Claims
- 1. A crystalline R-guanidine of (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}-propanoate wherein R is straight or branched alkyl, straight or branched alkenyl, or straight or branched alkynyl, each of which is optionally substituted with one or more halogen(s), —OH, —CF3, —CN, C1-4-alkoxy, C1-4-alkylthio, —SCF3, —OCF3, —CONH2, —CSNH2, NH2 or COOH.
- 2. Crystalline Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}-propanoate.
- 3. Crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}-propanoate.
- 4. The crystalline form of (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate having substantially the same NMR spectrum as described above.
- 5. A process for the preparation of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate according to claims 3-8, which process comprises dissolving (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoic acid in appropriate organic solvent or a mixture of solvents and adding (L)-arginine in crystal form, as a suspension or dissolved in an appropiate solvent or mixture of solvents and crystallizing the resulting salt from the solution.
- 6. A process for the preparation of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate according to claims 3-8, which process comprises dissolving (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoic acid in an organic solvent or mixture of solvents and adding (L)-arginine dissolved in an appropiate solvent and crystallizing the resulting salt from the solution.
- 7. A process for the preparation of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate according to claims 3-8, which process comprises dissolving (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoic acid dissolved in an organic solvent and adding (L)-arginine dissolved in water and crystallizing the resulting salt from the solution.
- 8. A pharmaceutical composition comprising, as an active ingredient, (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate together with a pharmaceutically acceptable carrier or diluent.
- 9. A pharmaceutical composition according to claim 8 in unit dosage form, comprising from about 0.05 to about 100 mg, preferably from about 0.1 to about 50 mg of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate.
- 10. A pharmaceutical composition useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR), the composition comprising, as an active ingredient, crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate or together with a pharmaceutically acceptable carrier or diluent.
- 11. A pharmaceutical composition useful in the treatment and/or prevention of diabetes and/or obesity, the composition comprising, as an active ingredient, crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate or together with a pharmaceutically acceptable carrier or diluent.
- 12. A pharmaceutical composition according to any one of the claims 8-11 for oral, nasal, transdermal, pulmonary or parenteral administration.
- 13. A method for the treatment of ailments, which method comprises administering to a subject in need thereof an effective amount of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate or of a pharmaceutical composition according to claims 8-12.
- 14. A method for the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR), which method comprises administering to a subject in need thereof an effective amount of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate or of a pharmaceutical composition according to claims 8-12.
- 15. A method for the treatment and/or prevention of diabetes and/or obesity which method comprises administering to a subject in need thereof an effective amount of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate or of a pharmaceutical composition according to claims 8-12.
- 16. The method according to claim 13, 14 or 15, wherein the effective amount of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate is in the range of from about 0.05 to about 100 mg per day, preferably from about 0.1 to about 50 mg per day.
- 17. Use of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate for the preparation of a medicament.
- 18. Use of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate for the preparation of a medicament useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
- 19. Use of crystalline (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate for the preparation of a medicament useful in the treatment and/or prevention of diabetes and/or obesity.
Priority Claims (2)
Number |
Date |
Country |
Kind |
PA 1999 00536 |
Apr 1999 |
DK |
|
PCT/IB99/00681 |
Apr 1999 |
US |
|
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims priority under 35 U.S.C. 119 of Danish application PA 1999 00536 filed on Apr. 20, 1999, of U.S. Provisional application No. 60/132,636 filed on May 5, 1999 and of PCT/IB99/00681 filed on Apr. 16, 1999, the contents of which are fully incorporated herein by reference.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60132636 |
May 1999 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
09550843 |
Apr 2000 |
US |
Child |
10209567 |
Jul 2002 |
US |