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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 2004·Die Pharmazie

Synthesis of a polysulfated heparin degradation product.

Article

Author: Kuszmann, J ; Boros, S ; Medgyes, G

Two suitable methods for the synthesis of the heparin degradation product 2,5-anyhydro-3-O-(alpha-L-idopyranosyluronate)-D-mannitol hexa O-sulfate are reported. The synthesis pathways start from D-glucose and D-glucosamine.

01 May 2004·Die Pharmazie

Anti-inflammatory effect and soft properties of etiprednol dicloacetate (BNP-166), a new, anti-asthmatic steroid.

Article

Author: Mészáros, S ; Török, K ; Bodor, N ; Németh, K ; Zubovics, Z ; Horváth, K ; Nagy, Z ; Kurucz, I

In vitro and in vivo anti-inflammatory properties and soft characteristics of etiprednol dicloacetate (BNP-166) a new steroid, which has been developed for the treatment of asthma, were investigated in this study. The compound effectively decreased cytokine production in lipopolysaccharide stimulated lymphocytes and attenuated lectin-induced proliferation of blood mononuclear cells in tissue culture. In an animal model of allergen sensitized and challenged Brown Norway rats, using topical treatment, etiprednol dicloacetate substantially attenuated the extent of allergen induced bronchoalveolar fluid eosinophilia. At every examined parameter its pharmacological effects were comparable to those of budesonide. By means of in vitro biological and analytical methods the soft character of BNP-166 was also investigated. The anti-inflammatory effect of etiprednol dicloacetate in vitro was shown to be the function of the quantity of serum components, present in the assay. This loss of activity was most likely the result of the fast metabolism of etiprednol dicloacetate, which in the presence of sera could have been demonstrated by LC/MS/MS. Our data indicate that the significant local effect of the compound will very likely be accompanied with a drastically reduced systemic activity indicating an encouraging selectivity of the pharmacological action of etiprednol dicloacetate.

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 24 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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Current Projects

Drug(Targets)	Indications	Global Highest Phase

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