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1
Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2S,3R)‑N‑((S)‑3-(Cyclopent-1-en-1-yl)-1-((R)‑2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)‑2-(2-morpholinoacetamido)­propanamido)­propenamide)
Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2S,3R)‑N‑((S)‑3-(Cyclopent-1-en-1-yl)-1-((R)‑2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)‑2-(2-morpholinoacetamido)­propanamido)­propenamide)
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Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2S,3R)‑N‑((S)‑3-(Cyclopent-1-en-1-yl)-1-((R)‑2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)‑2-(2-morpholinoacetamido)­propanamido)­propenamide)

Johnson, Henry W. B ; Lowe, Eric ; Anderl, Janet L ; Fan, Andrea ; Muchamuel, Tony ; Bowers, Simeon ; Moebius, David C ; Kirk, Christopher ; McMinn, Dustin L

Journal of medicinal chemistry, 2018-12, Vol.61 (24), p.11127-11143 [Periódico revisado por pares]

United States: American Chemical Society

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2
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4‑d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4‑d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family
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Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4‑d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family

Smaill, Jeff B ; Gonzales, Andrea J ; Spicer, Julie A ; Lee, Helen ; Reed, Jessica E ; Sexton, Karen ; Althaus, Irene W ; Zhu, Tong ; Black, Shannon L ; Blaser, Adrian ; Denny, William A ; Ellis, Paul A ; Fakhoury, Stephen ; Harvey, Patricia J ; Hook, Ken ; McCarthy, Florence O. J ; Palmer, Brian D ; Rivault, Freddy ; Schlosser, Kevin ; Ellis, Teresa ; Thompson, Andrew M ; Trachet, Erin ; Winters, R. Thomas ; Tecle, Haile ; Bridges, Alexander

Journal of medicinal chemistry, 2016-09, Vol.59 (17), p.8103-8124 [Periódico revisado por pares]

United States: American Chemical Society

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3
Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses
Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses
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Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses

Ivashchenko, Andrei A ; Mitkin, Oleg D ; Jones, Jeremy C ; Nikitin, Alexander V ; Koryakova, Angela G ; Ryakhovskiy, Alexey ; Karapetian, Ruben N ; Kravchenko, Dmitry V ; Aladinskiy, Vladimir ; Leneva, Irina A ; Falynskova, Irina N ; Glubokova, Ekaterina A ; Govorkova, Elena A ; Ivachtchenko, Alexandre V

Journal of medicinal chemistry, 2020-09, Vol.63 (17), p.9403-9420 [Periódico revisado por pares]

United States: American Chemical Society

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4
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models
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Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models

Lücking, Ulrich ; Wortmann, Lars ; Wengner, Antje M ; Lefranc, Julien ; Lienau, Philip ; Briem, Hans ; Siemeister, Gerhard ; Bömer, Ulf ; Denner, Karsten ; Schäfer, Martina ; Koppitz, Marcus ; Eis, Knut ; Bartels, Florian ; Bader, Benjamin ; Bone, Wilhelm ; Moosmayer, Dieter ; Holton, Simon J ; Eberspächer, Uwe ; Grudzinska-Goebel, Joanna ; Schatz, Christoph ; Deeg, Gesa ; Mumberg, Dominik ; von Nussbaum, Franz

Journal of medicinal chemistry, 2020-07, Vol.63 (13), p.7293-7325 [Periódico revisado por pares]

United States: American Chemical Society

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5
Discovery of Small-Molecule Inhibitors Selectively Targeting the DNA-Binding Domain of the Human Androgen Receptor
Discovery of Small-Molecule Inhibitors Selectively Targeting the DNA-Binding Domain of the Human Androgen Receptor
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Discovery of Small-Molecule Inhibitors Selectively Targeting the DNA-Binding Domain of the Human Androgen Receptor

Li, Huifang ; Ban, Fuqiang ; Dalal, Kush ; Leblanc, Eric ; Frewin, Kate ; Ma, Dennis ; Adomat, Hans ; Rennie, Paul S ; Cherkasov, Artem

Journal of medicinal chemistry, 2014-08, Vol.57 (15), p.6458-6467 [Periódico revisado por pares]

