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06/22/06
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USPTO Class 514
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#20060135404
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Water soluble paclitaxel derivatives
Title:
Water soluble paclitaxel derivatives
Related Patent Categories:
Drug, Bio-affecting And Body Treating Compositions
,
Designated Organic Active Ingredient Containing (doai)
,
Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai
Brief Patent Description
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Full Patent Description
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Patent Claims
The Patent Description & Claims data below is from USPTO Patent Application 20060135404, Water soluble paclitaxel derivatives.
1. A composition comprising (i) a conjugate of a therapeutic agent, contrast agent or drug and (ii) a water-soluble amino acid polymer in which there is more than one different type of amino acid residue and in which greater than 50% of the amino acid residues comprise glutamic acid and/or aspartic acid and/or lysine.
2. A composition as claimed in claim 1, wherein the drug is a chemotherapeutic or antiangiogenic drug, preferably a taxoid, tamoxifen, etoposide, teniposide, fludarabine, doxorubicin, daunomycin, emodin, 5-fluorouracil, FUDR, estradiol, camptothecin, a retinoid, verapamil, an epothilone or a cyclosporine.
3. A composition as claimed in claim 1, wherein the drug is a taxoid which is paclitaxel or taxotere.
4. A composition as claimed in claim 1, which contains, in addition to glutamic acid and/or aspartic acid and/or lysine residues, residues derived from at least one of the other amino acids provided through the genetic code, and/or residues derived from at least one of 2-Aminoadipic acid, 3-Aminoadipic acid, beta-alanine, 2-Aminobutyric acid, 4-Aminobutyric, 6-Aminocaproic acid, 2-Aminoheptanoic acid, 2-Aminoisobutyric acid, 3-Aminoisobutyric acid, 2-Aminopimelic acid, 2-4-Diaminobutyric acid, Desmosine, 2,2'-Diaminopimelic acid, 2,3-Diaminopropionic acid, N-Ethylgylcine, N-Ethylasparagine, Hydroxylysine, allo-Hydroxylysine, 3-Hydroxyproline, 4-Hydroxyproline, Isodesmosine, allo-Isoleucine, N-Methylglycine, N-Methylisoleucine, 6-N-Methyllysine, N-Methylvaline, Norvaline, Norleucine, and Ornithine.
5. A composition as claimed in claim 1, wherein said copolymer has a molecular weight of from about 5,000 to about 100,000 daltons, preferably from about 20,000 to about 80,000 daltons, more preferably from about 25,000 to about 50,000 daltons.
6. A composition as claimed in claim 1, wherein the amount of the drug is at least 10% (w/w), preferably from about 10% to about 40% (w/w), based on the mass of said conjugate.
7. A composition as claimed in claim 1, wherein said amino acid residues are in the I form.
8. A composition as claimed in claim 1 for use in a method of therapy.
9. A composition as claimed in claim 1 for use in the treatment of breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.
10. Use of a composition as claimed in claim 1 in the manufacture of a medicament for treating breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.
11. A water soluble amino acid chain or polymer comprising a mixture of glutamic acid, aspartic acid, and/or lysine having about 25%, about 26%, about 27%, about 28%, about 29%, about 30%, about 31%, about 32%, about 33%, about 34%, about 35%, about 36%, about 37%, about 38%, about 39%, about 40%, about 41%, about 42%, about 43%, about 44%, about 45%, about 46%, about 47%, about 48%, about 49%, to about 50% or so of the glutamic acid, aspartic acid, or lysine residues, respectively, substituted by any of the naturally occurring amino acids such that the majority of residues comprise glutamic acid and/or aspartic acid and/or lysine.
Brief Patent Description
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Full Patent Description
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Patent Claims
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