{"id":9944,"date":"2022-10-12T07:01:16","date_gmt":"2022-10-11T23:01:16","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=9944"},"modified":"2022-10-12T07:01:16","modified_gmt":"2022-10-11T23:01:16","slug":"swain-nigel-as-team-published-research-in-journal-of-medicinal-chemistry-in-2017-08-24-936250-20-3","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=9944","title":{"rendered":"Swain, Nigel A’s team published research in Journal of Medicinal Chemistry in 2017-08-24 | 936250-20-3"},"content":{"rendered":"

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 the artcile< 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>, Electric Literature of 936250-20-3<\/a>, the main research area is PF05089771 drug design synthesis NaV17 sodium channel inhibitor pain; diaryl ether aryl sulfonamide preparation sodium channel inhibitor pharmacokinetics.<\/p>\n

A series of acidic diaryl ether heterocyclic sulfonamides that are potent and sub-type selective NaV1.7 inhibitors is described. Optimization of early lead matter focused on removal of structural alerts, improving metabolic stability and reducing cytochrome P 450 inhibition driven drug-drug interaction concerns to deliver the desired balance of preclin. in vitro properties. Concerns over non-metabolic routes of clearance, variable clearance in pre-clin. species and subsequent low confidence human pharmacokinetic predictions led to the decision to conduct a human microdose study to determine clin. pharmacokinetics. The design strategies and results from pre-clin. PK and clin. human microdose PK data are described leading to the discovery of the first sub-type selective NaV1.7 inhibitor clin. candidate PF-05089771 (34) which binds to a site in the voltage sensing domain.<\/p>\n

Journal of Medicinal Chemistry published new progress about Analgesics. 936250-20-3 belongs to class pyrazoles-derivatives, and the molecular formula is C10H17BN2O2, Electric Literature of 936250-20-3<\/a>.<\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

Journal of Medicinal Chemistry published new progress about Analgesics. 936250-20-3 belongs to class pyrazoles-derivatives, and the molecular formula is C10H17BN2O2, Electric Literature of 936250-20-3<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[736,131],"tags":[716],"class_list":["post-9944","post","type-post","status-publish","format-standard","hentry","category-936250-20-3","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nSwain, Nigel A's team published research in Journal of Medicinal Chemistry in 2017-08-24 | 936250-20-3 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"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 the artcile< 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>, Electric Literature of 936250-20-3, the main research area is PF05089771 drug design synthesis NaV17 sodium channel inhibitor pain; diaryl ether aryl sulfonamide preparation sodium channel inhibitor pharmacokinetics.\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.pyrazoles-derivatives.com\/?p=9944\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Swain, Nigel A's team published research in Journal of Medicinal Chemistry in 2017-08-24 | 936250-20-3 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"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 the artcile< 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>, Electric Literature of 936250-20-3, the main research area is PF05089771 drug design synthesis NaV17 sodium channel inhibitor pain; diaryl ether aryl sulfonamide preparation sodium channel inhibitor pharmacokinetics.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=9944\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-11T23:01:16+00:00\" \/>\n<meta name=\"author\" content=\"Jessica.F\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"Jessica.F\" \/>\n\t<meta name=\"twitter:label2\" content=\"Est. reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9944\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9944\",\"name\":\"Swain, Nigel A's team published research in Journal of Medicinal Chemistry in 2017-08-24 | 936250-20-3 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-11T23:01:16+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"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 the artcile< 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>, Electric Literature of 936250-20-3, the main research area is PF05089771 drug design synthesis NaV17 sodium channel inhibitor pain; diaryl ether aryl sulfonamide preparation sodium channel inhibitor pharmacokinetics.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9944#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=9944\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9944#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Swain, Nigel A’s team published research in Journal of Medicinal Chemistry in 2017-08-24 | 936250-20-3\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/\",\"name\":\"pyrazoles-derivatives\",\"description\":\"Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. 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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. 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