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Claims for Patent: 5,698,582

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Claims for Patent: 5,698,582

Title: Compositions containing taxane derivatives
Abstract:This invention relates to compositions containing taxane derivatives, consisting of a solution of such derivatives in a surfactant. These compositions can be used to prepare perfusion solutions.
Inventor(s): Bastart; Jean-Pierre (Lesigny, FR), Dupechez; Thierry (Villemoisson Sur Orge, FR), Fabre; Jean-Louis (Paris, FR)
Assignee: Rhone-Poulenc Rorer S.A. (Antony, FR)
Application Number:08/398,011
Patent Claims: 1. A composition comprising a taxane derivative dissolved in a surfactant selected from polysorbate or polyethoxylated castor oil, and essentially free or free of ethanol.

2. The composition of claim 1, wherein said polyethoxylated castor oil is a non-ionic solubilizer and emulsifier containing glycerol-polyethylene glycol ricinoleate, fatty acid esters of polyethylene glycol, polyethylene glycols, and ethoxylated glycerol.

3. The composition of claim 1, said composition being a stock solution and containing less than 5% by volume ethanol.

4. The composition of claim 3, said composition containing less than 2% by volume ethanol.

5. The composition of claim 1, said composition being a perfusion containing less than 0.5 mg/ml of said taxane derivative of claim 1, less than 1 ml/l of said ethanol, and less than 15 ml/l of said surfactant.

6. The composition of claim 1, said composition being a perfusion containing less than or equal to 1 mg/ml of said taxane derivative of claim 1, and less than 1 ml/l of said ethanol.

7. A stock solution comprising a taxane derivative dissolved in a surfactant selected from polysorbate or polyethoxylated castor oil, wherein said stock solution contains from 10 to 200 mg/ml of said taxane derivative, and wherein said stock solution is essentially free or free of ethanol.

8. The stock solution of claim 7, wherein said stock solution contains from 10 to 80 mg/ml of said taxane derivative.

9. The stock solution of claim 8, wherein said stock solution contains from 12 to 80 mg/ml of said taxane derivative.

10. The stock solution of claim 9, wherein said stock solution contains from 20 to 80 mg/ml of said taxane derivative.

11. The stock solution of claim 7, wherein said surfactant is polysorbate.

12. The stock solution of claim 7, wherein said surfactant is polyethoxylated castor oil.

13. The stock solution of claim 12, wherein said polyethoxylated castor oil is a non-ionic solubilizer and emulsifier containing glycerol-polyethylene glycol ricinoleate, fatty acid esters of polyethylene glycol, polyethylene glycols, and ethoxylated glycerol.

14. A composition comprising the compound 4.alpha.,10.beta.-diacetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1.beta.-h ydroxy-7.beta.,8.beta.-methylene-9-oxo-19-nor-11-taxen-13.alpha.-yl 3-t-butoxycarbonylamino-2-hydroxy-3-phenyl-(2R,3S)-propionate dissolved in a surfactant selected from polysorbate or polyethoxylated castor oil, wherein said composition is essentially free or free of ethanol.

15. The composition of claim 14, wherein said polyethoxylated castor oil is a non-ionic solubilizer and emulsifier containing glycerol-polyethylene glycol ricinoleate, fatty acid esters of polyethylene glycol, polyethylene glycols, and ethoxylated glycerol.

16. The composition of claim 14, said composition being a stock solution containing less than 5% by volume ethanol.

17. The composition of claim 16, said composition containing less than 2% by volume ethanol.

18. The composition according to claim 16, said composition containing from 1 to about 2.5% by volume ethanol.

19. The composition of claim 14, said composition being a stock solution and containing from 10 to 80 mg/ml of said compound of claim 14.

20. The composition of claim 19, said composition containing from 20 to 80 mg/ml of said compound.

21. The composition of claim 14, said composition being a stock solution and containing from 6 to 20 mg/ml of said compound of claim 14.

22. The composition of claim 14, said composition being a perfusion containing less than 0.5 mg/ml of said taxane derivative of claim 14, less than 1 ml/l of said ethanol, and less than 15 ml/l of said surfactant.

