Search Results - "Dombroski, Mark A"

Identification and characterization of a novel class of interleukin-1 post-translational processing inhibitors by Perregaux, D G, McNiff, P, Laliberte, R, Hawryluk, N, Peurano, H, Stam, E, Eggler, J, Griffiths, R, Dombroski, M A, Gabel, C A

“…Lipopolysaccharide (LPS)-activated monocytes and macrophages produce large quantities of pro-interleukin (IL)-1beta but externalize little mature cytokine…”
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Manganese(III)-based oxidative free-radical cyclization of unsaturated .beta.-keto esters, 1,3-diketones, and malonate diesters by Kates, Steven A, Dombroski, Mark A, Snider, Barry B

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Manganese(III)-based oxidative free-radical tandem and triple cyclizations by Dombroski, Mark A, Kates, Steven A, Snider, Barry B

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Theoretical and Experimental Design of Atypical Kinase Inhibitors:  Application to p38 MAP Kinase by McClure, Kim F, Abramov, Yuriy A, Laird, Ellen R, Barberia, John T, Cai, Weiling, Carty, Thomas J, Cortina, Santo R, Danley, Dennis E, Dipesa, Alan J, Donahue, Kathleen M, Dombroski, Mark A, Elliott, Nancy C, Gabel, Christopher A, Han, Seungil, Hynes, Thomas R, LeMotte, Peter K, Mansour, Mahmoud N, Marr, Eric S, Letavic, Michael A, Pandit, Jayvardhan, Ripin, David B, Sweeney, Francis J, Tan, Douglas, Tao, Yong

“…Mimics of the benzimidazolone nucleus found in inhibitors of p38 kinase are proposed, and their theoretical potential as bioisosteres is described. A set of…”
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Solvent effects on manganese(III)-based oxidative free-radical cyclizations: ethanol and acetic acid by Snider, Barry B, Merritt, John E, Dombroski, Mark A, Buckman, Brad O

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Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X7 receptor by Subramanyam, Chakrapani, Duplantier, Allen J., Dombroski, Mark A., Chang, Shang-Poa, Gabel, Christopher A., Whitney-Pickett, Carrie, Perregaux, David G., Labasi, Jeff M., Yoon, Kwansik, Shepard, Richard M., Fisher, Michael

“…The discovery, of a series of 2-Cl-5-heteroaryl-benzamide antagonists of the P2X7 receptor via parallel medicinal chemistry is described. Initial analogs…”
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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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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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Manganese(III)-based oxidative free radical cyclizations. 5. Termination of polycyclization by oxidative .beta.-hydride elimination by Snider, Barry B, Dombroski, Mark A

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Structure–activity relationships of triazolopyridine oxazole p38 inhibitors: Identification of candidates for clinical development by McClure, Kim F., Letavic, Michael A., Kalgutkar, Amit S., Gabel, Christopher A., Audoly, Laurent, Barberia, John T., Braganza, John F., Carter, Demetrius, Carty, Thomas J., Cortina, Santo R., Dombroski, Mark A., Donahue, Kathleen M., Elliott, Nancy C., Gibbons, Colleen P., Jordan, Crystal K., Kuperman, Alexander V., Labasi, Jeff M., LaLiberte, Ronald E., McCoy, Jennifer M., Naiman, Brian M., Nelson, Kendra L., Nguyen, Hang T., Peese, Kevin M., Sweeney, Francis J., Taylor, Timothy J., Trebino, Catherine E., Abramov, Yuriy A., Laird, Ellen R., Volberg, Walter A., Zhou, Jun, Bach, Justin, Lombardo, Franco

“…The synthesis, structure–activity relationship, in vivo activity, and metabolic profile for a series of triazolopyridine-oxazole based p38 inhibitors are…”
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Control of the regioselectivity of oxidative free-radical cyclizations by addition to haloalkenes by Snider, Barry B, Zhang, Qingwei, Dombroski, Mark A

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Benzimidazolone p38 inhibitors by DOMBROSKI, Mark A, LETAVIC, Michael A, JORDAN, Crystal K, LABASI, Jeff M, MARTIN, William H, PEESE, Kevin M, STOCK, Ingrid A, SVENSSON, Linne, SWEENEY, Francis J, YU, Chul H, MCCLURE, Kim F, BARBERIA, John T, CARTY, Thomas J, CORTINA, Santo R, CSIKI, Csilla, DIPESA, Alan J, ELLIOTT, Nancy C, GABEL, Christopher A

“…The synthesis and in vitro p38 alpha activity of a novel series of benzimidazolone inhibitors is described. The p38 alpha SAR is consistent with a mode of…”
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Cyclizations of unsaturated .bul.CR(COX)2 radicals. Manganese(III) acetate oxidative cyclizations of unsaturated acetoacetates and atom-transfer cyclizations of unsaturated haloacetoacetates give the same radicals by Curran, Dennis P, Morgan, Tina M, Schwartz, C. Eric, Snider, Barry B, Dombroski, Mark A

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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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Glutathione S-Transferase Omega 1-1 Is a Target of Cytokine Release Inhibitory Drugs and May Be Responsible for Their Effect on Interleukin-1 beta Posttranslational Processing by Laliberte, R E, Perregaux, D G, Hoth, L R, Rosner, P J, Jordan, C K, Peese, K M, Eggler, J, Dombroski, MA, Geoghegan, K F, Gabel, CA

“…Stimulus-induced posttranslational processing of human monocyte interleukin-1 beta (IL-1 beta ) is accompanied by major changes to the intracellular ionic…”
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Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X sub(7 receptor) by Subramanyam, Chakrapani, Duplantier, Allen J, Dombroski, Mark A, Chang, Shang-Poa, Gabel, Christopher A, Whitney-Pickett, Carrie, Perregaux, David G, Labasi, Jeff M, Yoon, Kwansik, Shepard, Richard M, Fisher, Michael

“…The discovery, of a series of 2-Cl-5-heteroaryl-benzamide antagonists of the P2X sub(7 receptor via parallel medicinal chemistry is described. Initial analogs…”
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Dichloroethylaluminum-catalyzed reactions of alkenes with electrophilic cyclopropanes. A new cyclopentane annelation reaction by Beal, Richard B, Dombroski, Mark A, Snider, Barry B

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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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Proton catalyzed cis-trans stereomutation of cis-1,2-diarylcyclobutanes by Flippin, Lee A, Dombroski, Mark A

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Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38α inhibitor: identification of an active metabolite in preclinical species and human liver microsomes by Kalgutkar, Amit S., Hatch, Heather L., Kosea, Frederick, Nguyen, Hang T., Choo, Edna F., McClure, Kim F., Taylor, Timothy J., Henne, Kirk R., Kuperman, Alexander V., Dombroski, Mark A., Letavic, Michael A.

“…The disposition of 6‐(4‐(2,5‐difluorophenyl)oxazol‐5‐yl)‐3‐isopropyl‐[1,2,4]‐triazolo[4,3‐a]pyridine (1), a potent and selective inhibitor of mitogen activated…”
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