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Expert Opinion on Therapeutic Patents Volume 22, 2012 - Issue 12
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Novel M1 allosteric ligands: a patent review

Scott D Kuduk
&
Douglas C BeshoreDepartment of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, [email protected]
Pages 1385-1398 | Published online: 23 Oct 2012

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Daniel J Foster, Derrick L Choi, P Jeffrey Conn & Jerri M Rook. (2014) Activation of M1 and M4 muscarinic receptors as potential treatments for Alzheimer’s disease and schizophrenia. Neuropsychiatric Disease and Treatment 10, pages 183-191.
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Articles from other publishers (29)

Huong T. M. Nguyen, Emma T. van der Westhuizen, Christopher J. Langmead, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos & Celine Valant. (2022) Opportunities and challenges for the development of M 1 muscarinic receptor positive allosteric modulators in the treatment for neurocognitive deficits . British Journal of Pharmacology.
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Chad R. Johnson, Brian D. Kangas, Emily M. Jutkiewicz, Jack Bergman & Andrew Coop. (2022) Drug Design Targeting the Muscarinic Receptors and the Implications in Central Nervous System Disorders. Biomedicines 10:2, pages 398.
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Md Ashrafur Rahman, Norifumi Tanaka, Md. Nuruzzaman, Shandhya DebNath & Shigenori Kawahara. (2020) Blockade of the M1 muscarinic acetylcholine receptors impairs eyeblink serial feature-positive discrimination learning in mice. PLOS ONE 15:8, pages e0237451.
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Karin Hellman, Jörgen Ohlsson, Marcus Malo, Roger Olsson & Fredrik Ek. (2019) Discovery of Procognitive Antipsychotics by Combining Muscarinic M 1 Receptor Structure–Activity Relationship with Systems Response Profiles in Zebrafish Larvae . ACS Chemical Neuroscience 11:2, pages 173-183.
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Shotaro Miura, Koichiro Fukuda, Shinichi Masada, Hirotsugu Usutani, Makoto Kanematsu, David G. Cork & Tetsuji Kawamoto. (2019) Rapid and efficient synthesis of a novel cholinergic muscarinic M 1 receptor positive allosteric modulator using flash chemistry . Organic & Biomolecular Chemistry 17:35, pages 8166-8174.
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Elham Khajehali, Celine Valant, Manuela Jörg, Andrew B. Tobin, P. Jeffrey Conn, Craig W. Lindsley, Patrick M. Sexton, Peter J. Scammells & Arthur Christopoulos. (2018) Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor. Biochemical Pharmacology 154, pages 243-254.
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Christian C. Felder, Paul J. Goldsmith, Kimberley Jackson, Helen E. Sanger, David A. Evans, Adrian J. Mogg & Lisa M. Broad. (2018) Current status of muscarinic M1 and M4 receptors as drug targets for neurodegenerative diseases. Neuropharmacology 136, pages 449-458.
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Jason M. Uslaner, Scott D. Kuduk, Marion Wittmann, Henry S. Lange, Steve V. Fox, Chris Min, Natasa Pajkovic, Dawn Harris, Caroline Cilissen, Chantal Mahon, Kate Mostoller, Steve Warrington & Douglas C. Beshore. (2018) Preclinical to Human Translational Pharmacology of the Novel M 1 Positive Allosteric Modulator MK-7622 . Journal of Pharmacology and Experimental Therapeutics 365:3, pages 556-566.
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Alexander Flohr, Roman Hutter, Barbara Mueller, Claudia Bohnert, Mélanie Pellisson & Hervé Schaffhauser. (2017) Discovery of the first low-shift positive allosteric modulators for the muscarinic M1 receptor. Bioorganic & Medicinal Chemistry Letters 27:24, pages 5415-5419.
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Pavan Kumar Chintamaneni, Praveen T. Krishnamurthy, Pachava Vengal Rao & SaiKiran S.S. Pindiprolu. (2017) Surface modified nano-lipid drug conjugates of positive allosteric modulators of M1 muscarinic acetylcholine receptor for the treatment of Alzheimer’s disease. Medical Hypotheses 101, pages 17-22.
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Bruce J. Melancon & Corey R. Hopkins. 2016. Allosterism in Drug Discovery. Allosterism in Drug Discovery 175 193 .
Arjan Blokland, Anke Sambeth, Jos Prickaerts & Wim J. Riedel. (2016) Why an M1 Antagonist Could Be a More Selective Model for Memory Impairment than Scopolamine. Frontiers in Neurology 7.
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Joseph D. Panarese, Hykeyung P. Cho, Jeffrey J. Adams, Kellie D. Nance, Pedro M. Garcia-Barrantes, Sichen Chang, Ryan D. Morrison, Anna L. Blobaum, Colleen M. Niswender, Shaun R. Stauffer, P. Jeffrey Conn & Craig W. Lindsley. (2016) Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration. Bioorganic & Medicinal Chemistry Letters 26:15, pages 3822-3825.
