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Last Updated: April 23, 2024

Claims for Patent: 9,707,248


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Summary for Patent: 9,707,248
Title:Use of thiopyrimidinecarboxamide for treating cancer
Abstract: There is disclosed is a method of treating cancer using compound having formula SX-682 ##STR00001## alone or in combination with an antineoplastic agent, microtubule affecting agents, antineoplastic agents, anti-angiogenesis agents, VEGF receptor kinase inhibitors, antibodies against the VEGF receptor, interferon, or radiation.
Inventor(s): Zebala; John A. (Issaquah, WA), Maeda; Dean Y. (Seattle, WA), Schuler; Aaron D. (Auburn, WA)
Assignee: Syntrix Biosystems Inc. (Auburn, WA)
Application Number:15/279,361
Patent Claims:1. A method for treating a subject with a cancer, comprising administering to the subject in need thereof a therapeutically effective amount of the compound having formula SX-682 ##STR00007## or a pharmaceutically acceptable salt or solvate thereof.

2. The method of claim 1, wherein SX-682 or a pharmaceutically acceptable salt or solvate thereof is administered concurrently or sequentially with at least one antineoplastic agent.

3. The method of claim 2, wherein the antineoplastic agent is selected from nitrogen mustards, ethylenimine derivatives, alkyl sulfonates, nitrosoureas and triazenes, uracil mustard, chlormethine, cyclophosphamide, ifosfamide, melphalan, chlorambucil, pipobroman, triethylene-melamine, triethylenethiophos-phoramine, busulfan, carmustine, lomustine, streptozocin, dacarbazine, and temozolomide.

4. The method of claim 2, wherein the antineoplastic agent is selected from folic acid antagonists, pyrimidine analogs, purine analogs and adenosine deaminase inhibitors, methotrexate, aminopterin, 5-fluorouracil, floxuridine, cytarabine, 6-mercaptopurine, 6-thioguanine, fludarabine phosphate, pentostatine, and gemcitabine.

5. The method of claim 2, wherein the antineoplastic agent is selected from vinca alkaloids, antitumor antibiotics, enzymes, lymphokines and epipodophyllotoxins, vinblastine, vincristine, vindesine, bleomycin, dactinomycin, daunorubicin, doxorubicin, epirubicin, idarubicin, paclitaxel (TAXOL.RTM.), mithramycin, deoxycoformycin, mitomycin-C, L-asparaginase, interferons (especially IFN-.gamma.), etoposide, and teniposide.

6. The method of claim 2, wherein the antineoplastic agent is selected from 17.alpha.-ethinylestradiol, diethylstilbestrol, testosterone, prednisone, fluoxymesterone, dromostanolone propionate, testolactone, megestrolacetate, tamoxifen, methylprednisolone, methyltestosterone, prednisolone, triamcinolone, chlorotrianisene, hydroxyprogesterone, aminoglutethimide, estramustine, medroxyprogesteroneacetate, leuprolide, flutamide, toremifene, and zoladex.

7. The method of claim 2, wherein the antineoplastic agent is selected from platinum coordination complexes, cisplatin, carboplatin, hydroxyurea, amsacrine, procarbazine, mitotane, mitoxantrone, levamisole, and hexamethylmelamine.

8. The method of claim 2, wherein the antineoplastic agent is selected from gemcitabine, paclitaxel, cyclophosphamide, 5-fluorouracil, temozolomide and vincristine.

9. The method of claim 1, wherein SX-682 or a pharmaceutically acceptable salt or solvate thereof, is administered concurrently or sequentially with a microtubule affecting agent selected from allocolchicine, halichondrin B, colchicine, colchicine derivatives, dolastatin 10, maytansine, rhizoxin, paclitaxel, TAXOL.RTM. derivatives, thiocolchicine, trityl cysteine, vinblastine sulfate, vincristine sulfate, epothilone A, epothilone, and discodermolide, estramustine, nocodazole, and MAP4.

10. The method of claim 1, wherein SX-682 or a pharmaceutically acceptable salt or solvate thereof, is administered concurrently or sequentially with an anti-angiogenesis agent, a VEGF receptor kinase inhibitor, an antibodies against the VEGF receptor, interferon, or radiation.

11. The method of claim 1, wherein the compound having formula SX-682 or a pharmaceutically acceptable salt or solvate thereof is administered orally, transdermally, parenterally, intranasally, or by inhalation.

12. The method of claim 1, wherein the compound having formula SX-682 or a pharmaceutically acceptable salt or solvate thereof is administered orally.

13. The method of claim 1, wherein the compound having formula SX-682 or a pharmaceutically acceptable salt or solvate thereof is administered in a 0.01 mg to 1000 mg dose.

14. The method of claim 1, wherein the compound having formula SX-682 or a pharmaceutically acceptable salt or solvate thereof is administered orally in a daily, twice-weekly or once-weekly dose of 0.04 mg to 4000 mg, given in two to four divided doses or as a single dose.

15. The method of claim 14, wherein the dose of the compound having formula SX-682 or a pharmaceutically acceptable salt or solvate thereof is 10 mg to 600 mg, 1000 mg, or 2000 mg.

16. A method for treating a subject with a tumor, comprising administering to the subject in need thereof a therapeutically effective amount of the compound having formula SX-682 ##STR00008## or a pharmaceutically acceptable salt or solvate thereof.

17. The method of claim 16, further comprising the step of successively measuring the tumor.

18. The method of claim 17, wherein the tumor is measured by CAT or MRI scan.

19. The method of claim 17, wherein SX-682 inhibits angiogenesis associated with tumor growth.

20. The method of claim 17, wherein SX-682 inhibits growth of a tumor.

21. The method of claim 20, wherein SX-682 inhibits growth of systemic tumors, CNS tumors, tumors dependent on angiogenesis for growth.

22. The method of claim 17, wherein administration of SX-682 inhibits metastasis of a tumor.

23. The method of claim 17, wherein administration of SX-682 decreases the size of a tumor.

24. The method of claim 17, wherein administration of SX-682 decreases the volume of a tumor.

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