Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis
Scanio, Marc J. C, Searle, Xenia B, Liu, Bo, Koenig, John R, Altenbach, Robert, Gfesser, Gregory A, Bogdan, Andrew, Greszler, Stephen, Zhao, Gang, Singh, Ashvani, Fan, Yihong, Swensen, Andrew M, Vortherms, Timothy, Manelli, Arlene, Balut, Corina, Jia, Ying, Gao, Wenqing, Yong, Hong, Schrimpf, Michael, Tse, Chris, Kym, Philip, Wang, Xueqing
Published in ACS medicinal chemistry letters (14.11.2019)
Published in ACS medicinal chemistry letters (14.11.2019)
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Journal Article
Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists
Perner, Richard J., Koenig, John R., DiDomenico, Stanley, Gomtsyan, Arthur, Schmidt, Robert G., Lee, Chih-Hung, Hsu, Margaret C., McDonald, Heath A., Gauvin, Donna M., Joshi, Shailen, Turner, Teresa M., Reilly, Regina M., Kym, Philip R., Kort, Michael E.
Published in Bioorganic & medicinal chemistry (01.07.2010)
Published in Bioorganic & medicinal chemistry (01.07.2010)
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Journal Article
Discovery and SAR of 4-aminopyrrolidine-2-carboxylic acid correctors of CFTR for the treatment of cystic fibrosis
Scanio, Marc J.C., Searle, Xenia B., Liu, Bo, Koenig, John R., Altenbach, Robert J., Gfesser, Gregory A., Bogdan, Andrew, Greszler, Stephen, Zhao, Gang, Singh, Ashvani, Fan, Yihong, Swensen, Andrew M., Vortherms, Timothy, Manelli, Arlene, Balut, Corina, Gao, Wenqing, Yong, Hong, Schrimpf, Michael, Tse, Chris, Kym, Philip, Wang, Xueqing
Published in Bioorganic & medicinal chemistry letters (15.09.2022)
Published in Bioorganic & medicinal chemistry letters (15.09.2022)
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Journal Article
A-995662 [(R)-8-(4-methyl-5-(4-(trifluoromethyl)phenyl)oxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol], a novel, selective TRPV1 receptor antagonist, reduces spinal release of glutamate and CGRP in a rat knee joint pain model
Puttfarcken, Pamela S., Han, Ping, Joshi, Shailen K., Neelands, Torben R., Gauvin, Donna M., Baker, Scott J., Lewis, La Geisha R., Bianchi, Bruce R., Mikusa, Joseph P., Koenig, John R., Perner, Richard J., Kort, Michael E., Honore, Prisca, Faltynek, Connie R., Kym, Philip R., Reilly, Regina M.
Published in Pain (Amsterdam) (01.08.2010)
Published in Pain (Amsterdam) (01.08.2010)
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Journal Article
Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists
Schmidt, Robert G., Bayburt, Erol K., Latshaw, Steven P., Koenig, John R., Daanen, Jerome F., McDonald, Heath A., Bianchi, Bruce R., Zhong, Chengmin, Joshi, Shailen, Honore, Prisca, Marsh, Kennan C., Lee, Chih-Hung, Faltynek, Connie R., Gomtsyan, Arthur
Published in Bioorganic & medicinal chemistry letters (01.03.2011)
Published in Bioorganic & medicinal chemistry letters (01.03.2011)
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Journal Article
Novel Transient Receptor Potential Vanilloid 1 Receptor Antagonists for the Treatment of Pain: Structure−Activity Relationships for Ureas with Quinoline, Isoquinoline, Quinazoline, Phthalazine, Quinoxaline, and Cinnoline Moieties
Gomtsyan, Arthur, Bayburt, Erol K, Schmidt, Robert G, Zheng, Guo Zhu, Perner, Richard J, Didomenico, Stanley, Koenig, John R, Turner, Sean, Jinkerson, Tammie, Drizin, Irene, Hannick, Steven M, Macri, Bryan S, McDonald, Heath A, Honore, Prisca, Wismer, Carol T, Marsh, Kennan C, Wetter, Jill, Stewart, Kent D, Oie, Tetsuro, Jarvis, Michael F, Surowy, Carol S, Faltynek, Connie R, Lee, Chih-Hung
Published in Journal of medicinal chemistry (10.02.2005)
Published in Journal of medicinal chemistry (10.02.2005)
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Journal Article
Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists
