Discovery of Clinical Candidate 4‑[2-(5-Amino‑1H‑pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro‑N‑1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7
Swain, Nigel. A, Batchelor, Dave, Beaudoin, Serge, Bechle, Bruce M, Bradley, Paul A, Brown, Alan D, Brown, Bruce, Butcher, Ken J, Butt, Richard P, Chapman, Mark L, Denton, Stephen, Ellis, David, Galan, Sebastien R. G, Gaulier, Steven M, Greener, Ben S, de Groot, Marcel J, Glossop, Mel S, Gurrell, Ian K, Hannam, Jo, Johnson, Matthew S, Lin, Zhixin, Markworth, Christopher J, Marron, Brian E, Millan, David S, Nakagawa, Shoko, Pike, Andy, Printzenhoff, David, Rawson, David J, Ransley, Sarah J, Reister, Steven M, Sasaki, Kosuke, Storer, R. Ian, Stupple, Paul A, West, Christopher W
Published in Journal of medicinal chemistry (24.08.2017)
Published in Journal of medicinal chemistry (24.08.2017)
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Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes
Storer, R. Ian, Pike, Andy, Swain, Nigel A., Alexandrou, Aristos J., Bechle, Bruce M., Blakemore, David C., Brown, Alan D., Castle, Neil A., Corbett, Matthew S., Flanagan, Neil J., Fengas, David, Johnson, M. Scott, Jones, Lyn H., Marron, Brian E., Payne, C. Elizabeth, Printzenhoff, David, Rawson, David J., Rose, Colin R., Ryckmans, Thomas, Sun, Jianmin, Theile, Jonathan W., Torella, Rubben, Tseng, Elaine, Warmus, Joseph S.
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
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Journal Article
The design and synthesis of a novel series of indole derived selective ETA antagonists
RAWSON, David J, DACK, Kevin N, DICKINSON, Roger P, JAMES, Kim
Published in Bioorganic & medicinal chemistry letters (21.01.2002)
Published in Bioorganic & medicinal chemistry letters (21.01.2002)
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Journal Article
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na V 1.7
Swain, Nigel A, Batchelor, Dave, Beaudoin, Serge, Bechle, Bruce M, Bradley, Paul A, Brown, Alan D, Brown, Bruce, Butcher, Ken J, Butt, Richard P, Chapman, Mark L, Denton, Stephen, Ellis, David, Galan, Sebastien R G, Gaulier, Steven M, Greener, Ben S, de Groot, Marcel J, Glossop, Mel S, Gurrell, Ian K, Hannam, Jo, Johnson, Matthew S, Lin, Zhixin, Markworth, Christopher J, Marron, Brian E, Millan, David S, Nakagawa, Shoko, Pike, Andy, Printzenhoff, David, Rawson, David J, Ransley, Sarah J, Reister, Steven M, Sasaki, Kosuke, Storer, R Ian, Stupple, Paul A, West, Christopher W
Published in Journal of medicinal chemistry (24.08.2017)
Published in Journal of medicinal chemistry (24.08.2017)
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Journal Article
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain
Bagal, Sharan K., Bungay, Peter J., Denton, Stephen M., Gibson, Karl R., Glossop, Melanie S., Hay, Tanya L., Kemp, Mark I., Lane, Charlotte A. L., Lewis, Mark L., Maw, Graham N., Million, William A., Payne, C. Elizabeth, Poinsard, Cedric, Rawson, David J., Stammen, Blanda L., Stevens, Edward B., Thompson, Lisa R.
