Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives
First Claim
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1. A pharmaceutical composition comprising:
- a) a C-21 modified epothilone compound of formula I;
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Abstract
Pharmaceutical compositions containing C-21 modified epothilone derivatives, methods for their preparation and dosing regimen for administration of these epothilone compounds are provided. The compositions are stable and readily prepared for administration by dissolution in aqueous vehicles suitable for intravenous administration. A process for formulating C-21 modified epothilone derivatives for oral and parenteral administration is disclosed.
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Citations
75 Claims
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1. A pharmaceutical composition comprising:
a) a C-21 modified epothilone compound of formula I; - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
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19. A method of preparing a pharmaceutical composition comprising the steps of:
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(a) preparing an aqueous solution containing a C-21 modified epothilone compound of formula I, a dibasic carboxylic acid, and a dextran polymer; (b) adjusting the pH of said solution to between about 5 and about 7; (c) lyophilizing said solution of step (b) to form a lyophile; and (d) drying said lyophile of step (c) wherein said C-21 modified epothilone compound of formula I is; - View Dependent Claims (20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 74, 75)
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- 35. A unit dose of a pharmaceutical composition comprising a sealed vial containing between about 10 mg and about 25 mg of citric acid, between about 50 mg and about 150 mg of dextran 40, and between about 5 mg and about 20 mg of [1S-[1R*,3R*(E),7R*,10S*, 11R*,12R*, 16S*]]-3-[2-[2-(aminomethyl)-4-thiazolyl]-1-methylethenyl]-7,11-dihydroxy-8,8,10,12,16-pentamethyl-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione.
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38. A method for treating cancer in a patient, wherein said cancer is selected from the group consisting of breast, head neck, sarcoma, colorectal, UPT, melanoma, esophagus, renal, cervix, thyroid, anal, ovarian, and colon cancer, comprising administering to said patient, by intravenous or oral administration, an effective amount of a pharmaceutical composition comprising:
a) a C-21 modified epothilone compound of formula I; - View Dependent Claims (39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73)
Specification