEATON, David N, WRIGHT, Lois L, HASSELL, Anne M, MCFADYEN, Robert B, MILLER, Aaron B, MILLER, Larry R, PAULICK, Margot G, SHEWCHUK, Lisa M, THOMPSON, James B, WILLARD, Derril H

“…The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S2 and S3 subsites…”
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