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1. WO1993016713 - COMPOSES A USAGE MEDICAL

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

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CLAIMS

1. The use of a muramyl peptide compound in the manufacture of a medicament for the treatment, prevention or management of toxicity.

2. The use of a muramyl peptide compound in the manufacture of a medicament for enhancing hepatic metabolism of toxins.

3. The use of a muramyl peptide compound in the manufacture of a medicament for enhancing the activity of the cytochrome P450 system.

4. The use as claimed in any one of claims 1 to 3, wherein the muramyl peptide compound conforms to general formula I:


wherein:

R1 represents a hydrogen atom or a C1-C22 acyl group; R2 represents a hydrogen atom or a C1-C22 acyl group; R3 represents a hydrogen atom or a C1-C6 alkyl group;

R4 represents a C1-C21 alkyl group or a C6 or C10 aryl group;
R5 represents a hydrogen atom; and
R represents the residue of an amino acid or a linear peptide built up of from 2 to 6 amino acid residues, at least one of the residues being optionally substituted with a lipophilic group.

5. The use as claimed in claim 4, wherein the compound of general formula I has any or all or any compatible combination of the following substituents:

each of R1 and R2 independently represents a C1-C3 acyl group such as acetyl;
R3 represents a C1-C4 alkyl group such as methyl or ethyl;
R4 represents a C1-C6 alkyl group, particularly a C1- C4 alkyl group, such as methyl or ethyl, or a phenyl group;
R represents a mono-, di- or tri-peptide.

6. The use as claimed in any one of claims 1 to 3 , wherein the muramyl peptide compound conforms to general formula II:


wherein :

R represents a residue of an amino acid or a linear peptide built of from 2 to 6 amino acid residues, at least one of the residues being optionally substituted with a lipophilic group; and

n is 1 or 2.

7. The use as claimed in claim 6, wherein n is 1.

8. The use as claimed in any one of claims 4 to 7, wherein the proximal amino acid residue (or the only amino acid residue, if there is only one) is a residue of an L-amino acid.

9. The use as claimed in claim 8, wherein the proximal amino acid residue (or the only amino acid residue, if there is only one) is a residue of L-alanine.

10. The use as claimed in any one of claims 4 to 9, wherein the second amino acid residue from the proximal end of the peptide is of the D-configuration.

11. The use as claimed in claim 10, wherein the said second amino acid residue is of D-glutamic or D-aspartic acid or a mono-, di- or mixed C1-C22 (preferably C1-C6) alkyl ester, amide or C1-C4 alkyl amide thereof.

12. The use as claimed in any one of claims 9 to 11, wherein the said second amine acid residue is D-isoglutaminyl or D-glutamyl.

13. The use as claimed in any one of claims 4 to 12, wherein the third amino acid residue from the proximal end of the peptide is in the L-configuration.

14. The use as claimed in claim 13, wherein the third amino acid residue is L-alanyl or L-lysyl.

15. The use as claimed in any one of claims 4 to 14, wherein the amino acid residue or linear peptide is optionally substituted with at least one lipophilic group.

16. The use as claimed in any one of claims 1 to 5, wherein the muramyl peptide compound is:

prototype muramyl dipeptide (N-acetylmuramyl-L- alanyl-d-isoglutamine);

muroctasin, otherwise known as MDP-Lys (L18) (N2-(N- acetylmuramyl-L-alanyl-D-isoglutaminyl)-N6-stearoyl- L-lysine);

MTP-PE (N-acetyl-muramyl-L-alanyl-D-isoglutaminyl-L- alanyl-2-(1',2'-dipalmitoyl-sn-glycero-3'-hydroxyphosphoryloxy)ethylamide, monosodium);

murabutide (N-acetylmuramyl-L-alanyl-D-glutamine-α- N-butyl ester); or

t-MDP (N-acetylmuramyl-L-threonyl-D-isoglutamine) .

17. The use as claimed in claim any one of claims 1 to 3 or claim 6, wherein the muramyl peptide compound is N-acety1-glucosaminyl-N-acetyl-muramyl-L-alanyl-D-isoglutamine (GMDP).

18. The use as claimed in any one of claims 1 to 3 or claim 6, wherein the muramyl peptide compound is N-acetyl-glucosaminyl-N-acetyl-muramyl-L-alanyl-D-glutamic acid (GMDP-A).

19. The use as claimed in any one of claims 1 to 18, wherein the toxicity is caused by ethanol or a metabolite thereof.

20. The use as claimed in any one of claims 1 to 18, wherein the toxicity is caused by a hypnotic and/or sedative.

21. The use as claimed in any one of claims 1 to 18, wherein the toxicity is caused by an anaesthetic.

22. The use as claimed in any one of claims 1 to 18, wherein the toxicity is caused by an opioid.

23. The use as claimed in any one of claims 1 to 18, wherein the toxicity results from drug abuse.

24. The use as claimed in any one of claims 1 to 18, wherein the toxicity arises from in vivo metabolism.

25. A method for the treatment, prevention or management of toxicity, the method comprising administering to a patient an effective amount of a muramyl peptide compound.

26. A method for enhancing hepatic metabolism of toxins, the method comprising administering to a patient an effective amount of a muramyl peptide compound.

27. A method for enhancing the activity of the cytochrome P450 system, the method comprising administering to a patient an effective amount of a muramyl peptide compound.

28. A method as claimed in any one of claims 25 to 27, wherein the muramyl peptide compound is as defined in any one of claims 4 to 18.

29. A method as claimed in any one of claims 25 to 28, wherein the administration is oral.

30. A method as claimed in claim 29, wherein the daily dosage is in the range of from 0.1 to 100 mg per day.

31. A method as claimed in any one of claims 25 to 28, wherein the administration is parenteral.

32. A method as claimed in claim 31, wherein the daily dosage is in the range of from 0.01 to 1 mg per day.