Delving into the Latest Updates on AZD-2716 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

sPLA2(AstraZeneca), AZD-2716

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

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

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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