US2003114397A1PendingUtilityA1

Water soluble paclitaxel derivatives

62
Assignee: PG TXL CO LPPriority: Mar 12, 1996Filed: Sep 12, 2002Published: Jun 19, 2003
Est. expiryMar 12, 2016(expired)· nominal 20-yr term from priority
Inventors:Chun LiSidney WallaceDong-Fang YuDavid J. Yang
A61K 47/645A61L 2300/416A61L 31/16A61K 38/13A61K 51/0497A61K 2123/00A61K 51/065A61L 2300/606A61K 41/0038A61P 35/02A61L 31/10A61K 47/60A61K 31/4375A61P 35/00A61K 47/547A61K 31/337C08G 73/1092A61K 47/59A61P 35/04A61K 2121/00
62
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Claims

Abstract

Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A method for treating cancer in a subject, comprising administering to a subject having cancer a water soluble conjugate comprising a taxoid in combination with an antibiotic.  
     
     
         2 . The method of  claim 1 , wherein said water soluble conjugate comprises paclitaxel.  
     
     
         3 . The method of  claim 1 , wherein said water soluble conjugate comprises docetaxel.  
     
     
         4 . The method of  claim 2 , wherein said water soluble conjugate comprises a water soluble polymer conjugated to said paclitaxel.  
     
     
         5 . The method of  claim 4 , wherein said water soluble polymer is polyglutamate.  
     
     
         6 . The method of  claim 5 , wherein said polyglutamate is poly(l-glutamic acid).  
     
     
         7 . The method of  claim 6 , wherein said polyglutamic acid has a molecular weight of about 5000 to about 100,000 daltons.  
     
     
         8 . The method of  claim 7 , wherein said polyglutamic acid has a molecular weight of about 20,000 to about 80,000 daltons.  
     
     
         9 . The method of  claim 8 , wherein said polyglutamic acid has a molecular weight of about 25,000 to about 50,000 daltons.  
     
     
         10 . The method of  claim 9 , wherein said polyglutamic acid has a molecular weight of about 35,000 daltons.  
     
     
         11 . The method of  claim 6 , wherein said composition comprises from about 2% to about 35% by weight of paclitaxel.  
     
     
         12 . The method of  claim 6 , wherein said composition comprises from about 37% by weight of paclitaxel.  
     
     
         13 . The method of  claim 6 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         14 . The method of  claim 12 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         15 . The method of  claim 3 , wherein said water soluble conjugate comprises a water soluble polymer conjugated to said docetaxel.  
     
     
         16 . The method of  claim 15 , wherein said water soluble polymer is polyglutamate.  
     
     
         17 . The method of  claim 16 , wherein said polyglutamate is poly(l-glutamic acid).  
     
     
         18 . The method of  claim 17 , wherein said polyglutamic acid has a molecular weight of about 5000 to about 100,000 daltons.  
     
     
         19 . The method of  claim 18 , wherein polyglutamic acid has a molecular weight of about 20,000 to about 80,000 daltons.  
     
     
         20 . The method of  claim 19 , wherein polyglutamic acid has a molecular weight of about 25,000 to about 50,000 daltons.  
     
     
         21 . The method of  claim 20 , wherein said polyglutamic acid has a molecular weight of about 35,000 daltons.  
     
     
         22 . The method of  claim 17 , wherein said composition comprises from about 2% to about 35% by weight of said docetaxel.  
     
     
         23 . The method of  claim 17 , wherein said composition comprises from about 37% by weight of said docetaxel.  
     
     
         24 . The method of  claim 22 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         25 . The method of  claim 23 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         26 . A method for treating cancer in a subject, comprising administering to a subject having cancer a water soluble conjugate comprising a taxoid in combination with doxorubicin.  
     
     
         27 . The method of  claim 26 , wherein said water soluble conjugate comprises paclitaxel.  
     
     
         28 . The method of  claim 26 , wherein said water soluble conjugate comprises docetaxel.  
     
     
         29 . The method of  claim 27 , wherein said water soluble conjugate comprises a water soluble polymer conjugated to said paclitaxel.  
     
     
         30 . The method of  claim 29 , wherein said water soluble polymer is polyglutamate.  
     
     
         31 . The method of  claim 30 , wherein said polyglutamate is poly(l-glutamic acid).  
     
     
         32 . The method of  claim 31 , wherein said polyglutamic acid has a molecular weight of about 5000 to about 100,000 daltons.  
     
     
         33 . The method of  claim 32 , wherein said polyglutamic acid has a molecular weight of about 20,000 to about 80,000 daltons.  
     
