Claims for Patent: 8,299,081

Summary for Patent: 8,299,081

Title:	Methods for treating drug resistant cancer
Abstract:	A method for treating drug-resistant cancer, includes: administering to a patient in need thereof, a compound of formula I, a tautomer of the compound, a salt of the compound, a salt of the tautomer, a mixture thereof, or a pharmaceutical composition comprising the compound, the tautomer, the salt of the compound, the salt of the tautomer, or the mixture, wherein the patient is a cancer patient with drug-resistant cancer, wherein the compound of Formula I is as defined in the application.
Inventor(s):	Michelson; Glenn C. (Emeryville, CA), Chan; Vivien W. (Emeryville, CA), Heise; Carla C. (Emeryville, CA), Wiesmann; Marion (Emeryville, CA), Dawes; Timothy D. (Emeryville, CA)
Assignee:	Novartis AG (Basel, CH)
Application Number:	11/913,828
Patent Claims:	1. A method of treating drug-resistant cancer comprising administering to a drug-resistant cancer subject in need thereof, a compound of formula II, a tautomer of the compound, a salt of the compound, a salt of the tautomer, a mixture thereof, or a pharmaceutical composition comprising the compound, the tautomer, the salt of the compound, the salt of the tautomer, or the mixture, by inhibiting a cytoplasmic tyrosine kinase or a receptor tyrosine kinase comprising a mutant gatekeeper residue in the subject, wherein the kinase is ABL, KIT, PDGFRa, EGFR, or FLT3, and wherein the cancer is resistant to an anti-cancer drug selected from the group consisting of imatinib mesylate, BAY43-9006, Brostallicin, erlotinib, gefitinib, and vatalanib, and further wherein the compound of formula II has the following formula: ##STR00021## wherein R.sup.7 is a substituted or unsubstituted heterocyclyl group selected from a substituted or unsubstituted piperidinyl group, piperazinyl group, or morpholinyl group. 2. The method of claim 1, wherein R.sup.7 is a substituted or unsubstituted N-alkyl piperazinyl group. 3. The method of claim 1, wherein the alkyl group of the N-alkyl piperazinyl comprises from 1 to 4 carbon atoms. 4. The method of claim 1, wherein the compound of formula II is a compound of formula III: ##STR00022## 5. The method of claim 1, wherein the lactic acid salt of the compound is administered to the subject. 6. The method of claim 1, wherein the cancer is resistant to imatinib mesylate, BAY43-9006, or Brostallicin. 7. The method of claim 1, wherein the cancer is resistant to erlotinib, gefitinib, or vatalanib. 8. The method of claim 1, wherein the cancer is resistant to imatinib mesylate. 9. The method of claim 1, wherein the compound, the tautomer, the salt of the compound, the salt of the tautomer, the mixture, or the pharmaceutical composition is administered to the subject after imatinib mesylate has been administered to the subject and the cancer in the subject has been found to be resistant to imatinib mesylate. 10. The method of claim 1, wherein the compound, the tautomer, the salt of the compound, the salt of the tautomer, the mixture, or the pharmaceutical composition is administered to the subject after BAY43-9006 has been administered to the subject and the cancer in the subject has been found to be resistant to BAY43-9006. 11. The method of claim 1, wherein the compound, the tautomer, the salt of the compound, the salt of the tautomer, the mixture, or the pharmaceutical composition is administered to the subject after Brostallicin has been administered to the subject and the cancer in the subject has been found to be resistant to Brostallicin. 12. The method of claim 1 further comprising co-administering an anti-cancer drug selected from the group consisting of imatinib mesylate, BAY43-9006, Brostallicin, lenalidomide, thalidomide, docetaxel, erlotinib, vatalinib, VEGF-trap, fenretidine, bortezomib, bevacizumab, pertuzumab, and rituximab. 13. The method of claim 12, wherein the compound, the tautomer, the salt of the compound, the salt of the tautomer, the mixture, or the pharmaceutical composition is to be administered after the anti-cancer drug has been administered, before the anti-cancer has been administered or at same time that at least some of anti-cancer drug is administered. 14. The method of claim 1, wherein the drug-resistant cancer is selected from prostate cancer, renal cancer, gastrointestinal stromal tumor, sarcoma, colorectal cancer, breast cancer, parotid cancer, gastric cancer, melanoma, oesophageal cancer, NET (sinonasal) cancer, colon cancer, ovarian cancer, or liver cancer. 15. The method of claim 1, wherein the drug-resistant cancer is selected from gastrointestinal stromal tumor, acute myelogenous leukemia, chronic myelogenous leukemia, multiple myeloma, renal cell carcinoma, non-small cell lung cancer, or hypereosinophilic syndrome. 16. The method of claim 1, wherein the cancer is selected from chronic myelogenous leukemia, multiple myeloma, or renal cell carcinoma. 17. The method of claim 1, wherein the drug-resistant cancer is gastrointestinal stromal tumor. 18. The method of claim 1, wherein the kinase is ABL(T315I), FLT3(D835Y), or EGFR. 19. A method of treating drug-resistant cancer comprising administering to a drug-resistant cancer subject in need thereof a compound, a tautomer of the compound, a salt of the compound, a salt of the tautomer, a mixture thereof, or a pharmaceutical composition comprising the compound, the tautomer, the salt of the compound, the salt of the tautomer, or the mixture, by inhibiting a cytoplasmic tyrosine kinase or a receptor tyrosine kinase comprising a mutant gatekeeper residue in the subject, wherein the kinase is ABL, KIT, PDGFRa, EGFR, or FLT3, and wherein the drug-resistant cancer is selected from the group consisting of prostate cancer, renal cancer, gastrointestinal stromal tumor, sarcoma, colorectal cancer, breast cancer, parotid cancer, gastric cancer, melanoma, oesophageal cancer, NET (sinonasal) cancer, colon cancer, ovarian cancer, liver cancer, acute myelogenous leukemia, chronic myelogenous leukemia, multiple myeloma, renal cell carcinoma, non-small cell lung cancer, and hypereosinophilic syndrome, and further wherein the compound has the following formula: ##STR00023## 20. The method of claim 4, wherein the drug-resistant cancer is resistant to an anti-cancer drug selected from the group consisting of imatinib mesylate, BAY43-9006, Brostallicin, erlotinib, gefitinib, and vatalanib.

Details for Patent 8,299,081

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2025-05-13
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002		2025-05-13
Genentech, Inc.	AVASTIN	bevacizumab	Injection	125085	02/26/2004		2025-05-13
Genentech, Inc.	PERJETA	pertuzumab	Injection	125409	06/08/2012		2025-05-13
Genentech, Inc.	RITUXAN HYCELA	rituximab and hyaluronidase human	Injection	761064	06/22/2017		2025-05-13