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Shailesh N. Mistry, Herman Lim, Manuela Jörg, Ben Capuano, Arthur Christopoulos, J. Robert Lane & Peter J. Scammells. (2016) Novel Fused Arylpyrimidinone Based Allosteric Modulators of the M 1 Muscarinic Acetylcholine Receptor . ACS Chemical Neuroscience 7:5, pages 647-661.
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Jennifer E. Davoren, Steven V. O’Neil, Dennis P. Anderson, Michael A. Brodney, Lois Chenard, Keith Dlugolenski, Jeremy R. Edgerton, Michael Green, Michelle Garnsey, Sarah Grimwood, Anthony R. Harris, Gregory W. Kauffman, Erik LaChapelle, John T. Lazzaro, Che-Wah Lee, Susan M. Lotarski, Deane M. Nason, R. Scott Obach, Veronica Reinhart, Romelia Salomon-Ferrer, Stefanus J. Steyn, Damien Webb, Jiangli Yan & Lei Zhang. (2016) Design and optimization of selective azaindole amide M 1 positive allosteric modulators. Bioorganic & Medicinal Chemistry Letters 26:2, pages 650-655.
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Ruben Vardanyan & Victor Hruby. 2016. Synthesis of Best-Seller Drugs. Synthesis of Best-Seller Drugs 215 225 .
Richie R. Bhandare, Rong Gao, Daniel J. Canney & Prashant S. Kharkar. 2016. Crystallizing Ideas – The Role of Chemistry. Crystallizing Ideas – The Role of Chemistry 155 179 .
Kevin P. Cusack, Ying Wang, Michael Z. Hoemann, Jasmina Marjanovic, Roland G. Heym & Anil Vasudevan. (2015) Design strategies to address kinetics of drug binding and residence time. Bioorganic & Medicinal Chemistry Letters 25:10, pages 2019-2027.
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Arann R Rowe, Louise Mercer, Valentina Casetti, Kyra-Verena Sendt, Giovanni Giaroli, Sukhwinder S Shergill & Derek K Tracy. (2015) Dementia praecox redux: A systematic review of the nicotinic receptor as a target for cognitive symptoms of schizophrenia. Journal of Psychopharmacology 29:2, pages 197-211.
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Xinyu Chen, Jessika Klöckner, Janine Holze, Cornelia Zimmermann, Wiebke K. Seemann, Ramona Schrage, Andreas Bock, Klaus Mohr, Christian Tränkle, Ulrike Holzgrabe & Michael Decker. (2014) Rational Design of Partial Agonists for the Muscarinic M 1 Acetylcholine Receptor . Journal of Medicinal Chemistry 58:2, pages 560-576.
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Changho Han, Arindam Chatterjee, Meredith J. Noetzel, Joseph D. Panarese, Emery Smith, Peter Chase, Peter Hodder, Colleen Niswender, P. Jeffrey Conn, Craig W. Lindsley & Shaun R. Stauffer. (2015) Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-Dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators. Bioorganic & Medicinal Chemistry Letters 25:2, pages 384-388.
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Alaa Abdul-Ridha, J.Robert Lane, Shailesh N. Mistry, Laura López, Patrick M. Sexton, Peter J. Scammells, Arthur Christopoulos & Meritxell Canals. (2014) Mechanistic Insights into Allosteric Structure-Function Relationships at the M1 Muscarinic Acetylcholine Receptor. Journal of Biological Chemistry 289:48, pages 33701-33711.
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Briana J. Davie, Celine Valant, Jonathan M. White, Patrick M. Sexton, Ben Capuano, Arthur Christopoulos & Peter J. Scammells. (2014) Synthesis and Pharmacological Evaluation of Analogues of Benzyl Quinolone Carboxylic Acid (BQCA) Designed to Bind Irreversibly to an Allosteric Site of the M 1 Muscarinic Acetylcholine Receptor . Journal of Medicinal Chemistry 57:12, pages 5405-5418.
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Zhi-Qiang Yang, Youheng Shu, Lei Ma, Marion Wittmann, William J. Ray, Matthew A. Seager, Kenneth A. Koeplinger, Charles D. Thompson, George D. Hartman, Mark T. Bilodeau & Scott D. Kuduk. (2014) Discovery of Naphthyl-Fused 5-Membered Lactams as a New Class of M 1 Positive Allosteric Modulators . ACS Medicinal Chemistry Letters 5:5, pages 604-608.
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Sophie J Bradley, Sajjad A Riaz & Andrew B Tobin. (2014) Employing novel animal models in the design of clinically efficacious GPCR ligands. Current Opinion in Cell Biology 27, pages 117-125.
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Takaaki Sumiyoshi & Takeshi Enomoto. 2015. Small Molecule Therapeutics for Schizophrenia. Small Molecule Therapeutics for Schizophrenia 183 211 .
Bruce J. Melancon, James C. Tarr, Joseph D. Panarese, Michael R. Wood & Craig W. Lindsley. (2013) Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease. Drug Discovery Today 18:23-24, pages 1185-1199.
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Christopher L. Cioffi. (2013) Modulation of NMDA receptor function as a treatment for schizophrenia. Bioorganic & Medicinal Chemistry Letters 23:18, pages 5034-5044.
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Briana J. Davie, Arthur Christopoulos & Peter J. Scammells. (2013) Development of M 1 mAChR Allosteric and Bitopic Ligands: Prospective Therapeutics for the Treatment of Cognitive Deficits . ACS Chemical Neuroscience 4:7, pages 1026-1048.
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