Rimegepant, an Oral Calcitonin Gene–Related Peptide Receptor Antagonist, for Migraine
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
Published in The New England journal of medicine (11.07.2019)
Published in The New England journal of medicine (11.07.2019)
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Journal Article
Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success
Dubowchik, Gene M, Conway, Charles M, Xin, Alison W
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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Design, Structure–Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2‑b]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors
Hartz, Richard A., Ahuja, Vijay T., Sivaprakasam, Prasanna, Xiao, Hong, Krause, Carol M., Clarke, Wendy J., Kish, Kevin, Lewis, Hal, Szapiel, Nicolas, Ravirala, Ramu, Mutalik, Sayali, Nakmode, Deepa, Shah, Devang, Burton, Catherine R., Macor, John E., Dubowchik, Gene M.
Published in Journal of medicinal chemistry (23.03.2023)
Published in Journal of medicinal chemistry (23.03.2023)
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Journal Article
Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core
Sivaprakasam, Prasanna, Han, Xiaojun, Civiello, Rita L., Jacutin-Porte, Swanee, Kish, Kevin, Pokross, Matt, Lewis, Hal A., Ahmed, Nazia, Szapiel, Nicolas, Newitt, John A., Baldwin, Eric T., Xiao, Hong, Krause, Carol M., Park, Hyunsoo, Nophsker, Michelle, Lippy, Jonathan S., Burton, Catherine R., Langley, David R., Macor, John E., Dubowchik, Gene M.
Published in Bioorganic & medicinal chemistry letters (01.05.2015)
Published in Bioorganic & medicinal chemistry letters (01.05.2015)
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Journal Article
Structure–activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors
Luo, Guanglin, Chen, Ling, Jacutin-Porte, Swanee, Han, Ying, Burton, Catherine R., Xiao, Hong, Krause, Carol M., Cao, Yang, Liu, Nengyin, Kish, Kevin, Lewis, Hal A., Macor, John E., Dubowchik, Gene M.
Published in Bioorganic & medicinal chemistry letters (01.02.2023)
Published in Bioorganic & medicinal chemistry letters (01.02.2023)
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Journal Article
Discovery of 2‑(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase‑3 (GSK-3) Inhibitors
Hartz, Richard A., Ahuja, Vijay T., Luo, Guanglin, Chen, Ling, Sivaprakasam, Prasanna, Xiao, Hong, Krause, Carol M., Clarke, Wendy J., Xu, Songmei, Tokarski, John S., Kish, Kevin, Lewis, Hal, Szapiel, Nicolas, Ravirala, Ramu, Mutalik, Sayali, Nakmode, Deepa, Shah, Devang, Burton, Catherine R., Macor, John E., Dubowchik, Gene M.
Published in Journal of medicinal chemistry (08.06.2023)
Published in Journal of medicinal chemistry (08.06.2023)
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Journal Article
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase‑3 Inhibitors
Luo, Guanglin, Chen, Ling, Burton, Catherine R, Xiao, Hong, Sivaprakasam, Prasanna, Krause, Carol M, Cao, Yang, Liu, Nengyin, Lippy, Jonathan, Clarke, Wendy J, Snow, Kimberly, Raybon, Joseph, Arora, Vinod, Pokross, Matt, Kish, Kevin, Lewis, Hal A, Langley, David R, Macor, John E, Dubowchik, Gene M
Published in Journal of medicinal chemistry (11.02.2016)
Published in Journal of medicinal chemistry (11.02.2016)
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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
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.
Published in Journal of medicinal chemistry (13.12.2012)
Published in Journal of medicinal chemistry (13.12.2012)
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Journal Article
Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead
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.
Published in Bioorganic & medicinal chemistry letters (01.07.2021)
Published in Bioorganic & medicinal chemistry letters (01.07.2021)
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Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists
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.
Published in Bioorganic & medicinal chemistry letters (01.01.2021)
Published in Bioorganic & medicinal chemistry letters (01.01.2021)
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Journal Article
Asymmetric Synthesis of Heterocyclic Analogues of a CGRP Receptor Antagonist for Treating Migraine
Luo, Guanglin, Chen, Ling, Conway, Charles M., Kostich, Walter, Macor, John E., Dubowchik, Gene M.
Published in Organic letters (18.12.2015)
Published in Organic letters (18.12.2015)
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Cathepsin B-Labile Dipeptide Linkers for Lysosomal Release of Doxorubicin from Internalizing Immunoconjugates: Model Studies of Enzymatic Drug Release and Antigen-Specific In Vitro Anticancer Activity
Dubowchik, Gene M, Firestone, Raymond A, Padilla, Linda, Willner, David, Hofstead, Sandra J, Mosure, Kathleen, Knipe, Jay O, Lasch, Shirley J, Trail, Pamela A
Published in Bioconjugate chemistry (01.07.2002)
Published in Bioconjugate chemistry (01.07.2002)
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Journal Article
Asymmetric Synthesis of the Major Metabolite of a Calcitonin Gene-Related Peptide Receptor Antagonist and Mechanism of Epoxide Hydrogenolysis
Luo, Guanglin, Chen, Ling, Conway, Charles M, Kostich, Walter, Johnson, Benjamin M, Ng, Alicia, Macor, John E, Dubowchik, Gene M
Published in Journal of organic chemistry (07.04.2017)
Published in Journal of organic chemistry (07.04.2017)
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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
Chaturvedula, Prasad V., Mercer, Stephen E., Pin, Sokhom S., Thalody, George, Xu, Cen, Conway, Charlie M., Keavy, Deborah, Signor, Laura, Cantor, Glenn H., Mathias, Neil, Moench, Paul, Denton, Rex, Macci, Robert, Schartman, Richard, Whiterock, Valerie, Davis, Carl, Macor, John E., Dubowchik, Gene M.
Published in Bioorganic & medicinal chemistry letters (01.06.2013)
Published in Bioorganic & medicinal chemistry letters (01.06.2013)
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Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists
Tora, George, Degnan, Andrew P., Conway, Charles M., Kostich, Walter A., Davis, Carl D., Pin, Sokhom S., Schartman, Richard, Xu, Cen, Widmann, Kimberly A., Macor, John E., Dubowchik, Gene M.
Published in Bioorganic & medicinal chemistry letters (15.10.2013)
Published in Bioorganic & medicinal chemistry letters (15.10.2013)
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Receptor-mediated and enzyme-dependent targeting of cytotoxic anticancer drugs
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Book Review
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Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines
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.
Published in Bioorganic & medicinal chemistry letters (15.02.2016)
Published in Bioorganic & medicinal chemistry letters (15.02.2016)
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Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor
Chaturvedula, Prasad V., Pin, Sokhom, Tholady, George, Conway, Charlie M., Macor, John E., Dubowchik, Gene M.
Published in Bioorganic & medicinal chemistry letters (15.07.2012)
Published in Bioorganic & medicinal chemistry letters (15.07.2012)
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