     
         34 . The method of  claim 33 , wherein said polyglutamic acid has a molecular weight of about 25,000 to about 50,000 daltons.  
     
     
         35 . The method of  claim 34 , wherein said polyglutamic acid has a molecular weight of about 35,000 daltons.  
     
     
         36 . The method of  claim 31 , wherein said composition comprises from about 2% to about 35% by weight of paclitaxel.  
     
     
         37 . The method of  claim 31 , wherein said composition comprises from about 37% by weight of paclitaxel.  
     
     
         38 . The method of  claim 31 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         39 . The method of  claim 37 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         40 . The method of  claim 28 , wherein said water soluble conjugate comprises a water soluble polymer conjugated to said docetaxel.  
     
     
         41 . The method of  claim 40 , wherein said water soluble polymer is polyglutamate.  
     
     
         42 . The method of  claim 41 , wherein said polyglutamate is poly(l-glutamic acid).  
     
     
         43 . The method of  claim 42 , wherein said polyglutamic acid has a molecular weight of about 5000 to about 100,000 daltons.  
     
     
         44 . The method of  claim 43 , wherein polyglutamic acid has a molecular weight of about 20,000 to about 80,000 daltons.  
     
     
         45 . The method of  claim 44 , wherein polyglutamic acid has a molecular weight of about 25,000 to about 50,000 daltons.  
     
     
         46 . The method of  claim 45 , wherein said polyglutamic acid has a molecular weight of about 35,000 daltons.  
     
     
         47 . The method of  claim 42 , wherein said composition comprises from about 2% to about 35% by weight of said docetaxel.  
     
     
         48 . The method of  claim 42 , wherein said composition comprises from about 37% by weight of said docetaxel.  
     
     
         49 . The method of  claim 47 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         50 . The method of  claim 48 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         51 . A method for treating cancer in a subject, comprising administering to a subject having cancer a water soluble conjugate comprising a taxoid in combination with daunorubicin.  
     
     
         52 . The method of  claim 51 , wherein said water soluble conjugate comprises paclitaxel.  
     
     
         53 . The method of  claim 51 , wherein said water soluble conjugate comprises docetaxel.  
     
     
         54 . The method of  claim 52 , wherein said water soluble conjugate comprises a water soluble polymer conjugated to said paclitaxel.  
     
     
         55 . The method of  claim 54 , wherein said water soluble polymer is polyglutamate.  
     
     
         56 . The method of  claim 55 , wherein said polyglutamate is poly(l-glutamic acid).  
     
     
         57 . The method of  claim 56 , wherein said polyglutamic acid has a molecular weight of about 5000 to about 100,000 daltons.  
     
     
         58 . The method of  claim 57 , wherein said polyglutamic acid has a molecular weight of about 20,000 to about 80,000 daltons.  
     
     
         59 . The method of  claim 58 , wherein said polyglutamic acid has a molecular weight of about 25,000 to about 50,000 daltons.  
     
     
         60 . The method of  claim 59 , wherein said polyglutamic acid has a molecular weight of about 35,000 daltons.  
     
     
         61 . The method of  claim 56 , wherein said composition comprises from about 2% to about 35% by weight of paclitaxel.  
     
     
         62 . The method of  claim 56 , wherein said composition comprises from about 37% by weight of paclitaxel.  
     
     
         63 . The method of  claim 56 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         64 . The method of  claim 62 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         65 . The method of  claim 53 , wherein said water soluble conjugate comprises a water soluble polymer conjugated to said docetaxel.  
     
     
         66 . The method of  claim 65 , wherein said water soluble polymer is polyglutamate.  
     
     
         67 . The method of  claim 66 , wherein said polyglutamate is poly(l-glutamic acid).  
     
     
         68 . The method of  claim 67 , wherein said polyglutamic acid has a molecular weight of about 5000 to about 100,000 daltons.  
     
     
         69 . The method of  claim 68 , wherein polyglutamic acid has a molecular weight of about 20,000 to about 80,000 daltons.  
     
     
         70 . The method of  claim 69 , wherein polyglutamic acid has a molecular weight of about 25,000 to about 50,000 daltons.  
     
     
         71 . The method of  claim 70 , wherein said polyglutamic acid has a molecular weight of about 35,000 daltons.  
     
     
         72 . The method of  claim 67 , wherein said composition comprises from about 2% to about 35% by weight of said docetaxel.  
     
     
         73 . The method of  claim 67 , wherein said composition comprises from about 37% by weight of said docetaxel.  
     
     
         74 . The method of  claim 72 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.  
     
     
         75 . The method of  claim 73 , wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, prostate cancer, colon cancer, head and neck cancer, leukemia or Kaposi's sarcoma.

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