GB2226759A

GB2226759A - Pharmaceutical compositions containing lysine

Info

Publication number: GB2226759A
Application number: GB8900048A
Authority: GB
Inventors: Wilhelm Hoerrmann
Original assignee: Individual
Current assignee: Individual
Priority date: 1987-12-30
Filing date: 1989-01-04
Publication date: 1990-07-11
Also published as: DE3744542B4; GB8900048D0; CH678490A5; DE3744542A1

Description

1 0, k. f 1 .. - k - 4 0 1 Drugs Containing Isomers-of Hydroxylysine or

Lysine.

:z-k:2 (s,e:5 E' c 1 1 1 11 I- t -X D - A The invpntion relates to drugs containing, by way of effective agents, at least one isomer of hydroxylysine or lysine, or of their pharmaceutically acceptable derivatives, together with usual carriers and/or adjuvants, as the case may be. Note is to be take -of the fact that said isomer of hydroxylysine or lysine may be present in its L or D configuration, said L configuration being preferred; that the hydroxyl group may be located in various positions from beta to delta along the carbon chain, 'S&id delta position being the preferred one; and that as regards the ster.eo- isomeric position of said hydroxyl group in respect of an asymmetrically placed carbon atom, both isomers are pharmaceutically useful.

The effectiveness of said drugs may be enhanced by adding N-methylaminoethanol and/or N-dimethyl-aminoethanol, for instance as acid addition salts.

J.

(0 -'d 0 3 The structural formulae of the above compounds, already fl known, are shown only for the sake of completeness.

C1, 4 2 -/1 0 Al P Mr 5 t. H,: 1 L., H l2 N - 00 A_ 3 i,,l k t, - tJ -- t i, 1 ' 1! - 1 '1 4 _I The compounds as such are known and can be produced by methods already known.

The drugs according: to the invention may contain hydroxylysine or lysine isomers in the form of pharmaceutically compatible derivatives, and more particularly those converted, within the body, into the free form of said derivatives. This class of compounds includes more particularly alkali salts, alkaline earth salts, acid addition salts, esters, amides and ethers of hydroxylysine or lysine and their N-alkyl derivatives as well as the oligopeptides or polypeptides thereof.

I; I -- J..

(.0 The drugs according to the invention serve to treat the followi.Ag disorders, whether administered alone or in support of any conventional therapy. Currently, conventional therapies arb frequently insatisfactory, a fact demonstrated if only by the not insignificant number of cases where surgical intervention can still not be avoided.

0 Fields of application for the drugs according to the invention:

1. Affections of the venous system: above all dilatations and phlebitic changes in veins as well as variqoceles and hemorrhoids, affections of dura mater sinuses or similar syndromes.

2. Cardiac affections: above all endocarditis and its sequels but also myocarditis and its sequels, arrhythmias being most prominent among the latter ones.

3. Scarlatina, rheumatic fever, septic athropathies, erysipelas, impetigo, etc.

4. Prostatites and adnexites 5. Anal fissures 6. Dental caries 7. Neurological diseases and more particularly those entailing motor and/or sensitivity disturbances.

8. Hernias ---4 0 6 In all,cases mentioned above, the effective principle resides in a strengthening, caused by the drugs according to the invention., of intra and extra-cellular fibre systems.

The drugs according to the invention are to be administered in ways basically similar to those normally employed in usual amino acid treatment, i.e. preferentially per os or intravenously, or by the central intravenous route. Administration by way of tablets, coated tablets, injection or infusion soluti'ons-. would likewise be identical.

With superficially accessible foci, localized administration in the form of solutions or powders or salves or similar compounds might be considered.

17 In view of the fact that the compounds in question are non-toxic, dosages may range widely even though they might initially be based on normally used therapeutical amino acid dosage levels of between 0.01 and 0.1 g of substance per kg of bodyweight.

Contraindications applicable to all amino acids will have to be taken into account.

Pharmaceutical production and processing will be performed in the usual Mnner, all legal rules and regulations concerning purity of substance;sterilization, absence of pyrogens, etc. being observed.

1 1 claims:., 1. Drugs containing, as active ingredients, at least one isomer of hydroxylysine or lysine, or one of their pharmaceutically acceptable derivatives, if nec-essary together with usual carriers and/or adjuvants.

Claims

2. Drugs according to Claim 1, characterized in that hydroxylysine or

lysine will be present as L-form compounds.

3. Drugs according to one of Claims 1 - 2, characterized in that the hydroxyl group of hydroxylysine is loca - ted in the delta position.

4. Drugs according to one of Claims 1 - 3, characterized in that the hydroxyl group of hydroxylysine is in one of the two isomeric alpha or beta positions.

Enhancement of the effectiveness of a drug according to Claims 1 - 4 by the addition of N-methyl-aminoethanol and/or N-dimethyl-aminoethanol.

6. Enhancement of the effectiveness of a drug according to Claims 1 - 5, characterized in that said added substances, N-methyl-aminoethanol and/or N-dimethyl-aminoethanol, are present in the form of acid addition saits.

Published 1990 at The Patent Office. State House, 66'71 High Holborn. London WClR 4TP_ Further copiesmaybe obtainedfrom ThePatentOffice Sales Branch, St Mary Cray. Orpington. Kent BR5 3RD. Printed by Multiplex techniques ltd, St Mary Cray. Kent, Con. V87