Search Results - "CONWAY, Charles M"

Rimegepant, an Oral Calcitonin Gene–Related Peptide Receptor Antagonist, for Migraine by Lipton, Richard B, Croop, Robert, Stock, Elyse G, Stock, David A, Morris, Beth A, Frost, Marianne, Dubowchik, Gene M, Conway, Charles M, Coric, Vladimir, Goadsby, Peter J

“…Treatment with the oral calcitonin gene–related peptide receptor antagonist rimegepant resulted in freedom from migraine pain 2 hours after the dose in 20% of…”
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Potential for treatment benefit of small molecule CGRP receptor antagonist plus monoclonal antibody in migraine therapy by Mullin, Kathleen, Kudrow, David, Croop, Robert, Lovegren, Meghan, Conway, Charles M., Coric, Vladimir, Lipton, Richard B.

“…OBJECTIVETo provide the first clinical report that 2 calcitonin gene-related peptide (CGRP) therapies, a small molecule CGRP receptor antagonist and an…”
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Safety of Rimegepant, an Oral CGRP Receptor Antagonist, Plus CGRP Monoclonal Antibodies for Migraine by Berman, Gary, Croop, Robert, Kudrow, David, Halverson, Philip, Lovegren, Meghan, Thiry, Alexandra C., Conway, Charles M., Coric, Vladimir, Lipton, Richard B.

“…Objective Evaluate the safety and tolerability of oral rimegepant when used for acute treatment concomitantly with a monoclonal antibody (mAb) targeting the…”
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Inhibition Mediated by Glycinergic and GABAergic Receptors on Excitatory Neurons in Mouse Superficial Dorsal Horn Is Location-Specific but Modified by Inflammation by Takazawa, Tomonori, Choudhury, Papiya, Tong, Chi-Kun, Conway, Charles M, Scherrer, Grégory, Flood, Pamela D, Mukai, Jun, MacDermott, Amy B

“…The superficial dorsal horn is the synaptic termination site for many peripheral sensory fibers of the somatosensory system. A wide range of sensory modalities…”
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Discovery of (5S,6S,9R)‑5-Amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro‑5H‑cyclohepta[b]pyridin-9-yl 4‑(2-oxo-2,3-dihydro‑1H‑imidazo[4,5‑b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): An Oral Calcitonin Gene-Related Peptide (CGRP) Antagonist in Clinical Trials for Treating Migraine by Luo, Guanglin, Chen, Ling, Conway, Charles M., Denton, Rex, Keavy, Deborah, Signor, Laura, Kostich, Walter, Lentz, Kimberley A., Santone, Kenneth S., Schartman, Richard, Browning, Marc, Tong, Gary, Houston, John G., Dubowchik, Gene M., Macor, John E.

“…Calcitonin gene-related peptide (CGRP) receptor antagonists have demonstrated clinical efficacy in the treatment of acute migraine. Herein, we describe the…”
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Discovery of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain by Dzierba, Carolyn D., Dasgupta, Bireshwar, Karageorge, George, Kostich, Walter, Hamman, Brian, Allen, Jason, Esposito, Kim M., Padmanabha, Ramesh, Grace, James, Lentz, Kimberley, Morrison, John, Morgan, Daniel, Easton, Amy, Bourin, Clotilde, Browning, Marc R., Rajamani, Ramkumar, Good, Andrew, Parker, Dawn D., Muckelbauer, Jodi K., Khan, Javed, Camac, Daniel, Ghosh, Kaushik, Halan, Vivek, Lippy, Jonathan S., Santone, Kenneth S., Denton, R. Rex, Westphal, Ryan, Bristow, Linda J., Conway, Charles M., Bronson, Joanne J., Macor, John E.

“…Adaptor protein 2-associated kinase 1 (AAK1) is a member of the Ark1/Prk1 family of serine/threonine kinases and plays a role in modulating receptor…”
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Oral rimegepant for preventive treatment of migraine: a phase 2/3, randomised, double-blind, placebo-controlled trial by Croop, Robert, Lipton, Richard B, Kudrow, David, Stock, David A, Kamen, Lisa, Conway, Charles M, Stock, Elyse G, Coric, Vladimir, Goadsby, Peter J

“…Rimegepant is a calcitonin gene-related peptide receptor antagonist that has shown efficacy and safety in the acute treatment of migraine. We aimed to compare…”
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Efficacy, safety, and tolerability of rimegepant orally disintegrating tablet for the acute treatment of migraine: a randomised, phase 3, double-blind, placebo-controlled trial by Croop, Robert, Goadsby, Peter J, Stock, David A, Conway, Charles M, Forshaw, Micaela, Stock, Elyse G, Coric, Vladimir, Lipton, Richard B

“…Rimegepant, a small molecule calcitonin gene-related peptide receptor antagonist, has shown efficacy in the acute treatment of migraine using a standard tablet…”
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Rimegepant 75 mg for acute treatment of migraine is associated with significant reduction in monthly migraine days: Results from a long-term, open-label study by L’Italien, Gilbert, Popoff, Evan, Johnston, Karissa, McGrath, Donnie, Conway, Charles M, Powell, Lauren, Harris, Linda, Kowalczyk, Nicole, Croop, Robert, Coric, Vladimir

“…Background: Rimegepant, a small molecule oral calcitonin gene-related peptide (CGRP) receptor antagonist, is approved for the acute and preventive treatment of…”
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Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success by Dubowchik, Gene M, Conway, Charles M, Xin, Alison W

