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Last Updated: April 25, 2024

Claims for Patent: 10,507,212


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Summary for Patent: 10,507,212
Title:Method for use of homopiperazinium compounds in the treatment of cancer
Abstract: A method for treating cancer including administering to a patient in need thereof an effective amount of a compound having the formula: ##STR00001## wherein R.sub.1, R.sub.2, Ya, Xa, and J.sup.- are as defined herein, and may be where R1 and R2 are independently selected from methyl, ethyl, n-propyl, or i-propyl; Xa is N or CH; Ya is hydrogen or independently selected from halogen, cyano, hydroxyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, heteroaryl of 6 members and aryl; n is 1 or 2; wherein J.sup.- is fluoride, chloride, bromide, iodide, acetate, sulfate or sulfonate such as tosylate, mesylate, besylate.
Inventor(s): Cormier; Yvon (Quebec, CA), Israel-Assayag; Evelyne (Quebec, CA)
Assignee: UNIVERSITE LAVAL (Quebec, CA)
Application Number:15/921,138
Patent Claims:1. A method for treating cancer comprising administering to a patient in need thereof an effective amount of a compound having the formula: ##STR00054## wherein R.sub.1 and R.sub.2 are independently alkyl of 1 to 6 carbon atoms or cycloalkyl of 3 to 6 carbon atoms, Xa is CH or N, Ya is hydrogen or independently selected from halogen, cyano, hydroxyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, heteroaryl of 6 members and aryl, n is an integer from 1 to 5, J is a counter ion; and wherein said cancer is a carcinoma or a blastoma, wherein said carcinoma is selected from the group of lung cancer and colon cancer, and wherein said blastoma is a neuroblastoma.

2. The method as defined in claim 1, wherein R.sub.1 and R.sub.2 are independently selected from methyl, ethyl, n-propyl, or i-propyl.

3. The method as defined in claim 1, wherein Xa is CH.

4. The method as defined in claim 1, wherein Xa is N.

5. The method as defined in claim 1, wherein n is 1 or 2.

6. The method as defined in claim 1, wherein R1 and R2 are independently selected from methyl, ethyl, n-propyl, or i-propyl; Xa is N or CH; Ya is hydrogen or independently selected from halogen, cyano, hydroxyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, heteroaryl of 6 members and aryl; n is 1 or 2; wherein J.sup.- is fluoride, chloride, bromide, iodide, acetate, sulfate or sulfonate.

7. The method as defined in claim 1, wherein R1 and R2 are independently selected from methyl, ethyl, n-propyl, or i-propyl; Xa is CH; Ya is hydrogen or independently selected from halogen, cyano, hydroxyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, heteroaryl of 6 members and aryl; n is 1; wherein J.sup.- is fluoride, chloride, bromide, iodide, acetate, sulfate or sulfonate.

8. The method as defined in claim 6, wherein said sulfonate is tosylate, mesylate or besylate.

9. The method as defined in claim 7, wherein said sulfonate is tosylate, mesylate or besylate.

10. The method as defined in claim 1, wherein said compound has the formula: ##STR00055##

11. The method as defined in claim 1, wherein said cancer is a cancer of the colon.

12. The method as defined in claim 1, wherein said cancer is neuroblastoma.

13. The method as defined in claim 1, further comprising administering a therapeutically effective amount of at least one or more therapeutic agents selected from: Alkylating agents, anti-metabolites, plant alkaloids and terpenoids, vinca alkaloids, podophyllotoxin, taxanes, topoisomerase inhibitors, and cytotoxic antibiotics.

14. The method as defined in claim 1, further comprising administering a therapeutically effective amount of at least one or more therapeutic agents selected from imatinib, paclitaxel, docetaxel, cisplatin, doxorubicine, vinblastine, zoledronate, avastatin, Velcade, arimidex, tamoxifen, bicalutamide, trastuzumab, and vemurafenib.

Details for Patent 10,507,212

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2034-04-03
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2034-04-03
Genentech, Inc. HERCEPTIN HYLECTA trastuzumab and hyaluronidase-oysk Injection 761106 02/28/2019 ⤷  Try a Trial 2034-04-03
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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