Delving into the Latest Updates on deCODE chemistry with Synapse

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Nervous System Diseases

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Small molecule drug

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Disease Domain	Count

Nervous System Diseases	1

Top 5 Drug Type	Count

Small molecule drug	1

Top 5 Target	Count

SMN2(Survival motor neuron protein)	1

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.

Investigation of critical process parameters (CPP) for production of Veliflapon (DG-031)

Author: Enache, Livia A. ; Stahl, Glenn L. ; Muellner, Frank W. ; Manna, Sukumar

Veliflapon is in clin. development for prevention of myocardial infarction via down-regulation of 5-lipoxygenase activating protein (FLAP), a principle component of the leukotriene B₄ pathway.In the spirit of Quality by Design, the synthetic process used for production of the API was investigated by selecting specific unit operations and determining the Critical Process Parameters (CPP).Parameters affecting the crystallization of the API, the final chem. step, and the penultimate chem. step were studied.The penultimate step, a stereoselective alkylation, was studied by Design of Experiment (DOE) and the results indicated that the alkylation step, once suspected of being sterically directed through the use of a chiral-directing menthol ester, may not be.Results from these studies are presented with emphasis on the final crystallization of the API and the DOE on the alkylation step.

EP-3 Receptor antagonists for Prostaglandin E-2 are novel potent antiplatelet agents that do not prolong bleeding

Author: Kiselyov, Alex

The platelet EP-3 receptor belongs to the family of GPCR′s.It facilitates platelet aggregation in response to multiple agonists.Similar to the P2Y12 receptor for ADP (ADP), the target of clopidogrel and prasugrel, EP3 regulates cAMP synthesis through the inhibitory G(i) pathway to reduce adenylyl cyclase activity.Current evidence suggests that EP-3 antagonists represent a novel class of anti-platelet agents, useful in addressing PGE-2 facilitated inflammatory risk of atherothrombosis in cardiovascular disease.We used a ligand-based design strategy to develop multiple classes of potent and selective EP-3 antagonists.Following optimization of our lead series, we have identified the clin. compound DG-041.It inhibits PGE-2 facilitation of platelet aggregation in vitro and ex vivo.DG-041 potentially has a superior safety profile to P(2)Y(12) antagonists as it does not affect bleeding times.Both discovery funnel and therapeutic window for DG041 will be discussed.

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 26 Dec 2024

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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