Search Results - "Lefker, Bruce A"

Efficacy and Pharmacology of the NLRP3 Inflammasome Inhibitor CP-456,773 (CRID3) in Murine Models of Dermal and Pulmonary Inflammation by Primiano, Michael J, Lefker, Bruce A, Bowman, Michael R, Bree, Andrea G, Hubeau, Cedric, Bonin, Paul D, Mangan, Matthew, Dower, Ken, Monks, Brian G, Cushing, Leah, Wang, Stephen, Guzova, Julia, Jiao, Aiping, Lin, Lih-Ling, Latz, Eicke, Hepworth, David, Hall, J Perry

“…A critical component of innate immune response to infection and tissue damage is the NACHT, LRR, and PYD domains-containing protein 3 (NLRP3) inflammasome, and…”
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Activation of the G-Protein-Coupled Receptor 119: A Conformation-Based Hypothesis for Understanding Agonist Response by McClure, Kim F, Darout, Etzer, Guimarães, Cristiano R. W, DeNinno, Michael P, Mascitti, Vincent, Munchhof, Michael J, Robinson, Ralph P, Kohrt, Jeffrey, Harris, Anthony R, Moore, Dianna E, Li, Bryan, Samp, Lacey, Lefker, Bruce A, Futatsugi, Kentaro, Kung, Daniel, Bonin, Paul D, Cornelius, Peter, Wang, Ruduan, Salter, Eben, Hornby, Sam, Kalgutkar, Amit S, Chen, Yue

“…The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is…”
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A Novel, Non‐Prostanoid EP2 Receptor‐Selective Prostaglandin E2 Agonist Stimulates Local Bone Formation and Enhances Fracture Healing by LI, Mei, KE, Hua Zhu, QI, Hong, Healy, David R, LI, Yan, Crawford, D Todd, Paralkar, Vishwas M, Owen, Thomas A, Cameron, Kimberly O, Lefker, Bruce A, Brown, Thomas A, Thompson, David D

“…CP‐533,536, a newly discovered, non‐prostanoid EP2 receptor‐selective PGE2 agonist, stimulates local bone formation and enhances fracture healing in rat…”
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Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor by Mascitti, Vincent, Stevens, Benjamin D., Choi, Chulho, McClure, Kim F., Guimarães, Cristiano R.W., Farley, Kathleen A., Munchhof, Michael J., Robinson, Ralph P., Futatsugi, Kentaro, Lavergne, Sophie Y., Lefker, Bruce A., Cornelius, Peter, Bonin, Paul D., Kalgutkar, Amit S., Sharma, Raman, Chen, Yue

“…The design and synthesis of a GPR119 agonist bearing a 2-(2,3,6-trifluorophenyl)acetamide group is described. The design capitalized on the conformational…”
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A Nonprostanoid EP4 Receptor Selective Prostaglandin E2 Agonist Restores Bone Mass and Strength in Aged, Ovariectomized Rats by Ke, Hua Zhu, Crawford, D Todd, Qi, Hong, Simmons, Hollis A, Owen, Thomas A, Paralkar, Vishwas M, Li, Mei, Lu, Bihong, Grasser, William A, Cameron, Kimberly O, Lefker, Bruce A, DaSilva‐Jardine, Paul, Scott, Dennis O, Zhang, Qing, Tian, Xiao Yan, Jee, Webster SS, Brown, Thomas A, Thompson, David D

“…CP432 is a newly discovered, nonprostanoid EP4 receptor selective prostaglandin E2 agonist. CP432 stimulates trabecular and cortical bone formation and…”
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Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications by Li, Jie Jack, Iula, Donna M, Nguyen, Maria N, Hu, Lain-Yen, Dettling, Danielle, Johnson, Theodore R, Du, Daniel Y, Shanmugasundaram, Veerabahu, Van Camp, Jennifer A, Wang, Zhi, Harter, William G, Yue, Wen-Song, Boys, Mark L, Wade, Kimberly J, Drummond, Elena M, Samas, Brian M, Lefker, Bruce A, Hoge, Garrett S, Lovdahl, Mark J, Asbill, Jeffrey, Carroll, Matthew, Meade, Mary Ann, Ciotti, Susan M, Krieger-Burke, Theresa

