Claims
- 1. A hydrated salt of N,N'-diacetylcystine, wherein the hydrated salt has the formula ##STR2## in which the N,N'-diacetylcystine is the D-, L-, or meso form, or any mixture thereof, R.sup.+ is the protonated form of lysine, and x is 2, designating the dihydrate.
- 2. A hydrated salt as claimed in claim 1, in which the N,N'-diacetylcystine is the L-form.
- 3. A hydrated salt as claimed in claim 1, wherein said salt is di-L-lysinium N,N'-diacetyl-L-cystinate dihydrate.
- 4. A process for the preparation of a hydrated salt of N,N'-diacetylcystine, wherein the hydrated salt has the formula ##STR3## in which the N,N'-diacetylcystine is the D-, L-, or meso form, or any mixture thereof, R.sup.+ is the protonated form of lysine designating the dihydrate, said process, comprising
- a) providing a first solution comprising i) N-acetyl cysteine, ii) lysin or the protonated form thereof, iii) a solvent, wherein the solvent is water or alcohol, and iv) optionally a catalytic amount of an alkali metal hydroxide;
- (b) applying an oxidant to the solution; and
- (c) adding to the first solution a second solution comprising ethanol, or adding the first solution to a second solution comprising a mixture of ethanol and water, wherein R.sup.+ is the protonated form of lysine and x is 2.
- 5. A therapeutic composition comprising as active ingredient a hydrated salt as claimed in claim 1.
- 6. A therapeutic composition as claimed in claim 5, formulated for administration by inhalation from a dry powder inhaler.
- 7. Di-ammonium-N,N'-diacetyl-L-cystinate monohydrate.
- 8. Di-ammonium-N,N'-diacetyl-L-cystinate dihydrate.
- 9. A method for the treatment of a disease involving an anergy of the immune response, an aberrant immune response or an ineffective immune response in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 1.
- 10. A method for the treatment of chronic bronchitis in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 1.
- 11. A method for the treatment of a malignant disease in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 1.
- 12. A method for the treatment of a chronic infection in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 1.
- 13. A method for the treatment of a chronic hepatitis B or C viral infection in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 1.
- 14. A therapeutic composition comprising as an active ingredient the hydrated salt of claim 2.
- 15. A therapeutic composition comprising as an active ingredient the hydrated salt of claim 3.
- 16. A therapeutic composition as claimed in claim 14, formulated for administration by inhalation from a dry powder inhaler.
- 17. A therapeutic composition as claimed in claim 15, formulated for administration by inhalation from a dry powder inhaler.
- 18. A method for the treatment of a disease involving an anergy of the immune response, an aberrant immune response or an ineffective immune response in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 2.
- 19. A method for the treatment of a disease involving an anergy of the immune response, an aberrant immune response or an ineffective immune response in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 3.
- 20. A method for the treatment of chronic bronchitis in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 2.
- 21. A method for the treatment of chronic bronchitis in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 3.
- 22. A method for the treatment of a malignant disease in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 2.
- 23. A method for the treatment of a malignant disease in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 3.
- 24. A method for the treatment of a chronic infection in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 2.
- 25. A method for the treatment of a chronic infection in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 3.
- 26. A method for the treatment of a chronic hepatitis B or C viral infection in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 2.
- 27. A method for the treatment of a chronic hepatitis B or C viral infection in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 3.
- 28. A hydrated salt of N,N'-diacetylcystine, wherein the hydrated salt has the formula ##STR4## in which the N,N'-diacetylcystine is the D-, L-, or meso form, or any mixture thereof, R.sup.+ is the protonated form of ammonia and x is 1, 1.5, or 2, designating the monohydrate, sesquihydrate, and dihydrate, respectively.
- 29. A hydrated salt as claimed in claim 28, in which the N,N'-diacetylcystine is the L-form.
- 30. A process for the preparation of a hydrated salt of N,N'-diacetylcystine, wherein the hydrated salt has the formula ##STR5## in which the N,N'-diacetylcystine is the D-, L-, or meso form, or any mixture thereof, R.sup.+ is the protonated form of ammonia and x is 1, 1.5, or 2, designating the monohydrate, sesquihydrate, and dehydrate, respectively, comprising
- (a) providing a first solution comprising i) N-acetyl cystine, ii) ammonia or the protonated form thereof, iii) a solvent, wherein the solvent is water or alcohol, and iv) optionally a catalytic amount of an alkali metal hydroxide;
- (b) applying an oxidant to the solution; and
- (c) (i) adding to the first solution a second solution, wherein the second solution comprises acetone, R.sup.+ is the protonated form of ammonia, and x is 1; or (ii) adding to the first solution a second solution comprising ethanol, or adding the first solution to a second solution comprising a mixture of ethanol and water, wherein R.sup.+ is the protonated form of ammonia and x is 2.
- 31. The process of claim 4, wherein step (c)(i) is followed.
- 32. The process of claim 4, wherein step (c)(ii) is followed.
- 33. A therapeutic composition comprising as active ingredient a hydrated salt as claimed in claim 28.
- 34. A therapeutic composition as claimed in claim 28, formulated for administration by inhalation from a dry powder inhaler.
- 35. A method for the treatment of a disease involving an anergy of the immune response, an aberrant immune response or an ineffective immune response in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 28.
- 36. A method for the treatment of chronic bronchitis in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 28.
- 37. A method for the treatment of a malignant disease in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 28.
- 38. A method for the treatment of a chronic infection in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 29.
- 39. A method for the treatment of a chronic hepatitis B or C viral infection in a mammal, said method comprising administering to the mammal a therapeutically effective amount of the hydrated salt of claim 28.
Priority Claims (2)
Number |
Date |
Country |
Kind |
9602416 |
Jun 1996 |
SEX |
|
9602419 |
Jun 1996 |
SEX |
|
Parent Case Info
This is a continuation of International Patent Application No. PCT/SE97/01069, with an international filing date of Jun. 17, 1997, now pending.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/SE97/01069 |
6/17/1997 |
|
|
12/18/1997 |
12/18/1997 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO97/48679 |
12/24/1997 |
|
|
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5385904 |
Andersson et al. |
Jan 1995 |
|
Continuations (1)
|
Number |
Date |
Country |
Parent |
PCTSE9701069 |
Jun 1997 |
|