1235406-58-2Relevant academic research and scientific papers
1,3,4-thiadiazole compound and preparation method thereof
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Paragraph 0016; 0036; 0037, (2017/03/08)
The invention discloses 2-(2,4-dimethoxy benzyl)-(5-chloro-2-fluoro-4-(2-(4-pyridazinyl)-4-(trifluoromethyl)phenoxy) phenyl)sulfamide-1,3,4-thiadiazole and a preparation method thereof. The structure of the 2-(2,4-dimethoxy benzyl)-(5-chloro-2-fluoro-4-(2-(4-pyridazinyl)-4-(trifluoromethyl)phenoxy) phenyl)sulfamide-1,3,4-thiadiazole is as shown in the formula (I), and the 2-(2,4-dimethoxy benzyl)-(5-chloro-2-fluoro-4-(2-(4-pyridazinyl)-4-(trifluoromethyl)phenoxy) phenyl)sulfamide-1,3,4-thiadiazole belongs to a novel 1,3,4-thiadiazole compound and is not reported in literature. The research field of 1,3,4-thiadiazole compounds is widened, the synthesis yield is high, the process is simple, and the method is suitable for industrial production.
A 1, 3, 4 - thiadiazole compound and its preparation method (by machine translation)
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Paragraph 0040; 0041; 0058; 0062, (2017/04/28)
The invention discloses 2 - (5 - chloro - 2 - fluoro - 4 - (2 - (4 - pyridazinyl) - 4 - (trifluoromethyl) phenoxy) phenyl) sulfonamide - 1, 3, 4 - thiadiazole and its preparation method. 2 - (5 - chloro - 2 - fluoro - 4 - (2 - (4 - pyridazinyl) - 4 - (trifluoromethyl) phenoxy) phenyl) sulfonamide - 1, 3, 4 - thiadiazole of formula (I) structural formula shown, belonging to a new 1, 3, 4 - thiadiazole compounds, has not seen the literature reports, widens the 1, 3, 4 - thiadiazole compounds of the study area, its synthesis yield is high, simple process, and is applicable to industrial production. (by machine translation)
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.
, p. 7029 - 7042 (2017/09/07)
A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead matter focused on removal of structural alerts, improving metabolic stability and reducing cytochrome P450 inhibition driven drug-drug interaction concerns to deliver the desired balance of preclinical in vitro properties. Concerns over nonmetabolic routes of clearance, variable clearance in preclinical species, and subsequent low confidence human pharmacokinetic predictions led to the decision to conduct a human microdose study to determine clinical pharmacokinetics. The design strategies and results from preclinical PK and clinical human microdose PK data are described leading to the discovery of the first subtype selective NaV1.7 inhibitor clinical candidate PF-05089771 (34) which binds to a site in the voltage sensing domain.
BICYCLOAMINE-SUBSTITUTED-N-BENZENESULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS
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Paragraph 0179, (2015/06/11)
Disclosed are compounds of Formula A-a, or a salt thereof: Where "B1" and "R1" through "R5" are as defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-a or their salts, and methods of treating neuropathic pain disorders using the same.
BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS
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Page/Page column 96, (2013/05/22)
This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain
DIHYDROBENZOXAZINE AND TETRAHYDROQUINOXALINE SODIUM CHANNEL INHIBITORS
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Page/Page column 63; 64; 85, (2013/08/28)
The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
CHEMICAL COMPOUNDS
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Page/Page column 58, (2012/02/01)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7
Chemical Compounds
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Page/Page column 34, (2012/01/15)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
CHEMICAL COMPOUNDS
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Page/Page column 49, (2012/02/01)
The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 in