Brown, Brian S., Keddy, Ryan, Zheng, Guo Zhu, Schmidt, Robert G., Koenig, John R., McDonald, Heath A., Bianchi, Bruce R., Honore, Prisca, Jarvis, Michael F., Surowy, Carol S., Polakowski, James S., Marsh, Kennan C., Faltynek, Connie R., Lee, Chih-Hung
Published in Bioorganic & medicinal chemistry (15.09.2008)
Published in Bioorganic & medicinal chemistry (15.09.2008)
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Journal Article
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: Effects of substitution about the rigidifying ring
KOENIG, John R, HUAQING LIU, BRIONI, Jorge D, COWART, Marlon, DRIZIN, Irene, WITTE, David G, CARR, Tracy L, MANELLI, Arlene M, MILICIC, Ivan, STRAKHOVA, Marina I, MILLER, Thomas R, ESBENSHADE, Timothy A
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
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Journal Article
Discovery of TRPV1 antagonist ABT-116
Brown, Brian S, Keddy, Ryan, Perner, Richard J, DiDomenico, Stanley, Koenig, John R, Jinkerson, Tammie K, Hannick, Steven M, McDonald, Heath A, Bianchi, Bruce R, Honore, Prisca, Puttfarcken, Pamela S, Moreland, Robert B, Marsh, Kennan C, Faltynek, Connie R, Lee, Chih-Hung
Published in Bioorganic & medicinal chemistry letters (01.06.2010)
Published in Bioorganic & medicinal chemistry letters (01.06.2010)
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Journal Article
α-Methylation at benzylic fragment of N-aryl- N′-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model
Gomtsyan, Arthur, Bayburt, Erol K., Keddy, Ryan, Turner, Sean C., Jinkerson, Tammie K., Didomenico, Stanley, Perner, Richard J., Koenig, John R., Drizin, Irene, McDonald, Heath A., Surowy, Carol S., Honore, Prisca, Mikusa, Joe, Marsh, Kennan C., Wetter, Jill M., Faltynek, Connie R., Lee, Chih-Hung
Published in Bioorganic & medicinal chemistry letters (15.07.2007)
Published in Bioorganic & medicinal chemistry letters (15.07.2007)
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Journal Article
In Vitro Structure−Activity Relationship and In Vivo Characterization of 1-(Aryl)-3-(4-(amino)benzyl)urea Transient Receptor Potential Vanilloid 1 Antagonists
Perner, Richard J, DiDomenico, Stanley, Koenig, John R, Gomtsyan, Arthur, Bayburt, Erol K, Schmidt, Robert G, Drizin, Irene, Zheng, Guo Zhu, Turner, Sean C, Jinkerson, Tammie, Brown, Brian S, Keddy, Ryan G, Lukin, Kurill, McDonald, Heath A, Honore, Prisca, Mikusa, Joe, Marsh, Kennan C, Wetter, Jill M, St. George, Karen, Jarvis, Michael F, Faltynek, Connie R, Lee, Chih-Hung
Published in Journal of medicinal chemistry (26.07.2007)
Published in Journal of medicinal chemistry (26.07.2007)
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Journal Article
Structure–activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists
Drizin, Irene, Gomtsyan, Arthur, Bayburt, Erol K., Schmidt, Robert G., Zheng, Guo Zhu, Perner, Richard J., DiDomenico, Stanley, Koenig, John R., Turner, Sean C., Jinkerson, Tammie K., Brown, Brian S., Keddy, Ryan G., McDonald, Heath A., Honore, Prisca, Wismer, Carol T., Marsh, Kennan C., Wetter, Jill M., Polakowski, James S., Segreti, Jason A., Jarvis, Michael F., Faltynek, Connie R., Lee, Chih-Hung
Published in Bioorganic & medicinal chemistry (15.07.2006)
Published in Bioorganic & medicinal chemistry (15.07.2006)
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Journal Article
Adenosine kinase inhibitors: polar 7-Substitutent of pyridopyrimidine derivatives improving their locomotor selectivity
Zheng, Guo Zhu, Mao, Yue, Lee, Chih-Hung, Pratt, John K., Koenig, John R., Perner, Richard J., Cowart, Marlon D., Gfesser, Gregory A., McGaraughty, Steve, Chu, Katharine L., Zhu, Chang, Yu, Haixia, Kohlhaas, Kathy, Alexander, Karen M., Wismer, Carol T., Mikusa, Joseph, Jarvis, Michael F., Kowaluk, Elizabeth A., Stewart, Andrew O.