“…4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile [PF-0998425, (−)-6a] is a novel, nonsteroidal androgen receptor antagonist for sebum control and…”
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Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging by Liang, Steven H., Chen, Jinshan Michael, Normandin, Marc D., Chang, Jeanne S., Chang, George C., Taylor, Christine K., Trapa, Patrick, Plummer, Mark S., Para, Kimberly S., Conn, Edward L., Lopresti-Morrow, Lori, Lanyon, Lorraine F., Cook, James M., Richter, Karl E. G., Nolan, Charlie E., Schachter, Joel B., Janat, Fouad, Che, Ye, Shanmugasundaram, Veerabahu, Lefker, Bruce A., Enerson, Bradley E., Livni, Elijahu, Wang, Lu, Guehl, Nicolas J., Patnaik, Debasis, Wagner, Florence F., Perlis, Roy, Holson, Edward B., Haggarty, Stephen J., El Fakhri, Georges, Kurumbail, Ravi G., Vasdev, Neil

“…Glycogen synthase kinase‐3 (GSK‐3) regulates multiple cellular processes in diabetes, oncology, and neurology…”
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Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis by Helal, Christopher J, Bundesmann, Mark, Hammond, Susan, Holmstrom, Melissa, Klug-McLeod, Jacquelyn, Lefker, Bruce A, McLeod, Dale, Subramanyam, Chakrapani, Zakaryants, Oleg, Sakata, Sylvie

“…Many pharmaceutical companies have invested millions of dollars in establishing internal chemical stores to provide reliable access to large numbers of…”
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Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists by Liu, Shenping, Dakin, Leslie A., Xing, Li, Withka, Jane M., Sahasrabudhe, Parag V., Li, Wei, Banker, Mary Ellen, Balbo, Paul, Shanker, Suman, Chrunyk, Boris A., Guo, Zuojun, Chen, Jinshan M., Young, Jennifer A., Bai, Guoyun, Starr, Jeremy T., Wright, Stephen W., Bussenius, Joerg, Tan, Sheng, Gopalsamy, Ariamala, Lefker, Bruce A., Vincent, Fabien, Jones, Lyn H., Xu, Hua, Hoth, Lise R., Geoghegan, Kieran F., Qiu, Xiayang, Bunnage, Mark E., Thorarensen, Atli

“…Interleukin-17A (IL-17A) is a principal driver of multiple inflammatory and immune disorders. Antibodies that neutralize IL-17A or its receptor (IL-17RA)…”
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Practical synthesis of capromorelin, a growth hormone secretagogue, via a crystallization-induced dynamic resolution by Rose, Colin R., Zawistoski, Michael P., Lefker, Bruce A., Mangano, F. Michael, Wright, Ann S., Carpino, Philip A.

“…[Display omitted] A practical synthesis of capromorelin (1), a growth hormone secretagogue, is described that utilizes as a key step a crystallization-induced…”
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From partial to full agonism: Identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor by Futatsugi, Kentaro, Mascitti, Vincent, Guimarães, Cristiano R.W., Morishita, Nao, Cai, Cuiman, DeNinno, Michael P., Gao, Hua, Hamilton, Michael D., Hank, Richard, Harris, Anthony R., Kung, Daniel W., Lavergne, Sophie Y., Lefker, Bruce A., Lopaze, Michael G., McClure, Kim F., Munchhof, Michael J., Preville, Cathy, Robinson, Ralph P., Wright, Stephen W., Bonin, Paul D., Cornelius, Peter, Chen, Yue, Kalgutkar, Amit S.

“…A novel GPR119 agonist based on the 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole scaffold was designed through lead optimization starting from pyrazole-based…”
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Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility by Kalgutkar, Amit S., Frederick, Kosea S., Hatch, Heather L., Ambler, Catherine M., Perry, David A., Garigipati, Ravi S., Chang, George C., Lefker, Bruce A., Clark, Ronald W., Morehouse, Lee A., Francone, Omar, Hu, Xiao

“…Abstract 1. Elaborate studies of cholesteryl ester transfer protein (CETP) polymorphisms and genetic deficiency in humans suggest direct links between CETP,…”
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Discovery of CP-533536 : An EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation by CAMERON, Kimberly O, LEFKER, Bruce A, LI YU, THOMPSON, David D, KE, Hua Z, MEI LI, ZAWISTOSKI, Michael P, TJOA, Christina M, WRIGHT, Ann S, DENINNO, Shari L, PARALKAR, Vishwas M, OWEN, Thomas A

