Search Results - "LIANG, Jimmy"

Convergent Synthesis of a 5HT7/5HT2 Dual Antagonist by Liang, Jimmy T, Deng, Xiaohu, Mani, Neelakandha S

“…The development of an efficient and convergent route to 3-(4-fluorophenyl)-2-isopropyl-2,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepine (1), a potent 5HT7/5HT2 dual…”
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Practical Synthesis of a Cathepsin S Inhibitor: Route Identification, Purification Strategies, and Serendipitous Discovery of a Crystalline Salt Form by Deng, Xiaohu, Liang, Jimmy T, Peterson, Matthew, Rynberg, Raymond, Cheung, Eugene, Mani, Neelakandha S

“…A “redox economical” strategy resulted in a concise, modular synthesis of compound 1, a potent Cathepsin S inhibitor. Starting from three building blocks,…”
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Design of Concise, Scalable Route to a Cholecystokinin 1 (CCK 1) Receptor Antagonist by Liang, Jimmy T, Mani, Neelakandha S, Jones, Todd K

“…Development of efficient, scalable routes for the synthesis of (S)-3-[5-(3,4-dichlorophenyl)-1-(4-methoxyphenyl)-1H-pyrazol-3-yl]-2-m-tolyl propionic acid, a…”
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Identification of benzofuran central cores for the inhibition of leukotriene A4 hydrolase by Eccles, Wendy, Blevitt, Jonathan M., Booker, Jamila N., Chrovian, Christa C., Crawford, Shelby, de Leon, Aimee Rose, Deng, Xiaohu, Fourie, Anne M., Grice, Cheryl A., Herman, Krystal, Karlsson, Lars, Kearney, Aaron M., Lee-Dutra, Alice, Liang, Jimmy, Luna, Rosa, Pippel, Dan, Rao, Navin, Riley, Jason P., Santillán, Alejandro, Savall, Brad, Tanis, Virginia M., Xue, Xiaohua, Young, Arlene L.

“…Leukotrienes (LT’s) are known to play a physiological role in inflammatory immune response. Leukotriene A4 hydrolase (LTA4H) is a cystolic enzyme that…”
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A Practical Synthesis of Regioisomeric 6- and 7-Methoxytetrahydro-3-benzazepines by Liang, Jimmy T, Liu, Jing, Shireman, Brock T, Tran, Vi, Deng, Xiaohu, Mani, Neelakandha S

“…A concise and versatile synthetic route for 6- and 7-methoxy tetrahydro-3-benzazepines is described. The key feature of the synthesis is a one-pot…”
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Regioselective assembly of fused pyrazole-azepine heterocycles: Synthesis of the 5-HT7 antagonist 1-benzyl-3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepine by Dvorak, Curt A., Liang, Jimmy, Mani, Neelakandha S., Carruthers, Nicholas I.

“…[Display omitted] •Selective pyrazole construction.•Regioselective fused azepine-pyrazole assembly.•Pyrazole triflate coupling.•Selective Ring…”
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Selective Metalation of Functionalized Quinazolines to Enable Discovery and Advancement of Covalent KRAS Inhibitors by Allison, Brett D., Deng, Xiaohu, Li, Lian-Sheng, Liang, Jimmy, Mani, Neelakandha S., Ren, Pingda, Sales, Zachary S.

“…The quinazoline compound ARS-1620 is a recently discovered, mutant-specific covalent inhibitor of KRASG12C. Route scouting in support of multigram ARS-1620…”
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Regioselective Synthesis of 4-Nitro- or 4-Chloro-Tetrasubstituted Pyrazoles from Hydrazones and β-Halo-β-nitrostyrenes by Deng, Xiaohu, Liang, Jimmy T., Mani, Neelakandha S.

“…We report an acid‐catalyzed cycloaddition reaction of hydrazones with β‐bromo‐ or β‐chloro‐β‐nitrostyrenes for the regioselective synthesis of 4‐nitro‐ or…”
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4‑Methyl-6,7-dihydro‑4H‑triazolo[4,5‑c]­pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate by Letavic, Michael A, Savall, Brad M, Allison, Brett D, Aluisio, Leah, Andres, Jose Ignacio, De Angelis, Meri, Ao, Hong, Beauchamp, Derek A, Bonaventure, Pascal, Bryant, Stewart, Carruthers, Nicholas I, Ceusters, Marc, Coe, Kevin J, Dvorak, Curt A, Fraser, Ian C, Gelin, Christine F, Koudriakova, Tatiana, Liang, Jimmy, Lord, Brian, Lovenberg, Timothy W, Otieno, Monicah A, Schoetens, Freddy, Swanson, Devin M, Wang, Qi, Wickenden, Alan D, Bhattacharya, Anindya

“…The synthesis and preclinical characterization of novel 4-(R)-methyl-6,7-dihydro-4H-triazolo­[4,5-c]­pyridines that are potent and selective brain penetrant…”
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Allyl-Assisted, Cu(I)-Catalyzed Azide–Alkyne Cycloaddition/Allylation Reaction: Assembly of the [1,2,3]Triazolo-4,5,6,7-tetrahydropyridine Core Structure by Deng, Xiaohu, Liang, Jimmy, Allison, Brett B, Dvorak, Curt, McAllister, Heather, Savall, Brad M, Mani, Neelakandha S

“…We report a Cu­(I)-catalyzed azide–alkyne–allyl halide three-component reaction for a one-pot synthesis of 1,4-disubstituted 5-allyl-1,2,3-triazoles. The allyl…”
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Regioselective Synthesis of 4-Nitro- or 4-Chloro-Tetrasubstituted Pyrazoles from Hydrazones and [beta]-Halo-[beta]-nitrostyrenes by Deng, Xiaohu, Liang, Jimmy T, Mani, Neelakandha S