“…The pivotal role of calcitonin gene-related peptide (CGRP) in migraine pathophysiology was identified over 30 years ago, but the successful clinical…”
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Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain by Luo, Guanglin, Chen, Ling, Kostich, Walter A., Hamman, Brian, Allen, Jason, Easton, Amy, Bourin, Clotilde, Gulianello, Michael, Lippy, Jonathan, Nara, Susheel, Pattipati, Sreenivasulu Naidu, Dandapani, Kumaran, Dokania, Manoj, Vattikundala, Pradeep, Sharma, Vivek, Elavazhagan, Saravanan, Verma, Manoj Kumar, Lal Das, Manish, Wagh, Santosh, Balakrishnan, Anand, Johnson, Benjamin M., Santone, Kenneth S., Thalody, George, Denton, Rex, Saminathan, Hariharan, Holenarsipur, Vinay K., Kumar, Anoop, Rao, Abhijith, Putlur, Siva Prasad, Sarvasiddhi, Sarat Kumar, Shankar, Ganesh, Louis, Justin V., Ramarao, Manjunath, Conway, Charles M., Li, Yu-Wen, Pieschl, Rick, Tian, Yuan, Hong, Yang, Bristow, Linda, Albright, Charles F., Bronson, Joanne J., Macor, John E., Dzierba, Carolyn D.

“…Recent mouse knockout studies identified adapter protein-2-associated kinase 1 (AAK1) as a viable target for treating neuropathic pain. BMS-986176/LX-9211 (4),…”
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Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead by Luo, Guanglin, Jiang, Xiang-Jun, Chen, Ling, Conway, Charles M., Gulianello, Michael, Kostich, Walter, Keavy, Deborah, Signor, Laura J., Chen, Ping, Davis, Carl, Whiterock, Valerie J., Schartman, Richard, Widmann, Kimberly A., Macor, John E., Dubowchik, Gene M.

“…[Display omitted] In our efforts to identify orally bioavailable CGRP receptor antagonists, we previously discovered a novel series of orally available…”
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Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists by Mercer, Stephen E., Chaturvedula, Prasad V., Conway, Charles M., Cook, Deborah A., Davis, Carl D., Pin, Sokhom S., Macci, Robert, Schartman, Richard, Signor, Laura J., Widmann, Kimberly A., Whiterock, Valerie J., Chen, Ping, Xu, Cen, Herbst, John J., Kostich, Walter A., Thalody, George, Macor, John E., Dubowchik, Gene M.

“…[Display omitted] Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown clinically to be effective treatments for migraine. Zavegepant…”
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Asymmetric Synthesis of Heterocyclic Analogues of a CGRP Receptor Antagonist for Treating Migraine by Luo, Guanglin, Chen, Ling, Conway, Charles M., Kostich, Walter, Macor, John E., Dubowchik, Gene M.

“…An asymmetric synthesis of novel heterocyclic analogue of the CGRP receptor antagonist rimegepant (BMS-927711, 3) is reported. The cycloheptane ring was…”
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Asymmetric Synthesis of the Major Metabolite of a Calcitonin Gene-Related Peptide Receptor Antagonist and Mechanism of Epoxide Hydrogenolysis by Luo, Guanglin, Chen, Ling, Conway, Charles M, Kostich, Walter, Johnson, Benjamin M, Ng, Alicia, Macor, John E, Dubowchik, Gene M

“…An asymmetric synthesis of the major metabolite of the calcitonin gene-related peptide recepotor antagonist BMS-846372 is presented. The variously substituted…”
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The Acute Antihyperalgesic Action of Nonsteroidal, Anti-Inflammatory Drugs and Release of Spinal Prostaglandin E2 Is Mediated by the Inhibition of Constitutive Spinal Cyclooxygenase-2 (COX-2) but not COX-1 by Yaksh, Tony L, Dirig, David M, Conway, Charles M, Svensson, Camilla, Luo, Z. David, Isakson, Peter C

“…Western blots show the constitutive expression of COX-1 and COX-2 in the rat spinal dorsal and ventral horns and in the dorsal root ganglia. Using selective…”
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Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines by Civiello, Rita L., Han, Xiaojun, Beno, Brett R., Chaturvedula, Prasad V., Herbst, John J., Xu, Cen, Conway, Charles M., Macor, John E., Dubowchik, Gene M.

“…[Display omitted] Calcitonin gene-related peptide (CGRP) is a potent neuropeptide implicated in the pathophysiology of migraine. In the course of seeking CGRP…”
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Discovery of (R)-4-(8-Fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): A Potent Antagonist of the Human Calcitonin Gene-Related Peptide Receptor for Migraine with Rapid and Efficient Intranasal Exposure by Degnan, Andrew P, Chaturvedula, Prasad V, Conway, Charles M, Cook, Deborah A, Davis, Carl D, Denton, Rex, Han, Xiaojun, Macci, Robert, Mathias, Neil R, Moench, Paul, Pin, Sokhom S, Ren, Shelly X, Schartman, Richard, Signor, Laura J, Thalody, George, Widmann, Kimberly A, Xu, Cen, Macor, John E, Dubowchik, Gene M

“…Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Early chemistry leads suffered from modest potency, significant…”
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Oxime Carbamate—Discovery of a series of novel FAAH inhibitors by Sit, S.Y., Conway, Charles M., Xie, Kai, Bertekap, Robert, Bourin, Clotilde, Burris, Kevin D.

“…The rationale behind the discovery and the biological evaluations of this novel class of FAAH inhibitors are presented. Both in vitro and in vivo results of…”
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Calcitonin gene-related peptide (CGRP) receptor antagonists: Pyridine as a replacement for a core amide group by Luo, Guanglin, Chen, Ling, Civiello, Rita, Pin, Sokhom S., Xu, Cen, Kostich, Walter, Kelley, Michelle, Conway, Charles M., Macor, John E., Dubowchik, Gene M.

“…In our continuing efforts to identify CGRP receptor antagonists that can be dosed orally for the treatment of migraine headache, we have investigated a…”
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