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Overview

A review with 129 referencesFactor Xa is a key enzyme in the production of thrombin from its precursor prothrombin and is an important target for antithrombotic drug development.The patient literature for the last four to five years illustrates a variety of peptide and non-peptide Factor Xa inhibitors, including small proteins isolated from natural sources, rationally designed peptides and peptidomimetics based on substrate cleavage sites, and non-peptide small mols. derived from screening and rational design.This report reviews the status of the patent literature in the field of Factor Xa inhibitors through 1998.

01 May 1998·The Journal of Organic Chemistry

Solid-Phase Synthesis of Heterocycles Containing an 1-Acyl-3-oxopiperazine Skeleton

Author: Weichsel, Aleksandra ; Vojkovský, Tomáš ; Pátek, Marcel

A new acetal-type linker was synthesized by attachment of bromoacetaldehyde di-Et acetal to the TentaGel OH resin.Transformation of the resulting bromoacetal resin into the corresponding aminoacetals, followed by acylation with a number of amino acids provided solid phase-bound peptoid-aldehyde dialkyl acetals.Subsequent acylation with a number of acyl components containing different nucleophilic centers afforded polymer-bound products in nearly quant. overall yields.Upon treatment with formic acid, new bi-, tri-, and tetracyclic derivatives of 1-acyl-3-oxopiperazines were obtained via a tandem N-acyliminium ion cyclization-nucleophilic addition reaction sequence.General availability of amines and amino acids enhances the utility of these reactions for the construction of large combinatorial libraries of peptidomimetics and heterocycles bearing one or two heteroatoms.

01 Oct 1997·Tetrahedron Letters

Polymer-supported synthesis of diverse perhydro-1,4-diazepine-2,5-diones

Author: Weichsel, Aleksandra S. ; Krchnak, Viktor

The chem., synthesis of model compounds, selection of building blocks, and synthesis of a library of 1,4,7-trisubstituted perhydro-1,4-diazepine-2,5-diones are described.Secondary diamines and Fmoc protected amino alcs. were attached to chlorotrityl resin and the amino group acylated with Fmoc-Asp(OAll).The Fmoc group was cleaved, and the amino group alkylated.Then bromoacetic acid was coupled to the amino group and the bromide displaced by primary amines.After removal of the allyl ester function, the seven membered ring was closed upon mild activation of the carboxyl group.Products were cleaved from the resin by TFA vapor.

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Pipeline

Pipeline Snapshot as of 22 Feb 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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