Search Results - "Kohrt, Jeffrey"

Oxidative diversification of amino acids and peptides by small-molecule iron catalysis by Osberger, Thomas J., Rogness, Donald C., Kohrt, Jeffrey T., Stepan, Antonia F., White, M. Christina

“…Two small-molecule iron catalysts are shown to be capable of facilitating the targeted C–H oxidative modification of amino acids and peptides with preservation…”
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Late-stage oxidative C(sp3)–H methylation by Feng, Kaibo, Quevedo, Raundi E., Kohrt, Jeffrey T., Oderinde, Martins S., Reilly, Usa, White, M. Christina

“…Frequently referred to as the ‘magic methyl effect’, the installation of methyl groups—especially adjacent (α) to heteroatoms—has been shown to dramatically…”
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Enantioselective Single and Dual α‑C–H Bond Functionalization of Cyclic Amines via Enzymatic Carbene Transfer by Ren, Xinkun, Couture, Bo M., Liu, Ningyu, Lall, Manjinder S., Kohrt, Jeffrey T., Fasan, Rudi

“…Cyclic amines are ubiquitous structural motifs found in pharmaceuticals and biologically active natural products, making methods for their elaboration via…”
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Fluorodecarboxylation for the Synthesis of Trifluoromethyl Aryl Ethers by Zhang, Qing-Wei, Brusoe, Andrew T., Mascitti, Vincent, Hesp, Kevin D., Blakemore, David C., Kohrt, Jeffrey T., Hartwig, John F.

“…The synthesis of mono‐, di‐, and trifluoromethyl aryl ethers by fluorodecarboxylation of the corresponding carboxylic acids is reported. AgF2 induces…”
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Cell‐free in vitro reduction of carboxylates to aldehydes: With crude enzyme preparations to a key pharmaceutical building block by Schwarz, Anna, Hecko, Sebastian, Rudroff, Florian, Kohrt, Jeffrey T., Howard, Roger M., Winkler, Margit

“…The scarcity of practical methods for aldehyde synthesis in chemistry necessitates the development of mild, selective procedures. Carboxylic acid reductases…”
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Application of Flow and Biocatalytic Transaminase Technology for the Synthesis of a 1‑Oxa-8-azaspiro[4.5]decan-3-amine by Kohrt, Jeffrey T, Dorff, Peter H, Burns, Michael, Lee, Chewah, O’Neil, Steven V, Maguire, Robert J, Kumar, Rajesh, Wagenaar, Melissa, Price, Loren, Lall, Manjinder S

“…Spirocyclic ring systems are useful intermediates in the design and synthesis of medicinally active agents and commonly found as cores in natural products…”
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PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease by Gopalsamy, Ariamala, Aulabaugh, Ann E, Barakat, Amey, Beaumont, Kevin C, Cabral, Shawn, Canterbury, Daniel P, Casimiro-Garcia, Agustin, Chang, Jeanne S, Chen, Ming Z, Choi, Chulho, Dow, Robert L, Fadeyi, Olugbeminiyi O, Feng, Xidong, France, Scott P, Howard, Roger M, Janz, Jay M, Jasti, Jayasankar, Jasuja, Reema, Jones, Lyn H, King-Ahmad, Amanda, Knee, Kelly M, Kohrt, Jeffrey T, Limberakis, Chris, Liras, Spiros, Martinez, Carlos A, McClure, Kim F, Narayanan, Arjun, Narula, Jatin, Novak, Jonathan J, O'Connell, Thomas N, Parikh, Mihir D, Piotrowski, David W, Plotnikova, Olga, Robinson, Ralph P, Sahasrabudhe, Parag V, Sharma, Raman, Thuma, Benjamin A, Vasa, Dipy, Wei, Liuqing, Wenzel, A Zane, Withka, Jane M, Xiao, Jun, Yayla, Hatice G

“…Sickle cell disease (SCD) is a genetic disorder caused by a single point mutation (β6 Glu → Val) on the β-chain of adult hemoglobin (HbA) that results in…”
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Expedient synthesis of novel β-ketoesters from the Mizoroki–Heck coupling of ethyl 3-ethoxyacrylate with aryl and pyridyl halides by Kohrt, Jeffrey T., Conn, Ed, Maguire, Robert, Wright, Stephen W., Singer, Robert

“…It is well known that β-ketoesters are useful intermediates for the synthesis of a range of heterocyclic templates. While there are many useful synthetic…”
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Novel and selective spiroindoline-based inhibitors of sky kinase by Powell, Noel A., Kohrt, Jeffrey T., Filipski, Kevin J., Kaufman, Michael, Sheehan, Derek, Edmunds, Jeremy E., Delaney, Amy, Wang, Yuli, Bourbonais, Francis, Lee, Doh-Yeel, Schwende, Frank, Sun, Fang, McConnell, Pat, Catana, Cornel, Chen, Huifen, Ohren, Jeff, Perrin, Lisa A.

“…We report the discovery of a novel series of spiroindoline-based inhibitors of Sky kinase. Structure determination using X-ray crystallography clearly…”
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Synthesis of Spiropiperidine Lactam Acetyl-CoA Carboxylase Inhibitors by Huard, Kim, Bagley, Scott W, Menhaji-Klotz, Elnaz, Préville, Cathy, Southers, James A, Smith, Aaron C, Edmonds, David J, Lucas, John C, Dunn, Matthew F, Allanson, Nigel M, Blaney, Emma L, Garcia-Irizarry, Carmen N, Kohrt, Jeffrey T, Griffith, David A, Dow, Robert L

“…The synthesis of 4′,6′-dihydrospiro[piperidine-4,5′-pyrazolo[3,4-c]pyridin]-7′(2′H)-one-based acetyl-CoA carboxylase inhibitors is reported. The hitherto…”
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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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Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase by Powell, Noel A., Hoffman, Jennifer K., Ciske, Fred L., Kohrt, Jeffrey T., Baxi, Sangita M., Peng, Yun-Wen, Zhong, Min, Catana, Cornel, Ohren, Jeff, Perrin, Lisa A., Edmunds, Jeremy J.