Published in Bioorganic & medicinal chemistry letters (15.09.2003)
Published in Bioorganic & medicinal chemistry letters (15.09.2003)
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Journal Article
Pyridopyrimidine analogues as novel adenosine kinase inhibitors
Zheng, Guo Zhu, Lee, Chih-Hung, Pratt, John K, Perner, Richard J, Jiang, Mei Qun, Gomtsyan, Arthur, Matulenko, Mark A, Mao, Yui, Koenig, John R, Kim, Ki H, Muchmore, Steve, Yu, Haixia, Kohlhaas, Kathy, Alexander, Karen M, McGaraughty, Steve, Chu, Katharine L, Wismer, Carol T, Mikusa, Joseph, Jarvis, Michael F, Marsh, Kennan, Kowaluk, Elizabeth A, Bhagwat, Shripad S, Stewart, Andrew O
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
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Journal Article
Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl) pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na(v)1.7/Nav1.8 blockers for the treatment of pain
Patel, Meena, Peltier, Hillary M., Matulenko, Mark A., Koenig, John R., Scanio, Marc J. C., Gum, Rebecca J., El-Kouhen, Odile F., Fricano, Meagan M., Lundgaard, Greta L., Neelands, Torben, Zhang, Xu-Feng, Zhan, Cenchen, Pai, Madhavi, Ghoreishi-Haack, Nayereh, Hudzik, Thomas, Gintant, Gary, Martin, Ruth, McGaraughty, Steve, Xu, Jun, Bow, Daniel, Kalvass, John C., Kym, Philip R., DeGoey, David A., Kort, Michael E.
Published in Bioorganic & medicinal chemistry (01.06.2022)
Published in Bioorganic & medicinal chemistry (01.06.2022)
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Journal Article
CHROMANYLUREA COMPOUNDS THAT INHIBIT VANILLOID RECEPTOR SUBTYPE 1(VR1) RECEPTOR AND USES THEREOF
SCHMIDT ROBERT G. JR, BROWN S. BRIAN, GOMTSYAN ARTHUR R, KOENIG R. JOHN, BAYBURT EROL K, DAANEN F. JEROME, LATSHAW STEVE, LEE CHIH HUNG, JINKERSON K. TAMMIE
Year of Publication 20.12.2012
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Year of Publication 20.12.2012
Patent
Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na v 1.7/ Nav1.8 blockers for the treatment of pain
Patel, Meena V, Peltier, Hillary M, Matulenko, Mark A, Koenig, John R, C Scanio, Marc J, Gum, Rebecca J, El-Kouhen, Odile F, Fricano, Meagan M, Lundgaard, Greta L, Neelands, Torben, Zhang, Xu-Feng, Zhan, Cenchen, Pai, Madhavi, Ghoreishi-Haack, Nayereh, Hudzik, Thomas, Gintant, Gary, Martin, Ruth, McGaraughty, Steve, Xu, Jun, Bow, Daniel, Kalvass, John C, Kym, Philip R, DeGoey, David A, Kort, Michael E
Published in Bioorganic & medicinal chemistry (01.06.2022)
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Published in Bioorganic & medicinal chemistry (01.06.2022)
Journal Article
Rigidified 2-aminopyrimidines as histamine H 4 receptor antagonists: Effects of substitution about the rigidifying ring
Koenig, John R., Liu, Huaqing, Drizin, Irene, Witte, David G., Carr, Tracy L., Manelli, Arlene M., Milicic, Ivan, Strakhova, Marina I., Miller, Thomas R., Esbenshade, Timothy A., Brioni, Jorge D., Cowart, Marlon
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
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Journal Article
Rigidified 2-aminopyrimidines as histamine H sub(4) receptor antagonists: Effects of substitution about the rigidifying ring
Koenig, John R, Liu, Huaqing, Drizin, Irene, Witte, David G, Carr, Tracy L, Manelli, Arlene M, Milicic, Ivan, Strakhova, Marina I, Miller, Thomas R, Esbenshade, Timothy A, Brioni, Jorge D, Cowart, Marlon
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
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Journal Article
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
BAYBURT EROL K.,DIDOMENICO STANLEY JR.,DRIZIN IRENE,GOMTSYAN ARTHUR R.,KOENIG JOHN R.,PENNER RICHARD J.,SCHMIDT ROBERT G. JR.,TURNER SEAN C.,WHITE TAMMIE K.,ZHENG GUO ZHU
Year of Publication 15.11.2006
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Year of Publication 15.11.2006
Patent