23. The composition of claim 14, said composition being a perfusion containing less than or equal to 1 mg/ml of said taxane derivative of claim 14, and less than 1 ml/l of said ethanol.

24. The composition of claim 14, wherein said surfactant is polysorbate.

25. The composition of claim 14, wherein said surfactant is polyethoxylated castor oil.

26. The composition of claim 25, wherein said polyethoxylated castor oil is a non-ionic solubilizer and emulsifier containing glycerol-polyethylene glycol ricinoleate, fatty acid esters of polyethylene glycol, polyethylene glycols, and ethoxylated glycerol.

27. A composition comprising the compound 4.alpha.,10.beta.-diacetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1.beta.-h ydroxy-7.beta.,8.beta.-methylene-9-oxo-19-nor-11-taxen-13.alpha.-yl 3-t-butoxycarbonylamino-2-hydroxy-3-phenyl-(2R,3S)-propionate dissolved in a surfactant selected from polysorbate or polyethoxylated castor oil, wherein said composition is a stock solution containing from 6 to 200 mg/ml of said compound, and wherein said composition is essentially free or free of ethanol.

28. The composition of claim 27, wherein said composition contains from 10 to 200 mg/ml of said compound.

29. The composition of claim 28, wherein said surfactant is polysorbate.

30. The composition of claim 28, wherein said surfactant is polyethoxylated castor oil.

31. The composition of claim 30, wherein said polyethoxylated castor oil is a non-ionic solubilizer and emulsifier containing glycerol-polyethylene glycol ricinoleate, fatty acid esters of polyethylene glycol, polyethylene glycols, and ethoxylated glycerol.

32. A composition comprising a compound of formula (I): ##STR2## in which R.sub.2 represents a hydrogen atom and R.sub.1 forms a single bond together with the methyl carbon atom situated in the .alpha. position, so they together form a cyclopropane ring,

one of R.sub.3 and R.sub.4 represents a hydrogen atom and the other represents a hydroxy radical, or

R.sub.3 and R.sub.4 taken together form an oxo radical,

R.sub.5 and R.sub.6 each represents a hydrogen atom or one of R.sub.5 and R.sub.6 represents a hydrogen atom and the other represents a hydroxy, acyloxy or an alkoxymethylcarbonyloxy radical, or

R.sub.5 and R.sub.6 taken together form an oxo radical,

R.sub.7 represents an alkoxy, alkenyloxy, cycloalkoxy or phenyl radical and

Ar represents

a phenyl radical optionally substituted by one or several atoms or radicals which are identical or different and are selected from halogen, alkyl, alkoxy, dialkylamino, acylamino, and trifluoromethyl, or

a 5-membered heterocyclic radical with one or more identical or different heteroatoms selected from nitrogen, oxygen and sulfur

wherein said compound of formula (I) is dissolved in a surfactant selected from polysorbate or polyethoxylated castor oil, and further wherein said composition is essentially free or free of alcohol.

33. The composition of claim 32, wherein the alkyl radical and the alkyl portion of the radicals selected from alkoxymethylcarbonyloxy, alkoxy, and dialkylamino are independently straight or branched and contain 1 to 8 carbon atoms and the alkenyloxy radical contains 2 to 8 carbon atoms.

34. A perfusion comprising less than or equal to 1 mg/ml of said compound of formula (I) of claim 32, and less than 1 ml/l of said ethanol and less than 15 ml/l of surfactant.

35. The composition of claim 32, wherein R.sub.3 and R.sub.4 taken together form an oxo radical; either (i) R.sub.6 represents a hydrogen atom and R.sub.5 represents a hydrogen atom or a hydroxy, acetyloxy or methoxyacetyloxy radical, or (ii) R.sub.5 and R.sub.6 taken together form an oxo radical;

R.sub.7 represents a t.butoxy or a phenyl radical; and

Ar is a phenyl radical.

