Claims for Patent: 8,273,789

Summary for Patent: 8,273,789

Title:	Biologically active taxane analogs and methods of treatment by oral administration
Abstract:	The present invention relates to a novel chemical compound of formula S-(1): ##STR00001## for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.
Inventor(s):	McChesney; James D. (Etta, MS), Tapolsky; Gilles (Boulder, CO), Emerson; David L. (Longmont, CO), Marshall; John (Washington, DC), Ahmed; Tauseef (Hawthorne, NY), Cohn; Allen (Denver, CO), Kurman; Michael (Upper Saddle River, NJ), Modiano; Manuel (Tucson, AZ)
Assignee:	Tapestry Pharmaceuticals, Inc. (Boulder, CO)
Application Number:	12/873,477
Patent Claims:	1. A compound of the formula: ##STR00031## wherein the stereochemistry of the 7,9-vinyl acetal in said compound has S-configuration in a diastereomeric excess of at least 90%. 2. The compound according to claim 1 wherein the stereochemistry of the 7,9-vinyl acetal in the compound has a S-configuration diastereomeric excess of at least 95%. 3. The compound according to claim 2 wherein the stereochemistry of the 7,9-vinyl acetal in the compound has a S-configuration diastereomeric excess of at least 98%. 4. A pharmaceutical composition comprising the compound according to claim 1 together with a pharmaceutically acceptable diluent or carrier. 5. A pharmaceutical composition according to claim 4 which is an orally administrable composition. 6. An oral pharmaceutical composition according to claim 5 which is selected from a tablet, capsule, liquid, powder, lozenge, chew, multi-and nano-particulates, gel, solid solution, liposome, colloidal solution, suspension, film, ovule, spray and liquid formulation. 7. A pharmaceutical composition according to claim 4 which is a parenterally administrable composition. 8. A pharmaceutical composition according to claim 4 further comprising one or more therapeutic agents selected from the group consisting of aromatase inhibitors, antiestrogen, anti-androgen, a gonadorelin agonists, topoisomerase 1 inhibitors, topoisomerase 2 inhibitors, microtubule active agents, alkylating agents, anthracyclines, corticosteroids, IMiDs, protease inhibitors, IGF-1 inhibitors, CD40 antibodies, Smac mimetics, FGF3 modulators, mTOR inhibitors, HDAC inhibitors, IKK inhibitors, P38MAPK inhibitors, HSP90 inhibitors, akt inhibitors, antineoplastic agents, antimetabolites, platin containing compounds, lipid- or protein kinase-targeting agents, protein- or lipid phosphatase-targeting agents, anti-angiogentic agents, agents that induce cell differentiation, bradykinin 1 receptor antagonists, angiotensin II antagonists, cyclooxygenase inhibitors, heparanase inhibitors, lymphokine inhibitors, cytokine inhibitors, bisphosphanates, rapamycin derivatives, anti-apoptotic pathway inhibitors, apoptotic pathway agonists, PPAR agonists, inhibitors of Ras isoforms, telomerase inhibitors, protease inhibitors, metalloproteinase inhibitors and aminopeptidase inhibitors, cytostatic agent, cytotoxic agent, taxane, topoisomerase II inhibitor, topoisomerase I inhibitor, tubulin interacting agent, antibodies, antiangiogenics, COX-2 inhibitors, hormonal agent, thymidilate synthase inhibitor, anti-metabolite, alkylating agent, farnesyl protein transferase inhibitor, signal transduction inhibitor, EGFR kinase inhibitor, antibody to EGFR, C-abl kinase inhibitor, hormonal therapy combination and aromatase combination. 9. A pharmaceutical composition according to claim 8 wherein the one or more therapeutic agents is temozolomide and/or bevacizumab. 10. A kit comprising a composition according to claim 4 together with a chemotherapeutical agent selected from temozolomide, cisplatin, 5-flurouracil, taxotere or gemcitabine, for the separate, simultaneous or sequential use in the treatment of cancer. 11. A method for the treatment of cancer in a patient comprising administering to the patient a therapeutically effective amount of a compound according to claim 1, wherein the cancer is selected from the group consisting of brain, hepatocellular, sarcoma, leukemia, lymphoma, and other bone marrow dyscrasias, neuroblastoma, glioblastoma, cervical, colorectal, pancreatic, renal, thyroid, lung, small-cell lung, non-small cell lung, gastric, breast, ovarian, prostate, head and neck and melanoma. 