“…Sulfonamides, exemplified by 3a, were identified as highly selective EP(2) agonists. Lead optimization led to the identification of CP-533536, 7f, a potent and…”
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Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity by Liu, Kevin K.-C., Lefker, Bruce A., Dombroski, Mark A., Chiang, Phoebe, Cornelius, Peter, Patterson, Terrell A., Zeng, Yuan, Santucci, Stephanie, Tomlinson, Elizabeth, Gibbons, Colleen P., Marala, Ravi, Brown, Janice A., Kong, Jimmy X., Lee, Eunsun, Werner, Wendy, Wenzel, Zane, Giragossian, Craig, Chen, Hou, Coffey, Steven B.

“…Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry…”
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Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging by Liang, Steven H., Chen, Jinshan Michael, Normandin, Marc D., Chang, Jeanne S., Chang, George C., Taylor, Christine K., Trapa, Patrick, Plummer, Mark S., Para, Kimberly S., Conn, Edward L., Lopresti-Morrow, Lori, Lanyon, Lorraine F., Cook, James M., Richter, Karl E. G., Nolan, Charlie E., Schachter, Joel B., Janat, Fouad, Che, Ye, Shanmugasundaram, Veerabahu, Lefker, Bruce A., Enerson, Bradley E., Livni, Elijahu, Wang, Lu, Guehl, Nicolas J., Patnaik, Debasis, Wagner, Florence F., Perlis, Roy, Holson, Edward B., Haggarty, Stephen J., El Fakhri, Georges, Kurumbail, Ravi G., Vasdev, Neil

“…Glycogen synthase kinase‐3 (GSK‐3) regulates multiple cellular processes in diabetes, oncology, and neurology…”
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Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists by Chesworth, Richard, Zawistoski, Michael P., Lefker, Bruce A., Cameron, Kimberly O., Day, Robert F., Mangano, F.Michael, Rosati, Robert L., Colella, Stacy, Petersen, Donna N., Brault, Amy, Lu, Bihong, Pan, Lydia C., Perry, Pia, Ng, Oicheng, Castleberry, Tessa A., Owen, Thomas A., Brown, Thomas A., Thompson, David D., DaSilva-Jardine, Paul

“…Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER α…”
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Stereoselective Alkylations in Rigid Systems. Effect of Remote Substituents on π-Facial Additions to Lactam Enolates. Stereoelectronic and Steric Effects by Meyers, A. I, Seefeld, Mark A, Lefker, Bruce A, Blake, James F, Williard, Paul G

“…A series of chiral bicyclic lactams has been studied by both experiment and ab initio molecular orbital calculations. The facial selectivity of the alkylation…”
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Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats by Cameron, Kimberly O., Lefker, Bruce A., Chu-Moyer, Margaret Y., Crawford, David T., Jardine, Paul DaSilva, DeNinno, Shari L., Gilbert, Sandra, Grasser, William A., Ke, HuaZhu, Lu, Bihong, Owen, Thomas A., Paralkar, Vishwas M., Qi, Hong, Scott, Dennis O., Thompson, David D., Tjoa, Christina M., Zawistoski, Michael P.

“…We describe the synthesis, SAR, and in vivo efficacy of a series of EP4-selective lactam derivatives. Heptanoic acid lactams, exemplified by 2, were identified…”
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Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs): Discovery of capromorelin by Carpino, Philip A, Lefker, Bruce A, Toler, Steven M, Pan, Lydia C, Hadcock, John R, Cook, Ewell R, DiBrino, Joseph N, Campeta, Anthony M, DeNinno, Shari L, Chidsey-Frink, Kristin L, Hada, William A, Inthavongsay, John, Mangano, F.Michael, Mullins, Michelle A, Nickerson, David F, Ng, Oicheng, Pirie, Christine M, Ragan, John A, Rose, Colin R, Tess, David A, Wright, Ann S, Yu, Li, Zawistoski, Michael P, DaSilva-Jardine, Paul A, Wilson, Theresa C, Thompson, David D

“…Novel pyrazolinone-piperidine dipeptide derivatives were synthesized and evaluated as growth hormone secretagogues (GHSs). Two analogues, capromorelin ( 5,…”
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Chiral bicyclic lactams for asymmetric synthesis of quaternary carbons. The total synthesis of (-)-.alpha.-cuparenone by Meyers, A. I, Lefker, Bruce A

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