36. The composition of claim 32, said composition being a stock solution containing less than 5% by volume ethanol.

37. The composition of claim 36, said composition containing less than 2% by volume ethanol.

38. A composition comprising a compound of formula (I): ##STR3## in which R.sub.2 represents a hydrogen atom and R.sub.1 forms a single bond together with the methyl carbon atom situated in the .alpha. position, so they together form a cyclopropane ring,

one of R.sub.3 and R.sub.4 represents a hydrogen atom and the other represents a hydroxy radical, or

R.sub.3 and R.sub.4 taken together form an oxo radical,

R.sub.5 and R.sub.6 each represents a hydrogen atom or one of R.sub.5 and R.sub.6 represents a hydrogen atom and the other represents a hydroxy, acyloxy or an alkoxymethylcarbonyloxy radical, or

R.sub.5 and R.sub.6 taken together form an oxo radical,

R.sub.7 represents an alkoxy, alkenyloxy, cycloalkoxy or phenyl radical and

Ar represents

a phenyl radical optionally substituted by one or several atoms or radicals which are identical or different and are selected from halogen, alkyl, alkoxy, dialkylamino, acylamino, and trifluoromethyl, or

a 5-membered heterocyclic radical with one or more identical or different heteroatoms selected from nitrogen, oxygen and sulfur

wherein said compound of formula (I) is dissolved in a surfactant selected from polysorbate or polyethoxylated castor oil, and wherein said composition is a stock solution containing from 6 to 200 mg/ml of said compound of formula (I), and wherein said composition is essentially free or free of ethanol.

39. The composition of claim 38, wherein said composition contains from 10 to 200 mg/ml of said compound of formula (I).

40. The composition of claim 38, wherein said composition contains from 6 to 20 mg/ml of said compound of formula (I).

41. The composition of claim 39, wherein said surfactant is polysorbate.

42. The composition of claim 39, wherein said surfactant is polyethoxylated castor oil.

43. The composition of claim 42, wherein said polyethoxylated castor oil is a non-ionic solubilizer and emulsifier containing glycerol-polyethylene glycol ricinoleate, fatty acid esters of polyethylene glycol, polyethylene glycols, and ethoxylated glycerol.

44. A stock solution comprising a compound of formula (I): ##STR4## in which R.sub.1 and R.sub.2 each represent a hydrogen atom or one of R.sub.1 and R.sub.2 represents a hydrogen atom and the other represents a hydroxy, acyloxy or acylcarbonyloxy radical, or

R.sub.2 represents a hydrogen atom and R.sub.1 forms a single bond together with the methyl carbon atom situated in the .alpha. position, so they together form a cyclopropane ring,

one of R.sub.3 and R.sub.4 represents a hydrogen atom and the other represents a hydroxy radical,

or R.sub.3 and R.sub.4 taken together form an oxo radical,

R.sub.5 and R.sub.6 each represents a hydrogen atom or one of R.sub.5 and R.sub.6 represents a hydrogen atom and the other represents a hydroxy, acyloxy or an alkoxymethylcarbonyloxy radical, or

R.sub.5 and R.sub.6 taken together form an oxo radical,

R.sub.7 represents an alkoxy, alkenyloxy, cycloalkoxy or phenyl radical and

Ar represents

a phenyl radical optionally substituted by one or several atoms or radicals which are identical or different and are selected from halogen, alkyl, alkoxy, dialkylamino, acylamino, and trifluoromethyl, or

a 5-membered heterocyclic radical with one or more identical or different heteroatoms selected from nitrogen, oxygen and sulfur, and

wherein said compound of formula (I) is dissolved in a surfactant selected from polysorbate or polyethoxylated castor oil, and further wherein said composition is essentially free or free of alcohol.

45. A composition comprising a taxane derivative dissolved in a polyethoxylated vegetable oil, wherein said composition is essentially free or free of ethanol.

46. A stock solution comprising a taxane derivative dissolved in a polyethoxylated vegetable oil, wherein said stock solution contains from 10 to 200 mg/ml of said taxane derivative and is essentially free or free of ethanol.

