TREA

Pharmaceutical composition comprising a bi-cyclic compound and method for stabilizing the bi-cyclic compound

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Information

  • Patent Application
  • 20070172522
  • Publication Number
    20070172522
  • Date Filed
    January 23, 2007
    17 years ago
  • Date Published
    July 26, 2007
    17 years ago
Information
Abstract
Disclosed is a method for stabilizing a pharmaceutically active bi-cyclic compound of formula (i):
Description
Claims
  • 1. A pharmaceutical composition comprising a bi-cyclic compound represented by the formula (I):
  • 2. The composition of claim 1, wherein the bi-cyclic compound is the compound of the formula (I), wherein A is —COOH or functional derivative thereof;X1 and X2 are halogen;W1 is ═O, or where one of R4 and R5 is hydrogen, another is hydroxy;W2 is where R4 and R5 are both hydrogen;Z is oxygen;R1 is a saturated or unsaturated bivalent unsubstituted lower-medium aliphatic hydrocarbon residue,R2 is a saturated or unsaturated unsubstituted lower-medium aliphatic hydrocarbon residue;R3 is a hydrogen.
  • 3. The composition of claim 1, wherein the polyol is glycerin, propylene glycol or polyethylene glycol.
  • 4. The composition of claim 1, wherein said fatty acid ester is propylene glycol fatty acid ester.
  • 5. The composition of claim 1, wherein the fatty acid ester is an ester of a fatty acid and a C1-6 monovalent alcohol.
  • 6. The composition of claim 5, wherein said fatty acid ester is isopropyl palmitate.
  • 7. The composition of claim 1, which is in a dosage form suitable for oral administration.
  • 8. The composition of claim 7, which is formulated as capsule.
  • 9. A method for stabilizing a bi-cyclic compound represented by the formula (I):
  • 10. The method of claim 9, wherein A is —COOH or functional derivative thereof;X1 and X2 are halogenW1 is ═O, or where one of R4 and R5 is hydrogen, another is hydroxy;W2 is where R4 and R5 are both hydrogen;Z is oxygen;R1 is a saturated or unsaturated bivalent unsubstituted lower-medium aliphatic hydrocarbon residue;R2 is a saturated or unsaturated unsubstituted lower-medium aliphatic hydrocarbon residue; andR3 is hydrogen.
  • 11. The method of claim 9, wherein the polyol is glycerin, propylene glycol or polyethylene glycol.
  • 12. The method of claim 9, wherein said fatty acid ester is propylene glycol fatty acid ester.
  • 13. The method of claim 9, wherein the fatty acid ester is an ester of a fatty acid and C1-6 monovalent alcohol.
  • 14. The method of claim 13, wherein said fatty acid ester is isopropyl palmitate.
  • 15. The method of claim 9, which is in a dosage form suitable for oral administration.
  • 16. The method of claim 15, which is formulated as capsule.
  • 17. A soft gelatin capsule formulation of a bi-cyclic compound of formula (I):
  • 18. The formulation of claim 17, wherein A is —COOH or functional derivative thereof;X1 and X2 are halogen;W1 is ═O, or where one of R4 and R5 is hydrogen, another is hydroxy;W2 is where R4 and R5 are both hydrogen;Z is oxygen;R1 is a saturated or unsaturated bivalent unsubstituted lower-medium aliphatic hydrocarbon residue;R2 is a saturated or unsaturated unsubstituted lower-medium aliphatic hydrocarbon residue;R3 is hydrogen.
  • 19. The formulation of claim 17, wherein the pharmaceutically acceptable vehicle is a fatty acid ester or a polyol.
  • 20. The formulation of claim 19, wherein the fatty acid ester is a glyceride.
  • 21. The formulation of claim 19, wherein the polyol is glycerin.
  • 22. A method for stabilizing a bi-cyclic compound of formula (I):
Provisional Applications (1)
Number Date Country
60761362 Jan 2006 US