Delving into the Latest Updates on JNJ-26990990 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

N-type calcium channel x Sodium channels

Mechanism

N-type calcium channel inhibitors(Calcium channel inhibitor N-types inhibitors), Sodium channels blockers

Therapeutic Areas

Nervous System Diseases

Active Indication

Epilepsy

Inactive Indication-

Originator Organization

Johnson & Johnson

Active Organization

Johnson & Johnson

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

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Structure

Molecular FormulaC9H10N2O2S2

InChIKeyAWSKBQNOSRREEY-UHFFFAOYSA-N

CAS Registry877316-38-6

Author: Parker, Michael H. ; Qin, Ning ; Milewski, Michael E. ; Malatynska, Ewa ; Lubin, Mary Lou ; Cuyckens, Filip ; Smith-Swintosky, Virginia L. ; Klein, Brian ; Leclercq, Laurent ; White, H. Steve ; Brenneman, Douglas ; Liu, Yi ; Maryanoff, Bruce E. ; Reitz, Allen B. ; Herb, Mark ; Finley, Michael F. A. ; Iannucci, Robert ; McComsey, David F. ; Huang, Yifang

In seeking broad-spectrum anticonvulsants to treat epilepsy and other neurological disorders, we synthesized and tested a group of sulfamide derivatives (4a-k, 5), which led to the clinical development of 4a (JNJ-26990990). This compound exhibited excellent anticonvulsant activity in rodents against audiogenic, electrically induced, and chemically induced seizures, with very weak inhibition of human carbonic anhydrase-II (IC(50) = 110 microM). The pharmacological profile for 4a supports its potential in the treatment of multiple forms of epilepsy, including pharmacoresistant variants. Mechanistically, 4a inhibited voltage-gated Na(+) channels and N-type Ca(2+) channels but was not effective as a K(+) channel opener. The pharmacokinetics and metabolic properties of 4a are discussed.

Organic & Biomolecular ChemistryQ3 · CHEMISTRY

The anticonvulsant sulfamide JNJ-26990990 and its S,S-dioxide analog strongly inhibit carbonic anhydrases: solution and X-ray crystallographic studies

Q3 · CHEMISTRY

Article

Author: Alterio, Vincenzo ; Winum, Jean-Yves ; De Simone, Giuseppina ; Riccio, Vincenzo ; Carta, Fabrizio ; Di Fiore, Anna ; Supuran, Claudiu T.

Inhibition and X-ray crystallographic data for the binding of JNJ-26990990 and itsS,S-dioxide analog to hCAs have been reported.

100 Deals associated with JNJ-26990990

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