47. A composition comprising a compound of formula (I): ##STR5## in which R.sub.2 represents a hydrogen atom and R.sub.1 forms a single bond together with the methyl carbon atom situated in the .alpha. position, so they together form a cyclopropane ring,

one of R.sub.3 and R.sub.4 represents a hydrogen atom and the other represents a hydroxy radical, or

R.sub.3 and R.sub.4 taken together form an oxo radical,

R.sub.5 and R.sub.6 each represents a hydrogen atom or one of R.sub.5 and R.sub.6 represents a hydrogen atom and the other represents a hydroxy, acyloxy or an alkoxymethylcarbonyloxy radical, or

R.sub.5 and R.sub.6 taken together form an oxo radical,

R.sub.7 represents an alkoxy, alkenyloxy, cycloalkoxy or phenyl radical and

Ar represents

a phenyl radical optionally substituted by one or several atoms or radicals which are identical or different and are selected from halogen, alkyl, alkoxy, dialkylamino, acylamino, and trifluoromethyl, or

a 5-membered heterocyclic radical with one or more identical or different heteroatoms selected from nitrogen, oxygen and sulfur

wherein said compound of formula (I) is dissolved in polyoxyethylated vegetable oil, and further wherein said composition is essentially free or free of alcohol.

48. A composition comprising a compound of formula (I): ##STR6## in which R.sub.2 represents a hydrogen atom and R.sub.1 forms a single bond together with the methyl carbon atom situated in the .alpha. position, so they together form a cyclopropane ring,

one of R.sub.3 and R.sub.4 represents a hydrogen atom and the other represents a hydroxy radical, or

R.sub.3 and R.sub.4 taken together form an oxo radical,

R.sub.5 and R.sub.6 each represents a hydrogen atom or one of R.sub.5 and R.sub.6 represents a hydrogen atom and the other represents a hydroxy, acyloxy or an alkoxymethylcarbonyloxy radical, or

R.sub.5 and R.sub.6 taken together form an oxo radical,

R.sub.7 represents an alkoxy, alkenyloxy, cycloalkoxy or phenyl radical and

Ar represents

a phenyl radical optionally substituted by one or several atoms or radicals which are identical or different and are selected from halogen, alkyl, alkoxy, dialkylamino, acylamino, and trifluoromethyl, or

a 5-membered heterocyclic radical with one or more identical or different heteroatoms selected from nitrogen, oxygen and sulfur

wherein said compound of formula (I) is dissolved in polyoxyethylated vegetable oil, and wherein said composition is a stock solution containing from 6 to 200 mg/ml of said compound of formula (I) and wherein said composition is essentially free of ethanol.

49. A composition comprising the compound 4.alpha.,10.beta.-diacetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1.beta.-h ydroxy-7.beta.,8.beta.-methylene-9-oxo-19-nor-11-taxen-13.alpha.-yl 3-t-butoxycarbonylamino-2-hydroxy-3-phenyl-(2R,3S)-propionate dissolved in polyethoxylated vegetable oil, wherein said composition is essentially free or free of ethanol.

50. A composition comprising the compound 4.alpha.,10.beta.-diacetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1.beta.-h ydroxy-7.beta.,8.beta.-methylene-9-oxo-19-nor-11-taxen-13.alpha.-yl 3-t-butoxycarbonylamino-2-hydroxy-3-phenyl-(2R,3S)-propionate dissolved in polyethoxylated vegetable oil, wherein said composition is a stock solution containing from 6 to 200 mg/ml of said compound and is essentially free or free of ethanol.

51. The stock solution of claim 44, wherein one of R.sub.3 and R.sub.4 represents a hydrogen atom and the other represents a hydroxy radical.

52. The stock solution of claim 44, wherein R.sub.5 and R.sub.6 each represents a hydrogen atom or one of R.sub.5 and R.sub.6 represents a hydrogen atom and the other represents an alkoxymethylcarbonyloxy radical, or R.sub.5 and R.sub.6 taken together form an oxo radical.

53. The stock solution of claim 44, wherein R.sub.7 represents an alkenyloxy or cycloalkoxy radical.
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