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Overview

AbstractVarious cell-penetrating peptides have been discovered recently that can translocate across plasma membranes and can even carry large cargo molecules into the cells. Because under physiological conditions most of these peptides carry considerable positive charges due to the presence of basic amino acids such as arginine, we decided to investigate whether molecular transporters composed of permanently charged side-chains also possess such cell penetrating ability. Arginine-rich oligomers that have a backbone with increased flexibility due to incorporation of non-α-amino acids (ε-aminocaproic acid) have been found to be effective molecular transporters. Here, we report the preparation of analogue structures by replacing the arginine residues with the quaternary form of a novel redox amino acid (Nys+) that contain a trigonelline moiety; it has already been shown possible to replace the original basic amino acid side-chain of neuropeptides without significant activity-loss due to the sufficiently close steric and electronic analogy between the new Nys+ and the original side-chains (in their protonated form, e.g., Arg+, Lys+). A nonamer analogue showed transporter activity resulting in increased cellular uptake in human carcinoma (HeLa) cells.

01 May 2006·Carbohydrate ResearchQ4 · CHEMISTRY

Glycosidation of 2,5-anhydro-3,4-di-O-benzyl-d-mannitol with different glucopyranosyl donors. A comparative study

Q4 · CHEMISTRY

Article

Author: Medgyes, Gabor ; Tegdes, Aniko ; Boros, Sandor ; Kuszmann, Janos

2,5-Anhydro-3,4-di-O-benzyl-D-mannitol was glycosylated using different donors such as tetra-O-acetyl-alpha-D-glucopyranosyl bromide in the presence of Hg(CN)(2), the corresponding beta-thiophenylglycoside in the presence of NIS and TfOH as well as the alpha- and beta-trichloroimidate with TMSOTf as promoter. The resulting mixtures were analyzed by HPLC and the following main components were isolated and characterized: 2,5-anhydro-3,4-di-O-benzyl-1-O-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)-d-mannitol; 6-O-acetyl-2,5-anhydro-3,4-di-O-benzyl-1-O-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)-D-mannitol; 2,5-anhydro-3,4-di-O-benzyl-1,6-bis-O-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)-D-mannitol; 2,5-anhydro-3,4-di-O-benzyl-1-O-[-2-O-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)-3,4,6-tri-O-acetyl-beta-D-glucopyranosyl]-6-O-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)-D-mannitol and 2,5-anhydro-3,4-di-O-benzyl-1,6-bis-O-(3,4,6-tri-O-acetyl-1,2-O-ethylidene-2'-yl-alpha-D-glucopyranosyl)-D-mannitol. The latter compound representing a bis-orthoester might be a common intermediate in all the investigated reactions, as its rearrangement and/or decomposition can yield all of the isolated compounds.

01 Jan 2006·Current pharmaceutical design

Current Animal Models of Bronchial Asthma

Review

Author: Kurucz, I. ; Szelenyi, I.

Human asthma is on the rise worldwide. The necessity to develop effective treatments against it requires an organized effort which covers every aspect of the disease from the pathological alterations via the genetic background to the use and development of active remedies. In these processes animal experiments have served an indispensable role. As asthma is not a natural disease in the animal kingdom the variety for artificially established animal models is quite wide. The possible selection ranges from the laboratory mouse to the horse, it includes ferret and sheep and even favorite pets such as cats and dogs. The large number of the models indicates that to some extent they might not be appropriate or it means that there is no generally accepted model of human asthma. Whatever the reason for this diversity animal models helped us to understand the detailed pathogenesis of some aspects of the disease, they helped us to develop compounds which are more active then previously used ones, and these models proved to us that human asthma is a unique, possibly species-specific disease the eradication of which requires a huge effort. This enormous task should include the collaboration of the clinical and basic research for the development of improved, advanced animal models, which in turn could strengthen our understanding about human asthma.

100 Deals associated with Ivax Drug Research Institute LLC

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100 Translational Medicine associated with Ivax Drug Research Institute LLC

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Pipeline

Pipeline Snapshot as of 23 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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Current Projects

Drug(Targets)	Indications	Global Highest Phase

GYKI-16084 ( ADRA1 x ADRA2 )	Prostatic Hyperplasia More	Discontinued
GYKI-66323 ( thrombin )	Thrombosis More	Discontinued
GYKI-66319 ( thrombin )	Thrombosis More	Pending
GYKI-24417 ( Lipid peroxidase )	-	Pending
GYKI-16036 ( Potassium channel )	Arrhythmias, Cardiac More	Pending