DE3819870A1 - Pharmaceuticals based on fatty amino alcohols - Google Patents

Pharmaceuticals based on fatty amino alcohols

Info

Publication number
DE3819870A1
DE3819870A1 DE19883819870 DE3819870A DE3819870A1 DE 3819870 A1 DE3819870 A1 DE 3819870A1 DE 19883819870 DE19883819870 DE 19883819870 DE 3819870 A DE3819870 A DE 3819870A DE 3819870 A1 DE3819870 A1 DE 3819870A1
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DE
Germany
Prior art keywords
fatty amino
amino alcohols
sphingosine
medicament according
fatty
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
DE19883819870
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German (de)
Inventor
Wilhelm Dr Hoerrmann
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Individual
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Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Individual filed Critical Individual
Priority to DE19883819870 priority Critical patent/DE3819870A1/en
Publication of DE3819870A1 publication Critical patent/DE3819870A1/en
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7004—Monosaccharides having only carbon, hydrogen and oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

This patent application relates to the use of fatty amino alcohols and compounds thereof as pharmaceuticals for AIDS and other diseases.

Description

Die Erfindung betrifft ein Arzneimittel, das als Wirksubstanz mindestens ein Isomer eines Fett-amino-alkohols oder dessen pharmazeutisch annehmbaren Abkömmling gegebenenfalls zusammen mit üblichen Trägern und/oder Hilfsmitteln enthält.The invention relates to a medicament that acts as an active substance at least one isomer of a fatty amino alcohol or its pharmaceutically acceptable derivative if appropriate contains together with conventional carriers and / or auxiliaries.

Ein wichtiger solcher Fett-amino-alkohol ist das Sphingosin, wobei es sich um 2-amino-4-octadecen 1,3 diol handelt:An important such fatty amino alcohol is sphingosine, which is 2-amino-4-octadecene 1.3 diol:

Es ist besonders zu beachten, daß diese Fett-amino-alkohole in zahlreichen isomeren Formen auftreten können. Da beim Sphingosin das Kohlenstoffatom Nr. 2 ebenso wie das Kohlenstoffatom Nr. 3, die Amino- bzw. die Hydroxylgruppe tragend, beide asymmetrisch sind, ergeben sich bereits daraus 4 optische Isomere. Sie kombinieren sich mit 2 geometrischen Isomeren auf Grund der Doppelbindung. Es gibt also insgesamt 8 Isomere des Sphingosins.It is particularly important to note that these are fatty amino alcohols can occur in numerous isomeric forms. Since in sphingosine the carbon atom no the carbon atom No. 3, the amino or the hydroxyl group bearing, both are asymmetrical, already result 4 optical isomers. You combine with 2 geometric isomers due to the double bond. So there are a total of 8 isomers of sphingosine.

Eines dieser Isomere ist das trans-d-erythro-2-amino- 4-octadecen 1,3 diol.One of these isomers is the trans-d-erythro-2-amino 4-octadecene 1.3 diol.

Die erfindungsgemäßen Arzneimittel können die Fett-amino- alkohole, so auch das Sphingosin, auch in Form von pharmazeutisch verträglichen Abkömmlingen enthalten. Dazu gehören insbesondere die Ether, Ester, Amide, Salze und Säureadditionssalze der genannten Verbindungen. Typische Beispiele hierfür sind die N-acyl-Derivate mit gesättigten oder ungesättigten Fettsäuren, auch als Ceramide bezeichnet.The medicaments according to the invention can contain the fatty amino alcohols, including sphingosine, also in the form of pharmaceuticals compatible descendants included. This includes in particular the ethers, esters, amides, salts and acid addition salts of the connections mentioned. Typical examples for this are the N-acyl derivatives with saturated or unsaturated fatty acids, also known as ceramides.

Zusammen mit Phosphorylcholin, Phosphorylserin, Phosphorylethanolamin und Phosphorylinositol handelt es sich um Sphingomyeline. Together with phosphorylcholine, phosphorylserine, phosphorylethanolamine and phosphorylinositol Sphingomyeline.  

In Verbindung von Ceramid mit Zuckermolekülen (Glukose, Galaktose, N-acetyl-Glukosamin, N-acetyl-Galaktosamin, Mannose, Neuraminsäure und anderen) handelt es sich um Cerebroside, um Ganglioside, allgemein gesprochen um Glycolipide bzw. um Glycosphingolipide. Die genannten Verbindungen können durch die zusätzliche Gabe von Phosphoglyceriden und Plasmalogenen in ihrer Wirkung unterstützt werden.In connection with ceramide with sugar molecules (glucose, Galactose, N-acetyl-glucosamine, N-acetyl-galactosamine, Mannose, neuraminic acid and others) Cerebroside, around gangliosides, generally speaking around Glycolipids or around Glycosphingolipide. The compounds mentioned can be added Effect of phosphoglycerides and plasmalogens get supported.

