Delving into the Latest Updates on BAY-545 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

A2bR

Mechanism

A2bR antagonists(Adenosine A2b receptor antagonists)

Therapeutic Areas

Respiratory Diseases

Active Indication

Pulmonary Fibrosis

Inactive Indication-

Originator Organization

Bayer AG

Active Organization

Bayer AG

Inactive Organization-

Drug Highest PhaseDiscovery

First Approval Date-

Regulation-

Structure

Molecular FormulaC18H22F3N3O4S

InChIKeyNTYVAKNEYLJAPT-UHFFFAOYSA-N

CAS Registry1699717-32-2

The A_2B adenosine receptor is a G protein-coupled receptor that belongs to the four member family of adenosine receptors: A₁, A_2A, A_2B, A₃. While adenosine-mediated A_2B receptor signaling attenuates acute inflammation, facilitates tissue adaptation to hypoxia, and induces increased ischemia tolerance under conditions of an acute insult, persistently elevated adenosine levels and A_2B receptor signaling are characteristics of a number of chronic disease states. In this report we describe the discovery of certain thienouracils (thieno[2,3-d]pyrimidine-2,4(1H,3H)-diones) as antagonists of the A_2B adenosine receptor by high-throughput screening from our corporate substance collection. The structure optimization of the initial screening hits led to BAY-545, an A_2B receptor antagonist that was suitable for in vivo testing. The structure optimization work, SAR that was derived from there, as well as the properties of BAY-545 are also described. In vivo efficacy of BAY-545 was demonstrated in two models of lung fibrosis and data is presented.

100 Deals associated with BAY-545

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