1033221-38-3Relevant academic research and scientific papers
Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152)
O'Neill, David J.,Adedoyin, Adedayo,Bray, Jenifer A.,Deecher, Darlene C.,Fensome, Andrew,Goldberg, Joel A.,Harrison, Jim,Leventhal, Liza,Mann, Charles,Mark, Lilly,Nogle, Lisa,Sullivan, Nicole R.,Spangler, Taylor B.,Terefenko, Eugene A.,Trybulski, Eugene J.,Uveges, Albert J.,Vu, An,Whiteside, Garth T.,Zhang, Puwen
experimental part, p. 6824 - 6831 (2011/12/04)
Sequential modification of the previously identified 4-[3-aryl-2,2-dioxido- 2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols led to the identification of a new series of 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro- 2,1,3-benzothiadiazole 2,2-dioxides that are potent and selective inhibitors of the norepinephrine transporter over both the serotonin and dopamine transporters. One representative compound 10b (WYE-114152) had low nanomolar hNET potency (IC50 = 15 nM) and good selectivity for hNET over hSERT (>430-fold) and hDAT (>548-fold). 10b was additionally bioavailable following oral dosing and demonstrated efficacy in rat models of acute, inflammatory, and neuropathic pain.
ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE
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Page/Page column 147-148, (2008/12/06)
The present invention is directed to aryl sulfamide derivatives of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