Die hier genannten Verbindungen sind bekannt und können nach an sich bekannten Verfahren hergestellt werden.The compounds mentioned here are known and can be produced by methods known per se.

Das zentrale Molekül der Glycosphingolipide und Sphingomyeline ist das Sphingosin, da es den jeweiligen molekularen Gesamtkomplex in der Zellmembran verankert, wobei es säureamideartig an eine langkettige oder ungesättigte Fettsäure gebunden ist. Störungen in der molekularen Struktur des Sphingosins bzw. Ceramids haben deshalb schwerwiegende Folgen für die Zellmembran und ihre Anhangsgebilde.The central molecule of glycosphingolipids and sphingomyeline is the sphingosine because it is the respective molecular Total complex anchored in the cell membrane, whereby it acidic amide to a long chain or unsaturated Fatty acid is bound. Disorders in the molecular Therefore have the structure of sphingosine or ceramide serious consequences for the cell membrane and its appendages.

Die Hauptanwendungsgebiete dieses Arzneimittels sind AIDS (das erworbene Immung-Defekt-Syndrom), Drogensucht, Haemophilie und andere Erkrankungen, speziell des Nervensystems.The main areas of application of this drug are AIDS (the acquired immunodeficiency syndrome), drug addiction, Haemophilia and other diseases, especially of the nervous system.

Der Anmelder dieser Patentanmeldung kam auf Grund seiner Studien zu dem Ergebnis, daß bei all diesen Erkrankungen, besonders aber bei AIDS, Störungen in der Struktur und Funktion der körpereigenen Glycosphingolipide und Sphingomyeline äußerst wesentlich sind. Eine besonders wesentliche Rolle kommt dabei dem Sphingosinbestandteil dieser Substanzen zu.The applicant for this patent application came on the basis of his Studies have shown that with all of these diseases, but especially with AIDS, structural disorders and Function of the body's glycosphingolipids and sphingomyeline are extremely essential. A particularly essential one The role of the sphingosine component is this Substances too.

Störungen des Sphingosins und seiner Verbindungen stellen zumindest für einen Teil der Fälle eine biochemische Praedisposition für den Erwerb der genannten Krankheiten dar. Mit den erfindungsgemäßen Arzneimitteln ist eine günstige Beeinflussung einer solchen praedispositionellen Vorschädigung ("Risikogruppen") ebenso möglich, wie die einer klinisch manifesten Erkrankung.Make disorders of sphingosine and its compounds Biochemical predisposition at least for some of the cases for the acquisition of the diseases mentioned.  With the pharmaceuticals according to the invention is a cheap one Influencing such predispositional pre-damage ("Risk groups") as well as those clinically manifest disease.

Die Isomere der Fett-amino-alkohole können per se aber auch in der Form ihrer Ceramide, Sphingomyeline, Cerebroside oder Ganglioside zugeführt werden, wobei auch Bindungen an Proteine und Peptide möglich sind.The isomers of fatty amino alcohols can, however, per se also in the form of their ceramides, sphingomyeline, cerebroside or gangliosides are added, with bonds of proteins and peptides are possible.

Chemisch sind die genannten Verbindungen bekannt und insofern können sie auch nach bekannten chemischen Verfahren hergestellt werden. Das trifft auch auf die Trennung der Isomeren zu.The compounds mentioned are known chemically and in this respect you can also use known chemical methods getting produced. This also applies to the separation of the isomers too.

Neu aber ist der Gebrauch dieser Substanzen bei Krankheiten wie AIDS, Drogensucht, Haemophilie und Erkrankungen des Nervensystems.But what is new is the use of these substances in diseases like AIDS, drug addiction, hemophilia and diseases of the nervous system.

Nach allem unserem heutigen Wissen sind die genannten Verbindungen nicht toxisch und können deshalb in einem weiteren Dosierbereich angewandt werden. Ca. 100-400 mg/kg Körpergewicht gemessen am Fett-amino-alkohol können täglich gegeben werden.As far as we know today, the connections mentioned are non-toxic and can therefore be used in another Dosing range can be applied. Approx. 100-400 mg / kg Body weight as measured by fat amino alcohol can be taken daily are given.

Die Art der Zufuhr kann oral, anal und parenteral sein. Die Substanzen können in Pflanzenölen gelöst werden, in Kapseln oder Suppositorien eingeschlossen oder in Emulsionen gemischt werden. Ganz moderne Techniken, wie die Liposomen, können Verwendung finden.The mode of delivery can be oral, anal and parenteral. The substances can be dissolved in vegetable oils in Capsules or suppositories included or in emulsions be mixed. Very modern techniques like that Liposomes can be used.