“…We report an acid-catalyzed cycloaddition reaction of hydrazones with [beta]-bromo- or [beta]-chloro-[beta]-nitrostyrenes for the regioselective synthesis of…”
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4-Methyl-6,7-dihydro-4 H -triazolo[4,5- c ]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate by Letavic, Michael A., Savall, Brad M., Allison, Brett D., Aluisio, Leah, Andres, Jose Ignacio, De Angelis, Meri, Ao, Hong, Beauchamp, Derek A., Bonaventure, Pascal, Bryant, Stewart, Carruthers, Nicholas I., Ceusters, Marc, Coe, Kevin J., Dvorak, Curt A., Fraser, Ian C., Gelin, Christine F., Koudriakova, Tatiana, Liang, Jimmy, Lord, Brian, Lovenberg, Timothy W., Otieno, Monicah A., Schoetens, Freddy, Swanson, Devin M., Wang, Qi, Wickenden, Alan D., Bhattacharya, Anindya

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Convergent Synthesis of a 5HT 7 /5HT 2 Dual Antagonist by Liang, Jimmy T., Deng, Xiaohu, Mani, Neelakandha S.

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A Practical Synthesis of Enantiopure 7-Alkoxy-4-aryl-tetrahydroisoquinoline, a Dual Serotonin Reuptake Inhibitor/Histamine H 3 Antagonist by Deng, Xiaohu, Liang, Jimmy T., Liu, Jing, McAllister, Heather, Schubert, Carsten, Mani, Neelakandha S.

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Identification of benzofuran central cores for the inhibition of leukotriene A(4) hydrolase by Eccles, Wendy, Blevitt, Jonathan M, Booker, Jamila N, Chrovian, Christa C, Crawford, Shelby, de Leon, Aimee Rose, Deng, Xiaohu, Fourie, Anne M, Grice, Cheryl A, Herman, Krystal, Karlsson, Lars, Kearney, Aaron M, Lee-Dutra, Alice, Liang, Jimmy, Luna, Rosa, Pippel, Dan, Rao, Navin, Riley, Jason P, Santillán, Alejandro, Savall, Brad, Tanis, Virginia M, Xue, Xiaohua, Young, Arlene L

“…Leukotrienes (LT's) are known to play a physiological role in inflammatory immune response. Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that…”
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Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: discovery of TR-14035, a dual alpha(4)beta(7)/alpha(4)beta(1) integrin antagonist by Sircar, Ila, Gudmundsson, Kristjan S, Martin, Richard, Liang, Jimmy, Nomura, Sumihiro, Jayakumar, Honnappa, Teegarden, Bradley R, Nowlin, Dawn M, Cardarelli, Pina M, Mah, Jason R, Connell, Samuel, Griffith, Ronald C, Lazarides, Elias

“…alpha(4)beta(1) and alpha(4)beta(7) integrins are key regulators of physiologic and pathologic responses in inflammation and autoimmune disease. The…”
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Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: Discovery of TR-14035, a dual α4β7/α4β1 integrin antagonist by SIRCAR, Ila, GUDMUNDSSON, Kristjan S, CONNELL, Samuel, GRIFFITH, Ronald C, LAZARIDES, Elias, MARTIN, Richard, LIANG, Jimmy, NOMURA, Sumihiro, JAYAKUMAR, Honnappa, TEEGARDEN, Bradley R, NOWLIN, Dawn M, CARDARELLI, Pina M, MAH, Jason R

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Novel Stereoselective Syntheses of the Fused Benzazepine Dopamine D1 Antagonist (6aS,13b R)-11-Chloro-6,6a,7,8,9,13b-hexahydro-7-methyl- 5H-benzo[d]naphth[2,1-b]azepin-12-ol (Sch 39166):  2. l-Homophenylalanine-Based Syntheses by Draper, Richard W, Hou, Donald, Iyer, Radha, Lee, Gary M, Liang, Jimmy T, Mas, Janet L, Vater, Eugene J

“…Two enantioselective syntheses of the fused benzazepine dopamine D1 antagonist…”
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Synthesis and SAR of N-Benzoyl- l-Biphenylalanine Derivatives: Discovery of TR-14035, A Dual α 4β 7/α 4β 1 Integrin Antagonist by Sircar, Ila, Gudmundsson, Kristjan S, Martin, Richard, Liang, Jimmy, Nomura, Sumihiro, Jayakumar, Honnappa, Teegarden, Bradley R, Nowlin, Dawn M, Cardarelli, Pina M, Mah, Jason R, Connell, Samuel, Griffith, Ronald C, Lazarides, Elias

“…α 4β 1 and α 4β 7 integrins are key regulators of physiologic and pathologic responses in inflammation and autoimmune disease. The effectiveness of…”
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Novel Stereoselective Syntheses of the Fused Benzazepine Dopamine D1 Antagonist (6aS,13bR)-11-Chloro-6,6a,7,8,9,13b-hexahydro-7-methyl-5H- benzo[d]naphth[2,1-b]azepin-12-ol (Sch 39166):  1. Aziridinium Salt Based Syntheses by Draper, Richard W, Hou, Donald, Iyer, Radha, Lee, Gary M, Liang, Jimmy T, Mas, Janet L, Tormos, Wanda, Vater, Eugene J, Günter, Frank, Mergelsberg, Ingrid, Scherer, Dominik

“…Several novel enantioselective syntheses of the dopamine D1 antagonist…”
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