Published in ACS medicinal chemistry letters (11.06.2015)
Published in ACS medicinal chemistry letters (11.06.2015)
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Journal Article
The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics
Rawson, David J., Ballard, Stephen, Barber, Christopher, Barker, Laura, Beaumont, Kevin, Bunnage, Mark, Cole, Susan, Corless, Martin, Denton, Stephen, Ellis, David, Floc’h, Marion, Foster, Laura, Gosset, James, Holmwood, Frances, Lane, Charlotte, Leahy, David, Mathias, John, Maw, Graham, Million, William, Poinsard, Cedric, Price, Jenny, Russel, Rachel, Street, Stephen, Watson, Lesa
Published in Bioorganic & medicinal chemistry (01.01.2012)
Published in Bioorganic & medicinal chemistry (01.01.2012)
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Journal Article
Absorption, Distribution, Metabolism, and Excretion Considerations in Selection of Orally Active Indole-Containing Endothelin Antagonist
WALKER, Donald K, DACK, Kevin N, DICKINSON, Roger P, FENNER, Katherine S, JAMES, Kim, RAWSON, David J, SMITH, Dennis A
Published in Drug metabolism and disposition (01.11.2001)
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Published in Drug metabolism and disposition (01.11.2001)
Journal Article
Part 2: Design, synthesis and evaluation of hydroxyproline-derived α₂δ ligands
Rawson, David J, Brugier, Delphine, Harrison, Anthony, Hough, Jo, Newman, Julie, Otterburn, Joe, Maw, Graham N, Price, Jenny, Thompson, Lisa R, Turnpenny, Paul, Warren, Andrew N
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
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Journal Article
Part 3: Design and synthesis of proline-derived α₂δ ligands
Rawson, David J, Brugier, Delphine, Harrison, Anthony, Hough, Jo, Newman, Julie, Otterburn, Joe, Maw, Graham N, Price, Jenny, Thompson, Lisa R, Turnpenny, Paul, Warren, Andrew N
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
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Journal Article
A Novel Series of Potent and Selective PDE5 Inhibitors with Potential for High and Dose-Independent Oral Bioavailability
Allerton, Charlotte M. N, Barber, Christopher G, Beaumont, Kevin C, Brown, David G, Cole, Susan M, Ellis, David, Lane, Charlotte A. L, Maw, Graham N, Mount, Natalie M, Rawson, David J, Robinson, Colin M, Street, Stephen D. A, Summerhill, Nicholas W
Published in Journal of medicinal chemistry (15.06.2006)
Published in Journal of medicinal chemistry (15.06.2006)
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Journal Article
Part 1: N-Alkylated glycines as potent α₂δ ligands
Thompson, Lisa R, Blakemore, David C, Brugier, Delphine, Bryans, Justin S, Chu, Wai-Lam A, Maw, Graham N, Poinsard, Cedric, Rawson, David J, Warren, Andrew N
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
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Journal Article
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na(V)1.7
Swain, Nigel. A., Batchelor, Dave, Beaudoin, Serge, Bechle, Bruce M., Bradley, Paul A., Brown, Alan D., Brown, Bruce, Butcher, Kent J., Butt, Richard P., Chapman, Mark L., Denton, Stephen, Ellis, David, Galan, Sebastien R. G., Gaulier, Steven M., Greener, Ben S., de Groot, Marcel J., Glossop, Mel S., Gurrell, Ian K., Hannan, Jo, Johnson, Matthew S., Lin, Zhixin, Markworth, Christopher J., Marron, Brian E., Milan, David S., Nakaawa, Shoko, Pike, Andy, Printzephoff, David, Rawson, David J., Ransley, Sarah J., Reister, Steven M., Sasaki, Kosuke, Storer, R. Ian, Stupple, Paul A., West, Christopher W.
Published in Journal of medicinal chemistry (24.08.2017)
Published in Journal of medicinal chemistry (24.08.2017)
Get full text
Journal Article
Highly potent and selective Na(V)1.7 inhibitors for use as intravenous agents and chemical probes
Storer, R. Ian, Pike, Andy, Swain, Nigel A., Alexandrou, Aristos J., Bechle, Bruce M., Blakemore, David C., Brown, Alan D., Castle, Neil A., Corbett, Matthew S., Flanagan, Neil J., Fengas, David, Johnson, M. Scott, Jones, Lyn H., Marron, Brian E., Payne, C. Elizabeth, Printzenhoff, David, Rawson, David J., Rose, Colin R., Ryckmans, Thomas, Sun, Jianmin, Theile, Jonathan W., Torella, Rubben, Tseng, Elaine, Warmus, Joseph S.
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
Get full text
Journal Article
Discovery and Optimization of Selective Na(v)1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain
Bagal, Sharan K., Bungay, Peter J., Denton, Stephen M., Gibson, Karl R., Glossop, Melanie S., Hay, Tanya L., Kemp, Mark I., Lane, Charlotte A. L., Lewis, Mark L., Maw, Graham N., Million, William A., Payne, C. Elizabeth, Poinsard, Cedric, Rawson, David J., Stammen, Blanda L., Stevens, Edward B., Thompson, Lisa R.
Published in ACS medicinal chemistry letters (01.06.2015)
Published in ACS medicinal chemistry letters (01.06.2015)
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Journal Article
Part 3: Design and synthesis of proline-derived α 2δ ligands
Rawson, David J., Brugier, Delphine, Harrison, Anthony, Hough, Jo, Newman, Julie, Otterburn, Joe, Maw, Graham N., Price, Jenny, Thompson, Lisa R., Turnpenny, Paul, Warren, Andrew N.
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
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Journal Article
Part 2: Design, synthesis and evaluation of hydroxyproline-derived α 2δ ligands
Rawson, David J., Brugier, Delphine, Harrison, Anthony, Hough, Jo, Newman, Julie, Otterburn, Joe, Maw, Graham N., Price, Jenny, Thompson, Lisa R., Turnpenny, Paul, Warren, Andrew N.
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
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Journal Article