12. A method according to claim 11 wherein the compound is administered orally. 13. A method according to claim 11 wherein the compound is administered parenterally. 14. The method according to claim 13 wherein the parenteral administration is via intravenous injection or infusion. 15. The method according to claim 11 wherein the cancer is brain cancer. 16. The method according to claim 15 wherein the cancer is selected from the group consisting of astrocytoma, craniopharyngioma, glioma, ependymoma, neuroglioma, oligodendroglioma, glioblastoma multiforme, meningioma, medulloblastoma and other primitive neuroectoderma. 17. The method according to claim 11 wherein the cancer is neuroblastoma. 18. The method according to claim 11 wherein the cancer is colorectal cancer. 19. The method according to claim 11 wherein the cancer is pancreatic cancer. 20. The method according to claim 11 wherein the compound is administered separately, simultaneously, or sequentially with a chemotherapeutical agent selected from temozolomide, cisplatin, 5-flurouracil, taxotere or gemcitabine. 21. The method according to claim 20 wherein the compound is administered separately, simultaneously, or sequentially with temozolomide. 22. The method according to claim 11 further comprising administering radiation therapy. 23. The method, according to claim 11 further comprising surgical removal of a cancer. 24. The method according to claim 11 wherein the composition is administered separately, simultaneously, or sequentially with one or more therapeutic agents selected from the group consisting of aromatase inhibitors, antiestrogen, anti-androgen, a gonadorelin agonists, topoisomerase 1 inhibitors, topoisomerase 2 inhibitors, microtubule active agents, alkylating agents, anthracyclines, corticosteroids, IMiDs, protease inhibitors, IGF-1 inhibitors, CD40 antibodies, Smac mimetics, FGF3 modulators, mTOR inhibitors, HDAC inhibitors, IKK inhibitors, P38MAPK inhibitors, HSP90 inhibitors, akt inhibitors, antineoplastic agents, antimetabolites, platin containing compounds, lipid- or protein kinase- targeting agents, protein- or lipid phosphatase-targeting agents, anti-angiogentic agents, agents that induce cell differentiation, bradykinin 1 receptor antagonists, angiotensin II antagonists, cyclooxygenase inhibitors, heparanase inhibitors, lymphokine inhibitors, cytokine inhibitors, bisphosphanates, rapamycin derivatives, anti-apoptotic pathway inhibitors, apoptotic pathway agonists, PPAR agonists, inhibitors of Ras isoforms, telomerase inhibitors, protease inhibitors, metalloproteinase inhibitors and aminopeptidase inhibitors, cytostatic agent, cytotoxic agent, taxane, topoisomerase II inhibitor, topoisomerase I inhibitor, tubulin interacting agent, antibodies, antiangiogenics, COX-2 inhibitors, hormonal agent, thymidilate synthase inhibitor, anti-metabolite, alkylating agent, farnesyl protein transferase inhibitor, signal transduction inhibitor, EGFR kinase inhibitor, antibody to EGFR, C-abl kinase inhibitor, hormonal therapy combination and aromatase combination. 25. The method according to claim 24 wherein the one or more therapeutic agents is temozolomide and/or bevacizumab. 26. The method according to claim 14 wherein the administration is for about 60 minutes or less. 27. The method according to claim 26 wherein the administration administered via intravenous infusion once every 7 days for 3 weeks, followed by a 7 day rest period, in a 28 day cycle; for at least one cycle. 28. The method according claim 26 wherein the administration administered via intravenous infusion once every 21 days, in a 21 day cycle; for at least one cycle. 29. The method according to claim 27 wherein the intravenous infusion comprises S-(I) at a dose of 185 mg/m.sup.2 or less, or 160 mg/m.sup.2 or less. 30. A compound of the formula: ##STR00032## 31. The compound according to claim 30 wherein wherein the stereochemistry of the 7,9-vinyl acetal in the compound has a S-configuration diastereomeric excess of at least 95%. 32. The compound according to claim 31 wherein the stereochemistry of the 7,9-vinyl acetal in the compound has a S-configuration diastereomeric excess of at least 98%.

Details for Patent 8,273,789

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	AVASTIN	bevacizumab	Injection	125085	02/26/2004		2039-02-26