Search Results - "Kraus, Kenneth G"

3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization by Duplantier, Allen J., Efremov, Ivan, Candler, John, Doran, Angela C., Ganong, Alan H., Haas, Jessica A., Hanks, Ashley N., Kraus, Kenneth G., Lazzaro, John T., Lu, Jiemin, Maklad, Noha, McCarthy, Sheryl A., O’Sullivan, Theresa J., Rogers, Bruce N., Siuciak, Judith A., Spracklin, Douglas K., Zhang, Lei

“…The discovery, synthesis and SAR of a novel series of 3-benzyl-1,3-oxazolidin-2-ones as positive allosteric modulators (PAMs) of mGluR2 is described which led…”
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SAR of a Series of 5,6-Dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-α]pyridines as Potent Inhibitors of Human Eosinophil Phosphodiesterase by Duplantier, Allen J., Bachert, Elizabeth L., Cheng, John B., Cohan, Victoria L., Jenkinson, Teresa H., Kraus, Kenneth G., McKechney, Michael W., Pillar, Joann D., Watson, John W.

“…The potency and physical properties of a previously reported 7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine series of human eosinophil phosphodiesterase…”
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Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X₇ receptor antagonists leading to the discovery of the clinical candidate CE-224,535 by Duplantier, Allen J, Dombroski, Mark A, Subramanyam, Chakrapani, Beaulieu, Aimee M, Chang, Shang-Poa, Gabel, Christopher A, Jordan, Crystal, Kalgutkar, Amit S, Kraus, Kenneth G, Labasi, Jeff M, Mussari, Christopher, Perregaux, David G, Shepard, Rick, Taylor, Timothy J, Trevena, Kristen A, Whitney-Pickett, Carrie, Yoon, Kwansik

“…High throughput screening (HTS) of our compound file provided an attractive lead compound with modest P2X₇ receptor antagonist potency and high selectivity…”
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Biarylcarboxylic Acids and -amides:  Inhibition of Phosphodiesterase Type IV versus [3H]Rolipram Binding Activity and Their Relationship to Emetic Behavior in the Ferret by Duplantier, Allen J, Biggers, Michael S, Chambers, Robert J, Cheng, John B, Cooper, Kelvin, Damon, David B, Eggler, James F, Kraus, Kenneth G, Marfat, Anthony, Masamune, Hiroko, Pillar, Joann S, Shirley, John T, Umland, John P, Watson, John W

“…In addition to having desirable inhibitory effects on inflammation, anaphylaxis, and smooth muscle contraction, PDE-IV inhibitors also produce undesirable side…”
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Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors by Rizzi, James P, Schnur, Rodney C, Hutson, Nancy J, Kraus, Kenneth G, Kelbaugh, Paul R

“…Sorbinil (1), a spirocyclic hydantoin, is a potent inhibitor of the enzyme aldose reductase. Simulation of the rigid spirocyclic ring orientation found in…”
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Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent α4β1 integrin antagonists by DUPLANTIER, Allen J, BECKIUS, Gretchen E, WHITNEY, Carrie A, MILICI, Anthony J, CHAMBERS, Robert J, CHUPAK, Louis S, JENKINSON, Teresa H, KLEIN, Anne S, KRAUS, Kenneth G, KUDLACZ, Elizabeth M, MCKECHNEY, Michael W, PETTERSSON, Martin

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Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X 7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535 by Duplantier, Allen J., Dombroski, Mark A., Subramanyam, Chakrapani, Beaulieu, Aimee M., Chang, Shang-Poa, Gabel, Christopher A., Jordan, Crystal, Kalgutkar, Amit S., Kraus, Kenneth G., Labasi, Jeff M., Mussari, Christopher, Perregaux, David G., Shepard, Rick, Taylor, Timothy J., Trevena, Kristen A., Whitney-Pickett, Carrie, Yoon, Kwansik

“…High throughput screening (HTS) of our compound file provided an attractive lead compound with modest P2X 7 receptor antagonist potency and high selectivity…”
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7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as Novel Inhibitors of Human Eosinophil Phosphodiesterase by Duplantier, Allen J, Andresen, Catharine J, Cheng, John B, Cohan, Victoria L, Decker, Christian, DiCapua, Frank M, Kraus, Kenneth G, Johnson, Kerry L, Turner, Claudia R, UmLand, John P, Watson, John W, Wester, Ronald T, Williams, Alison S, Williams, John A

“…High-throughput file screening against inhibition of human lung PDE4 led to the discovery of…”
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Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X sub(7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535) by Duplantier, Allen J, Dombroski, Mark A, Subramanyam, Chakrapani, Beaulieu, Aimee M, Chang, Shang-Poa, Gabel, Christopher A, Jordan, Crystal, Kalgutkar, Amit S, Kraus, Kenneth G, Labasi, Jeff M, Mussari, Christopher, Perregaux, David G, Shepard, Rick, Taylor, Timothy J, Trevena, Kristen A, Whitney-Pickett, Carrie, Yoon, Kwansik

“…High throughput screening (HTS) of our compound file provided an attractive lead compound with modest P2X sub(7 receptor antagonist potency and high…”
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Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent α 4β 1 integrin antagonists by Duplantier, Allen J, Beckius, Gretchen E, Chambers, Robert J, Chupak, Louis S, Jenkinson, Teresa H, Klein, Anne S, Kraus, Kenneth G, Kudlacz, Elizabeth M, McKechney, Michael W, Pettersson, Martin, Whitney, Carrie A, Milici, Anthony J

“…A series of isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives derived from LDV was found to be a potent antagonist of the α 4β 1 integrin. The…”
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Synthesis and in vitro profile of a novel series of catechol benzimidazoles. The discovery of potent, selective phosphodiesterase type IV inhibitors with greatly attenuated affinity for the [ 3H]rolipram binding site by Cheng, John B., Cooper, Kelvin, Duplantier, Allen J., Eggler, James F., Kraus, Kenneth G., Marshall, Sally C., Marfat, Anthony, Masamune, Hiroko, Shirley, John T., Tickner, Jeenene E., Umland, John P.

“…The synthesis and biological properties of a novel series of potent and selective phosphodiesterase type IV (PDE IV) inhibitors are described. These catechol…”
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7-Oxo-4,5,6,7-tetrahydro-1 H -pyrazolo[3,4- c ]pyridines as Novel Inhibitors of Human Eosinophil Phosphodiesterase by Duplantier, Allen J., Andresen, Catharine J., Cheng, John B., Cohan, Victoria L., Decker, Christian, DiCapua, Frank M., Kraus, Kenneth G., Johnson, Kerry L., Turner, Claudia R., UmLand, John P., Watson, John W., Wester, Ronald T., Williams, Alison S., Williams, John A.

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The rearrangement of 2-amino-5-benzoyloxazoles with dimethylamine by Walker, Frederick J., Kraus, Kenneth G.

“…The rearrangement of 2‐amino‐5‐phenacyloxazoles with dimethylamine is described. One such rearrangement provided an unexpected tricyclic product…”
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