Delving into the Latest Updates on WYE-114152 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

WYE-114152

Target

NET

Action

inhibitors

Mechanism

NET inhibitors(Norepinephrine transporter inhibitors)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

InflammationNeuralgia

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Pfizer Inc.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC18H20FN3O3S

InChIKeyUIKJCHWTULEUKX-CQSZACIVSA-N

CAS Registry1033219-23-6

Author: O'Neill, David J. ; Zhang, Pu-Wen ; Terefenko, Eugene A. ; Nogle, Lisa ; Mann, Charles ; Trybulski, Eugene J. ; Goldberg, Joel A. ; Leventhal, Liza ; Mark, Lilly ; Adedoyin, Adedayo ; Uveges, Albert J. ; Whiteside, Garth T. ; Bray, Jenifer A. ; Vu, An ; Fensome, Andrew ; Sullivan, Nicole R. ; Spangler, Taylor B. ; Harrison, Jim ; Deecher, Darlene C.

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 (IC(50) = 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.

100 Deals associated with WYE-114152

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