Claims (5)

1. Arzneimittel, gekennzeichnet durch einen Gehalt an einem Isomer eines Fett-amino-alkohols oder dessen pharmazeutisch annehmbaren Abkömmling als Wirkstoff, gegebenenfalls neben üblichen Trägerstoffen, Hilfsmitteln und/oder Zusatzstoffen.1. Medicament, characterized by a content of an isomer of a fatty amino alcohol or its pharmaceutically acceptable derivative as an active ingredient, optionally in addition to conventional carriers, auxiliaries and / or additives. 2. Arzneimittel nach Anspruch 1, dadurch gekennzeichnet, daß der Fett-amino-alkohol ein Sphingosin ist.2. Medicament according to claim 1, characterized in that the fatty amino alcohol is a sphingosine. 3. Arzneimittel nach Anspruch 2, dadurch gekennzeichnet, daß das Isomer das trans-d-erythro-2-amino-4-octadecen 1,3 diol ist.3. Medicament according to claim 2, characterized in that the isomer is trans-d-erythro-2-amino-4-octadecene 1.3 diol. 4. Arzneimittel nach einem der Ansprüche 1 bis 3, dadurch gekennzeichnet, daß der Wirkstoff in Form von Ceramid, Sphingomyelin oder eines Glycolipids bzw. Glycosphingolipids vorliegt.4. Medicament according to one of claims 1 to 3, characterized characterized in that the active ingredient in the form of ceramide, Sphingomyelin or a glycolipid or Glycosphingolipids is present. 5. Arzneimittel nach einem der Ansprüche 1 bis 4, dadurch gekennzeichnet, daß die genannten Verbindungen zusätzlich in Form von Peptid-Eiweiß-Verbindungen vorliegen.5. Medicament according to one of claims 1 to 4, characterized characterized in that the compounds mentioned in addition are in the form of peptide-protein compounds.
DE19883819870 1987-06-12 1988-06-10 Pharmaceuticals based on fatty amino alcohols Ceased DE3819870A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
DE19883819870 DE3819870A1 (en) 1987-06-12 1988-06-10 Pharmaceuticals based on fatty amino alcohols

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE3719720 1987-06-12
DE19883819870 DE3819870A1 (en) 1987-06-12 1988-06-10 Pharmaceuticals based on fatty amino alcohols

Publications (1)

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DE3819870A1 true DE3819870A1 (en) 1988-12-29

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19909115A1 (en) * 1999-03-03 2000-09-07 Florian Lang Use of ceramides to treat cystic fibrosis
DE102018217334A1 (en) * 2018-10-10 2020-04-16 Harbins Ruhr Bioscience, Inc. Sphingoid base and / or active ingredient for use in the prophylaxis and / or therapy of a viral infection and / or viral infectious disease or disinfection, food / food supplements, feed / feed supplements and crop protection agents
US11298412B2 (en) 2020-07-16 2022-04-12 Harbins Ruhr Bioscience, Inc. Sphingoid compounds for prophylaxis and/or therapy of coronaviridae infection

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0072286A1 (en) * 1981-08-03 1983-02-16 FIDIA S.p.A. Organic amide compounds derived from nitrogenous lipids
WO1986003971A1 (en) * 1985-01-14 1986-07-17 Syn-Tek Ab Antiviral agents
EP0212400A2 (en) * 1985-08-13 1987-03-04 Solco Basel AG Method for the preparation of sphingosin derivatives
WO1987001939A1 (en) * 1985-10-01 1987-04-09 Angio-Medical Corporation Compositions containing lipid molecules with enhanced angiogenic activity

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0072286A1 (en) * 1981-08-03 1983-02-16 FIDIA S.p.A. Organic amide compounds derived from nitrogenous lipids
WO1986003971A1 (en) * 1985-01-14 1986-07-17 Syn-Tek Ab Antiviral agents
US4859769A (en) * 1985-01-14 1989-08-22 Symbicom Ab Antiviral agents
EP0212400A2 (en) * 1985-08-13 1987-03-04 Solco Basel AG Method for the preparation of sphingosin derivatives
WO1987001939A1 (en) * 1985-10-01 1987-04-09 Angio-Medical Corporation Compositions containing lipid molecules with enhanced angiogenic activity

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19909115A1 (en) * 1999-03-03 2000-09-07 Florian Lang Use of ceramides to treat cystic fibrosis
DE102018217334A1 (en) * 2018-10-10 2020-04-16 Harbins Ruhr Bioscience, Inc. Sphingoid base and / or active ingredient for use in the prophylaxis and / or therapy of a viral infection and / or viral infectious disease or disinfection, food / food supplements, feed / feed supplements and crop protection agents
US10688065B2 (en) 2018-10-10 2020-06-23 Harbins Ruhr Bioscience, Inc. Sphingoid compounds for prophylaxis and/or therapy of a viral infection
US12083079B2 (en) 2018-10-10 2024-09-10 Harbins Ruhr Bioscience, Inc. Sphingoid compounds for prophylaxis and/or therapy of a viral infection
US11298412B2 (en) 2020-07-16 2022-04-12 Harbins Ruhr Bioscience, Inc. Sphingoid compounds for prophylaxis and/or therapy of coronaviridae infection

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Legal Events

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8110 Request for examination paragraph 44
8125 Change of the main classification

Ipc: A61K 31/13

8131 Rejection