DHA-pharmaceutical agent conjugates of taxanes

• US 5,795,909 A
• Filed: 05/22/1996
• Issued: 08/18/1998
• Est. Priority Date: 05/22/1996
• Status: Expired due to Term

• Current Assignee: Luitpold Pharmaceuticals Incorporated (Daiichi Sankyo Company Limited)
• Original Assignee: Neuromedica Incorporated
• Inventors: Shashoua, Victor E., Swindell, Charles S., Bradley, Matthews O., Webb, Nigel L.
• Primary Examiner(s): Jarvis, William R. A.
• Application Number:
  US08/651,312
• Time in Patent Office: 818 Days
• Field of Search: 514/449, 514/549
• US Class Current: 514/449
• CPC Class Codes: A61K 47/542 Carboxylic acids, e.g. a fatty acid or an amino acid
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

The invention provides conjugates of cis-docosahexaenoic acid and taxanes useful in treating cell proliferative disorders. Conjugates of paclitaxel and docetaxel are preferred.

Claims

1. A method of treating a mammalian cell proliferative disorder comprising:

administering to a subject in need of such treatment a covalent conjugate of cis-docosahexanoic acid and a pharmaceutical agent effective for treating said condition, wherein the pharmaceutical agent is a taxane.

2. The method of claim 1, wherein the taxane is paclitaxel.

3. The method of claim 2, wherein the conjugate is ##STR13##

4. The method of claim 2, wherein the conjugate is ##STR14##

5. The method of claim 1, wherein the taxane is docetaxel.

6. The method of claim 5, wherein the conjugate is ##STR15##

7. The method of claim 5, wherein the conjugate is ##STR16##

8. The method of claim 5, wherein the conjugate is ##STR17##

9. The method of claim 5, wherein the conjugate is ##STR18##

10. The method of claim 1, 2, 3, 4, 5, 6, 7, 8 or 9, wherein the disorder is breast cancer.

11. The method of claim 1, 2, 3, 4, 5, 6, 7, 8 or 9, wherein the disorder is colon cancer.

12. The method of claim 1, 2, 3, 4, 5, 6, 7, 8 or 9, wherein the disorder is ovarian cancer.