Delving into the Latest Updates on AZD-2716 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

sPLA2(AstraZeneca)

Target

sPLA2

Mechanism

sPLA2 inhibitors(Secretory phospholipase A2 inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Coronary Artery Disease

Inactive Indication-

Originator Organization

AstraZeneca AB

Active Organization

AstraZeneca AB

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC24H23NO3

InChIKeyPXRCDPVYRPKGGI-MRXNPFEDSA-N

CAS Registry1845753-81-2

AbstractWe report a stereoselective conversion of terminal alkynes to α‐chiral carboxylic acids using a nickel‐catalyzed domino hydrocarboxylation‐transfer hydrogenation reaction. A simple nickel/BenzP* catalyst displayed high activity in both steps of regioselective hydrocarboxylation of alkynes and subsequent asymmetric transfer hydrogenation. The reaction was successfully applied in enantioselective preparation of three nonsteroidal anti‐inflammatory profens (>90 % ees) and the chiral fragment of AZD2716.

13 Oct 2016·ACS Medicinal Chemistry LettersQ3 · MEDICINE

Discovery of AZD2716: A Novel Secreted Phospholipase A₂ (sPLA₂) Inhibitor for the Treatment of Coronary Artery Disease

Q3 · MEDICINE

Article

Author: Dekker, Niek ; Pettersen, Daniel ; Larsson, Lars-Olof ; Nordberg, Peter ; Karlsson, Ulla ; Dahlström, Mikael ; Hurt-Camejo, Eva ; Knerr, Laurent ; Selmi, Nidhal ; Rosengren, Birgitta ; Sandmark, Jenny ; Castaldo, Marie ; Starke, Ingemar ; Giordanetto, Fabrizio

Expedited structure-based optimization of the initial fragment hit 1 led to the design of (R)-7 (AZD2716) a novel, potent secreted phospholipase A₂ (sPLA₂) inhibitor with excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and minimized safety risk. Based on accumulated profiling data, (R)-7 was selected as a clinical candidate for the treatment of coronary artery disease.

100 Deals associated with AZD-2716

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