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Fe(III) Complex Compounds For The Treatment And Prophylaxis Of Iron Deficiency Symptoms And Iron Deficiency Anemias

a technology of complex compounds which is applied in the field of complex compounds for the treatment and prophylaxis of iron deficiency symptoms and iron deficiency anemia, can solve the problems of low stability, less suitable for oral application, and nearly not applicable in pharmaceutical compositions, and achieves stable bioavailable iron complexes, treatment and prophylaxis, and low cognitive efficiency.

Active Publication Date: 2016-01-21
VIFOR INT AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to stable bioavailable iron complexes that can be used as a medicament for the treatment and prevention of iron deficiency symptoms and its associated anemias in humans and veterinary medicine. The technical effects of this invention are that it provides a reliable and effective treatment for iron deficiency and its related health issues, and the use of the compounds is safe and effective.

Problems solved by technology

However, in particular the hydroxypyridone Fe complex compounds exhibit a comparably low water solubility, which makes them less suitable for the oral application.
The cyclopentane or cyclohexane carboxamide iron(III) complexes shown therein exhibit, however, a very low stability which makes them nearly not applicable in pharmaceutical compositions and thus renders them unsuitable for medical applications.
These iron salts are very problematic in that, in part, they are highly incompatible (up to 50%) in the form of nausea, vomiting, diarrhea and also obstipation and cramps.
In the development of the new complexes, the stability improvement particularly in neutral aqueous media should not be achieved at the expense of solubility, since for oral use the solubility is a very important criterion.

Method used

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  • Fe(III) Complex Compounds For The Treatment And Prophylaxis Of Iron Deficiency Symptoms And Iron Deficiency Anemias
  • Fe(III) Complex Compounds For The Treatment And Prophylaxis Of Iron Deficiency Symptoms And Iron Deficiency Anemias
  • Fe(III) Complex Compounds For The Treatment And Prophylaxis Of Iron Deficiency Symptoms And Iron Deficiency Anemias

Examples

Experimental program
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Effect test

examples

[0122]The invention is illustrated in more detail by the following examples. The examples constitute only an exemplary illustration and it lies within the knowledge of a skilled person to extend the specific examples to further claimed compounds. The designation of the example names have been determined with the program ChemDraw Ultra Version 12.0.

Starting Compounds:

[0123]The starting compounds used in the examples were obtained as follows.

A. 3-Hydroxy-N,N-dimethylisonicotinamide

[0124]

[0125]0.09 mol (15 g) 3-hydroxyisonicotinic acid ethyl ester (in analogy to J. D. Crum, C. H. Fuchsman, J. Heterocyclic Chem. 1966, 3, 252-256) and 0.9 mol dimethylamine (160 ml 5.6 M solution in ethanol) were heated in a pressure vessel to 120° C. for 5 h. Then the reaction mixture was evaporated until dryness and the crude product was recrystallized from 200 ml tetrahydrofuran and 100 ml ethanol. 10 g (67% yield) of the title compound were obtained.

[0126]IR (in substance, cm−1): 1626, 1601, 1573, 150...

preparation examples

Example 1

Tris-(3-hydroxy-N,N-dimethylisonicotinamide) iron(III) complex

[0199]

[0200]72 mmol (12 g) 3-hydroxy-N,N-dimethylisonicotinamide were provided in 250 ml ethanol and 72 mmol sodium methanolate (30% solution in methanol) were added. 24 mmol (3.89 g) FeCl3 (anhydrous) were dissolved in 20 ml ethanol, added dropwise and stirred for 2 h. The reaction mixture was filtered off, the filtrate was evaporated at a rotary evaporator and the residue was dried. 13.6 g (96% Fe-yield) of the title compound were obtained.

[0201]IR (in substance, cm−1): 1574, 1525, 1473, 1394, 1308, 1273, 1236, 1206, 1161, 1059, 928, 867, 850, 826, 790, 732, 711, 652, 615.

[0202]CHN-elementary analysis: C, 51.11; H, 5.44; N, 14.37.

[0203]Fe-content: 9.47% [m / m]

2. Tris-(3-Hydroxyisonicotinamide) iron(III) complex

[0204]

[0205]9 mmol (1.37 g) 3-hydroxyisonicotinamide were dissolved in 60 ml methanol under slight heating and 3 mmol (0.49 g) FeCl3 (anhydrous) as well as 9 mmol sodium methanolate (1.67 ml of a 30% solut...

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PUM

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Abstract

The invention relates to iron(III) complex compounds and pharmaceutical compositions comprising them for the use as medicaments, in particular for the treatment and / or prophylaxis of iron deficiency symptoms and iron deficiency anemias.

Description

INTRODUCTION[0001]The invention relates to iron(III)-3-hydroxy-isonicotinamide complex compounds and pharmaceutical compositions comprising them for the use as medicaments, in particular for the treatment and / or prophylaxis of iron deficiency symptoms and iron deficiency anemias.BACKGROUND[0002]Iron is an essential trace element for almost all organisms and is relevant in particular with respect to growth and the formation of blood. The balance of the iron metabolism is in this case primarily regulated on the level of iron recovery from hemoglobin of ageing erythrocytes and the duodenal absorption of dietary iron. The released iron is taken up via the intestine, in particular via specific transport systems (DMT-1, ferroportin, transferrin, transferrin receptors), transferred into the circulation and thereby conveyed to the appropriate tissues and organs.[0003]In the human body, the element iron is of great importance for oxygen transport, oxygen uptake, cell functions such as mitoch...

Claims

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Application Information

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IPC IPC(8): A61K31/555A61K45/06
CPCA61K45/06A61K31/555A61K31/4412A61K33/26A61P1/04A61P25/00A61P25/04A61P25/24A61P37/02A61P7/06A61K2300/00
Inventor BARK, THOMASBUHR, WILMBURCKHARDT, SUSANNABURGERT, MICHAELCANCLINI, CAMILLODURRENBERGER, FRANZFUNK, FELIXGEISSER, PETER O.KALOGERAKIS, ARISMAYER, SIMONAPHILIPP, ERIKSIEBER, DIANASCHMITT, JORGSCHWARZ, KATRINREIM, STEFAN
Owner VIFOR INT AG
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