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Nervous System Diseases

Small molecule drug

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A glimpse into the focused therapeutic areas

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Disease Domain	Count

Nervous System Diseases	2

Top 5 Drug Type	Count

Small molecule drug	2

Top 5 Target	Count

SMN2(Survival motor neuron protein)	1
DCPS(Scavenger mRNA-decapping enzyme DcpS)	1

A series of novel 1,7-disubstituted oxyindoles were shown to be potent and selective EP(3) receptor antagonists. Variation of substitution pattern at the C-3 position of indole enhanced in vitro metabolic stability of the resulting derivatives. Series 27a-c showed >1000-fold selectivity over a panel of prostanoid receptors including IP, FP, EP(1), EP(2) and EP(4). These agents also featured low CYP inhibition and good activity in the functional rat platelet aggregation assay.

01 Jan 2010·Drugs of the Future

EP3 receptor antagonists: Potential for improving safety in the antiplatelet therapy field

Author: Singh, J. ; Kiselyov, A. S.

A review.Current antiplatelet therapies offer significant benefits for the treatment of patients at risk for recurrent cardiovascular events.However, clin. data suggest that many of these agents lead to an increased risk of severe or fatal hemorrhage by affecting general platelet function.It has been suggested that targeting the inflammatory component of the disease instead may address this issue.Human genetic data from peripheral arterial occlusive disease (PAOD), heart attack and stroke converged on the identification of the EP₃ receptor as a target, linking variations in the gene encoding EP₃ to an increased risk for the disease.Several small-mol. EP₃ antagonists employed either as monotherapy or in combination with clopidogrel and aspirin have been shown to inhibit platelet aggregation at the site of lesions in the vasculature, without increasing bleeding time.This suggests that targeting the inflammatory mechanism of arterial thrombosis mediated by the prostaglandin E₂ (PGE₂)-EP₃ receptor system may lead to a new generation of anti-platelet drugs with an enhanced safety and efficacy profile.

01 Mar 2009·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

3-Acrylamide-4-aryloxyindoles: Synthesis, biological evaluation and metabolic stability of potent and selective EP3 receptor antagonists

Q4 · MEDICINE

Article

Author: Ramirez, Jose ; Zhou, Nian ; Kiselyov, Alex S. ; Zhang, Jun ; Zeller, Wayne ; Andresson, Torkell ; Gurney, Mark E. ; Halldorsdottir, Guethrun ; Singh, Jasbir ; Onua, Emmanuel ; Palsdottir, Guethrun

A series of potent and selective EP(3) receptor antagonists are described. Utilizing a pharmacophore model developed for the EP(3) receptor, a series of 3,4-disubstituted indoles were found to be efficient ligands for this target. These compounds showed high selectivity over IP, FP and other EP receptors. An optimized molecule 7c featured a sound profile and potency in the functional rat and human platelet aggregation assays.

100 Deals associated with deCODE chemistry

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100 Translational Medicine associated with deCODE chemistry

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Pipeline

Pipeline Snapshot as of 31 Jan 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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