Delving into the Latest Updates on ZK-813039 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

factor Xa

Mechanism

factor Xa inhibitors(Factor Xa inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Venous Thrombosis

Originator Organization

Bayer AG

Active Organization-

Inactive Organization

Pfizer Inc.

Bayer AG

Drug Highest PhaseDiscontinuedPhase 1

First Approval Date-

Regulation-

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Structure

Molecular FormulaC23H19Cl3N6O3S

InChIKeyLLHSZBPXQIOQJJ-UHFFFAOYSA-N

CAS Registry229336-92-9

Author: Shaw, Kenneth J. ; Sullivan, Mark E. ; Kochanny, Monica J. ; Ewing, Janice ; Cheeseman, Sarah ; Walters, Janette ; Morrissey, Michael M. ; Karanjawala, Rushad ; White, Kathy A. ; Wang, Yi-Xin ; Zhao, Zuchun ; Sakata, Steven T. ; Rumennik, Galina ; Wu, Shung C. ; Lee, Wheeseong ; Morser, John ; Ye, Bin ; Post, Joseph ; Fitch, Richard ; Arnaiz, Damian O. ; Chou, Yuo-Ling ; Vergona, Ron ; Light, David ; Griedel, Brian D. ; Liang, Amy ; Whitlow, Marc ; Adler, Marc ; Subramanyam, Babu ; Sacchi, Karna L. ; Lentz, Dao ; Dole, William P.

There remains a high unmet medical need for a safe oral therapy for thrombotic disorders. The serine protease factor Xa (fXa), with its central role in the coagulation cascade, is among the more promising targets for anticoagulant therapy and has been the subject of intensive drug discovery efforts. Investigation of a hit from high-throughput screening identified a series of thiophene-substituted anthranilamides as potent nonamidine fXa inhibitors. Lead optimization by incorporation of hydrophilic groups led to the discovery of compounds with picomolar inhibitory potency and micromolar in vitro anticoagulant activity. Based on their high potency, selectivity, oral pharmacokinetics, and efficacy in a rat venous stasis model of thrombosis, compounds ZK 814048 (10b), ZK 810388 (13a), and ZK 813039 (17m) were advanced into development.

100 Deals associated with ZK-813039

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