Charles M. Conway

发表

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.

J. Macor, R. Schartman, G. Tong, 2012, Journal of medicinal chemistry.

Oxime carbamate--discovery of a series of novel FAAH inhibitors.

C. Bourin, R. Bertekap, S. Sit, 2010, Bioorganic & medicinal chemistry letters.

Novel inhibitors of fatty acid amide hydrolase.

C. Bourin, R. Bertekap, H. Deng, 2007, Bioorganic & medicinal chemistry letters.

Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.

J. Macor, R. Schartman, G. Thalody, 2013, Bioorganic & medicinal chemistry letters.

Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor.

J. Macor, G. Dubowchik, S. Pin, 2012, Bioorganic & medicinal chemistry letters.

Blocking the CGRP Pathway for Acute and Preventative Treatment of Migraine - The Evolution of Success.

G. Dubowchik, Charles M. Conway, Alison W. Xin, 2020, Journal of medicinal chemistry.

Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.

J. Macor, R. Schartman, G. Dubowchik, 2012, ACS medicinal chemistry letters.

Oral rimegepant for preventive treatment of migraine: a phase 2/3, randomised, double-blind, placebo-controlled trial

R. Lipton, P. Goadsby, V. Coric, 2020, The Lancet.

Safety of Rimegepant, an Oral CGRP Receptor Antagonist, Plus CGRP Monoclonal Antibodies for Migraine

R. Lipton, V. Coric, D. Kudrow, 2020, Headache.

Asymmetric Synthesis of Heterocyclic Analogues of a CGRP Receptor Antagonist for Treating Migraine.

J. Macor, G. Dubowchik, Guanglin Luo, 2015, Organic letters.

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

P. Isakson, C. Svensson, T. Yaksh, 2001, The Journal of Neuroscience.

Rimegepant, an Oral Calcitonin Gene-Related Peptide Receptor Antagonist, for Migraine.

R. Lipton, P. Goadsby, V. Coric, 2019, The New England journal of medicine.

Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability.

J. Macor, R. Schartman, R. Dalterio, 2009, Bioorganic & medicinal chemistry letters.

Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group.

J. Macor, G. Dubowchik, Cen Xu, 2012, Bioorganic & medicinal chemistry letters.

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 effici

Kimberly A. Widmann, J. Macor, R. Schartman, 2008, Journal of medicinal chemistry.

A655 IN VIVO NMDA-INDUCED RELEASE OF SPINAL ADENOSINE AND AMINO ACIDS

T. Yaksh, M. Marsala, Charles M. Conway, 1997 .

Calcitonin gene-related peptide (CGRP) receptor antagonists: novel aspartates and succinates.

J. Macor, G. Dubowchik, Cen Xu, 2012, Bioorganic & medicinal chemistry letters.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain

Alan G. E. Wilson, G. Shankar, S. Mandlekar, 2016, The Journal of Pharmacology and Experimental Therapeutics.

Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines.

B. Beno, J. Macor, G. Dubowchik, 2016, Bioorganic & medicinal chemistry letters.

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.

G. Shankar, J. Macor, C. Albright, 2022, Journal of medicinal chemistry.

Efficacy, safety, and tolerability of rimegepant orally disintegrating tablet for the acute treatment of migraine: a randomised, phase 3, double-blind, placebo-controlled trial

R. Lipton, P. Goadsby, V. Coric, 2019, The Lancet.

Discovery of (S)-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain.

Alan G. E. Wilson, G. Shankar, J. Macor, 2022, Journal of medicinal chemistry.

Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists.

Kimberly A. Widmann, J. Macor, R. Schartman, 2013, Bioorganic & medicinal chemistry letters.

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

V. Coric, K. Johnston, R. Croop, 2022, Cephalalgia Reports.

Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.

Kimberly A. Widmann, Ping Chen, J. Macor, 2020, Bioorganic & medicinal chemistry letters.

Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.

V. Gribkoff, Ping Chen, S. Dworetzky, 2013, Bioorganic & medicinal chemistry letters.

Inhibition Mediated by Glycinergic and GABAergic Receptors on Excitatory Neurons in Mouse Superficial Dorsal Horn Is Location-Specific but Modified by Inflammation

P. Flood, J. Mukai, T. Takazawa, 2017, The Journal of Neuroscience.

Discovery of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain

A. Good, J. Macor, L. Bristow, 2023, Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents.

Asymmetric Synthesis of the Major Metabolite of a Calcitonin Gene-Related Peptide Receptor Antagonist and Mechanism of Epoxide Hydrogenolysis.

J. Macor, G. Dubowchik, Alicia T. Ng, 2017, The Journal of organic chemistry.

Stereoselective synthesis of new conformationally restricted analogues of a potent CGRP receptor antagonist.

B. Beno, J. Macor, D. Zuev, 2005, Organic letters.

Inhibition of AAK 1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain s

Alan G. E. Wilson, Malley, G. Shankar, 2016 .

Potential for treatment benefit of small molecule CGRP receptor antagonist plus monoclonal antibody in migraine therapy

R. Lipton, V. Coric, D. Kudrow, 2020, Neurology.

Serendipitous oxidation product of BIBN4096BS: a potent CGRP receptor antagonist.

J. Macor, G. Dubowchik, Cen Xu, 2014, Bioorganic & medicinal chemistry letters.

Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonists: Heterocyclic Modification of a Novel Azepinone Lead.

Kimberly A. Widmann, Ping Chen, J. Macor, 2021, Bioorganic & medicinal chemistry letters.

The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.

Kimberly A. Widmann, J. Macor, R. Schartman, 2012, Bioorganic & medicinal chemistry letters.

Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.

J. Macor, R. Schartman, G. Dubowchik, 2012, ACS medicinal chemistry letters.