United States: American Chemical Society

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6
Development of the First Generation of Disulfide-Based Subtype-Selective and Potent Covalent Pyruvate Dehydrogenase Kinase 1 (PDK1) Inhibitors
Development of the First Generation of Disulfide-Based Subtype-Selective and Potent Covalent Pyruvate Dehydrogenase Kinase 1 (PDK1) Inhibitors
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Development of the First Generation of Disulfide-Based Subtype-Selective and Potent Covalent Pyruvate Dehydrogenase Kinase 1 (PDK1) Inhibitors

Liu, Yifu ; Xie, Zuoquan ; Zhao, Dan ; Zhu, Jin ; Mao, Fei ; Tang, Shuai ; Xu, Hui ; Luo, Cheng ; Geng, Meiyu ; Huang, Min ; Li, Jian

Journal of medicinal chemistry, 2017-03, Vol.60 (6), p.2227-2244 [Periódico revisado por pares]

United States: American Chemical Society

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7
An Optimized RAD51 Inhibitor That Disrupts Homologous Recombination without Requiring Michael Acceptor Reactivity
An Optimized RAD51 Inhibitor That Disrupts Homologous Recombination without Requiring Michael Acceptor Reactivity
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An Optimized RAD51 Inhibitor That Disrupts Homologous Recombination without Requiring Michael Acceptor Reactivity

Budke, Brian ; Kalin, Jay H ; Pawlowski, Michal ; Zelivianskaia, Anna S ; Wu, Megan ; Kozikowski, Alan P ; Connell, Philip P

Journal of medicinal chemistry, 2013-01, Vol.56 (1), p.254-263 [Periódico revisado por pares]

United States: American Chemical Society

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8
New Water-Soluble Copper(II) Complexes with Morpholine–Thiosemicarbazone Hybrids: Insights into the Anticancer and Antibacterial Mode of Action
New Water-Soluble Copper(II) Complexes with Morpholine–Thiosemicarbazone Hybrids: Insights into the Anticancer and Antibacterial Mode of Action
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New Water-Soluble Copper(II) Complexes with Morpholine–Thiosemicarbazone Hybrids: Insights into the Anticancer and Antibacterial Mode of Action

Ohui, Kateryna ; Afanasenko, Eleonora ; Bacher, Felix ; Ting, Rachel Lim Xue ; Zafar, Ayesha ; Blanco-Cabra, Núria ; Torrents, Eduard ; Dömötör, Orsolya ; May, Nóra V ; Darvasiova, Denisa ; Enyedy, Éva A ; Popović-Bijelić, Ana ; Reynisson, Jóhannes ; Rapta, Peter ; Babak, Maria V ; Pastorin, Giorgia ; Arion, Vladimir B

Journal of medicinal chemistry, 2019-01, Vol.62 (2), p.512-530 [Periódico revisado por pares]

United States: American Chemical Society

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9
Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H 3 Receptor Inverse Agonist with Robust Wake-Promoting Activity
Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H 3 Receptor Inverse Agonist with Robust Wake-Promoting Activity
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Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H 3 Receptor Inverse Agonist with Robust Wake-Promoting Activity

Nirogi, Ramakrishna ; Shinde, Anil ; Mohammed, Abdul Rasheed ; Badange, Rajesh Kumar ; Reballi, Veena ; Bandyala, Thrinath Reddy ; Saraf, Sangram Keshari ; Bojja, Kumar ; Manchineella, Sravanthi ; Achanta, Pramod Kumar ; Kandukuri, Kiran Kumar ; Subramanian, Ramkumar ; Benade, Vijay ; Palacharla, Raghava Choudary ; Jayarajan, Pradeep ; Pandey, Santoshkumar ; Jasti, Venkat

Journal of medicinal chemistry, 2019-02, Vol.62 (3), p.1203-1217 [Periódico revisado por pares]

United States

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10
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862)
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862)
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Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862)

Díaz, José Luis ; Cuberes, Rosa ; Berrocal, Joana ; Contijoch, Montserrat ; Christmann, Ute ; Fernández, Ariadna ; Port, Adriana ; Holenz, Jörg ; Buschmann, Helmut ; Laggner, Christian ; Serafini, Maria Teresa ; Burgueño, Javier ; Zamanillo, Daniel ; Merlos, Manuel ; Vela, José Miguel ; Almansa, Carmen

Journal of medicinal chemistry, 2012-10, Vol.55 (19), p.8211-8224 [Periódico revisado por pares]

United States

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