“…Optimization of the ADME properties of a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase resulted in the identification of highly…”
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Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase by Powell, Noel A., Hoffman, Jennifer K., Ciske, Fred L., Kaufman, Michael D., Kohrt, Jeffrey T., Quin, John, Sheehan, Derek J., Delaney, Amy, Baxi, Sangita M., Catana, Cornel, McConnell, Patrick, Ohren, Jeff, Perrin, Lisa A., Edmunds, Jeremy J.

“…We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but…”
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Intrinsic Electrophilicity of a 4-Substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine Derivative: Structural Characterization of Glutathione Conjugates in Vitro by Kalgutkar, Amit S, Mascitti, Vincent, Sharma, Raman, Walker, Gregory W, Ryder, Tim, McDonald, Thomas S, Chen, Yue, Preville, Cathy, Basak, Arindrajit, McClure, Kim F, Kohrt, Jeffrey T, Robinson, Ralph P, Munchhof, Michael J, Cornelius, Peter

“…Isopropyl 9-anti-[5-cyano-6-(2-methyl-pyridin-3-yloxy)-pyrimidin-4-yloxy]-3-oxa-7-aza-bicyclo[3.3.1]nonane-7-carboxylate (1) represents a prototypic compound…”
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Fluorodecarboxylation for the Synthesis of Trifluoromethyl Aryl Ethers by Zhang, Qing-Wei, Brusoe, Andrew T., Mascitti, Vincent, Hesp, Kevin D., Blakemore, David C., Kohrt, Jeffrey T., Hartwig, John F.

“…The synthesis of mono‐, di‐, and trifluoromethyl aryl ethers by fluorodecarboxylation of the corresponding carboxylic acids is reported. AgF2 induces…”
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The Discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an Orally Efficacious Factor Xa Inhibitor by Kohrt, Jeffrey T., Bigge, Christopher F., Bryant, John W., Casimiro-Garcia, Agustin, Chi, Liguo, Cody, Wayne L., Dahring, Tawny, Dudley, Danette A., Filipski, Kevin J., Haarer, Staci, Heemstra, Ron, Janiczek, Nancy, Narasimhan, Lakshmi, McClanahan, Thomas, Peterson, J. Thomas, Sahasrabudhe, Vaisheli, Schaum, Robert, Van Huis, Chad A., Welch, Kathleen M., Zhang, Erli, Leadley, Robert J., Edmunds, Jeremy J.

“…Herein, we report the discovery of novel, proline‐based factor Xa inhibitors containing a neutral P1 chlorophenyl pharmacophore. Through the additional…”
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Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action by Van Huis, Chad A., Casimiro-Garcia, Agustin, Bigge, Christopher F., Cody, Wayne L., Dudley, Danette A., Filipski, Kevin J., Heemstra, Ronald J., Kohrt, Jeffrey T., Leadley, Robert J., Narasimhan, Lakshmi S., McClanahan, Thomas, Mochalkin, Igor, Pamment, Michael, Thomas Peterson, J., Sahasrabudhe, Vaishali, Schaum, Robert P., Edmunds, Jeremy J.

“…With the intent to improve upon the projected human half-life of the previously disclosed Factor Xa inhibitor 5, a series of 4,4-disubstituted…”
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Pyrazole inhibitors of HMG-CoA reductase: An attempt to dramatically reduce synthetic complexity through minimal analog re-design by Larsen, Scott D., Poel, Toni-Jo, Filipski, Kevin J., Kohrt, Jeffrey T., Pfefferkorn, Jeffrey A., Sorenson, Roderick J., Tait, Bradley D., Askew, Valerie, Dillon, Lisa, Hanselman, Jeffrey C., Lu, Gina H., Robertson, Andrew, Sekerke, Catherine, Kowala, Mark C., Auerbach, Bruce J.

“…A highly effective new series of pyrazole statins 3 was transformed by a single atom change to the oxypyrazoles 4, reducing a complex synthetic route from 14…”
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The discovery of glycine and related amino acid-based factor Xa inhibitors by Kohrt, Jeffrey T., Filipski, Kevin J., Cody, Wayne L., Bigge, Christopher F., La, Frances, Welch, Kathleen, Dahring, Tawny, Bryant, John W., Leonard, Daniele, Bolton, Gary, Narasimhan, Lakshmi, Zhang, Erli, Peterson, J. Thomas, Haarer, Staci, Sahasrabudhe, Vaishali, Janiczek, Nancy, Desiraju, Shrilakshmi, Hena, Mostofa, Fiakpui, Charles, Saraswat, Neerja, Sharma, Raman, Sun, Shaoyi, Maiti, Samarendra N., Leadley, Robert, Edmunds, Jeremy J.

“…Herein, we report on the identification of three potent glycine and related amino acid-based series of FXa inhibitors containing a neutral P1 chlorophenyl…”
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The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex—Part 2 by Kohrt, Jeffrey T., Filipski, Kevin J., Cody, Wayne L., Cai, Cuiman, Dudley, Danette A., Van Huis, Chad A., Willardsen, J. Adam, Narasimhan, Lakshmi S., Zhang, Erli, Rapundalo, Stephen T., Saiya-Cork, Kamlai, Leadley, Robert J., Edmunds, Jeremy J.

“…The activated factor VII/tissue factor complex (FVIIa/TF) is known to play a key role in the formation of blood clots. Inhibition of this complex may lead to…”
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