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Last Updated: January 26, 2020

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Claims for Patent: 10,130,645

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Summary for Patent: 10,130,645
Title:Use of thiopyrimidinecarboxamide for treating cancer
Abstract: There is disclosed is a method of treating disease 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:15/627,766
Patent Claims:1. A method for treating a CXCR1/2 chemokine mediated disease in a patient in need of such treatment, comprising administering an effective amount of the compound having formula SX-682 ##STR00007## or a pharmaceutically acceptable salt or solvate thereof, wherein the CXCR1/2 chemokine mediated disease is selected from the group consisting of atopic dermatitis, asthma, inflammatory bowel disease, Crohn's disease, ulcerative colitis, Alzheimer's disease, atherosclerosis, cerebral ischemia, cardiac ischemia, multiple sclerosis, cystic fibrosis, psoriatic arthritis, tumors dependent on angiogenesis for growth, pancreatitis, alcoholic hepatitis, and alcoholic liver disease.

2. The method of claim 1, wherein SX-682 or a pharmaceutically acceptable salt or solvate thereof is administered concurrently or sequentially at least one additional agent, drug, medicament, antibody and/or inhibitor useful for the treatment of the CXCR1/2 chemokine mediated disease.

3. The method of claim 2, wherein the additional agent, drug, medicament, antibody and/or inhibitor useful for the treatment of the CXCR1/2 chemokine mediated disease is selected from the group consisting of disease modifying antirheumatic drugs; nonsteroidal antiinflammatory drugs (NSAIDs); COX-2 selective inhibitors; COX-1inhibitors; immunosuppressives; steroids; biological response modifiers; and other anti-inflammatory agents or therapeutics useful for the treatment of CXCR1/2 chemokine mediated diseases.

4. The method of claim 2, wherein the additional agent, drug, medicament, antibody and/or inhibitor useful for the treatment of the CXCR1/2 chemokine mediated disease is selected from the group consisting of glucocorticoids, 5-lipoxygenase inhibitors, beta-2 adrenoceptor agonists, muscarinic M1 antagonists, muscarinic M3antagonists, muscarinic M2 agonists, NK3 antagonists, LTB4 antagonists, cysteinyl leukotriene antagonists, bronchodilators, PDE4 inhibitors, PDE inhibitors, elastase inhibitors, MMP inhibitors, phospholipase A2 inhibitors, phospholipase D inhibitors, histamine H1 antagonists, histamine H3 antagonists, dopamine agonists, adenosine A2 agonists, NK1 and NK2antagonists, GABA-.beta.agonists, nociceptin agonists, expectorants, mucolytic agents, decongestants, antioxidants, anti-IL-8 antibodies, anti-IL-5 antibodies, anti-IgE antibodies, anti-TNF antibodies, IL-10, adhesion molecule inhibitors, and growth hormones.

5. The method of claim 2, wherein the additional agent, drug, medicament, antibody and/or inhibitor useful for the treatment of the CXCR1/2 chemokine mediated disease is selected from the group consisting of methotrexate, cyclosporin, leflunimide, sulfasalazine, .beta.-methasone, .beta.-interferon, glatiramer acetate, prednisone, etonercept, and infliximab.

6. The method of claim 2, wherein the additional agent, drug, medicament, antibody and/or inhibitor useful for the treatment of the CXCR1/2 chemokine mediated disease is selected from the group consisting of tenecteplase, TPA, alteplase, abciximab, eftiifbatide), anticoagulants, and heparin.

7. The method of claim 2, wherein the additional agent, drug, medicament, antibody and/or inhibitor useful for the treatment of the CXCR1/2 chemokine mediated disease is selected from the group consisting of NSAIDs, COX-1 and COX-2inhibitors, anti-depressants, and anti-convulsants.

8. The method of claim 7, wherein the anti-convulsant is selected from the group consisting of gabapentin, carbamazepine, pregabalin, and lamotragine.

9. A method for treating a transplant patient in need of such treatment, comprising administering an effective amount of the compound having formula SX-682 ##STR00008## or a pharmaceutically acceptable salt or solvate thereof, wherein the patient has graft vs. host reaction, allograft rejections, transplant reperfusion injury, early transplantation rejection, or renal reperfusion injury.

10. A method for treating pain in a patient in need of such treatment, comprising administering an effective amount of the compound having formula SX-682 ##STR00009## or a pharmaceutically acceptable salt or solvate thereof, wherein the patient has acute inflammatory pain, chronic inflammatory pain, or neuropathic pain.

11. A pharmaceutical formulation comprising a therapeutically effective amount of the compound having formula SX-682 ##STR00010## or a pharmaceutically acceptable salt or solvate thereof, and a self-emulsifying drug delivery system.

12. The pharmaceutical formulation of claim 1, wherein the self-emulsifying drug delivery system is selected from the group consisting of caprylocaproyl polyoxyl-8 glycerides, steroyl or lauroyl polyoxyl-32-glycerides, and glycerides of C12-C18 fatty acids.

13. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation is for oral or parenteral administration.

14. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation is in a unit dosage form, wherein the unit dosage form comprises a unit dose of SX-682.

15. The pharmaceutical formulation of claim 5, wherein the unit dose is about 0.01 mg to about 1000 mg.

16. The pharmaceutical formulation of claim 5, wherein the unit dose is about 0.01 mg to about 750 mg.

17. The pharmaceutical formulation of claim 5, wherein the unit dose is about 0.01 mg to about 500 mg.

18. The pharmaceutical formulation of claim 5, wherein the unit dose is about 0.01 mg to about 250 mg.

19. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation is for transdermal administration.

20. The pharmaceutical formulation of claim 11, wherein the pharmaceutical formulation is a cream, lotion, aerosol, emulsion, or a transdermal patch.

Details for Patent 10,130,645

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Genentech ACTIVASE alteplase VIAL; SINGLE-USE 103172 001 1987-11-13   Start Trial Syntrix Biosystems, Inc. (Auburn, WA) 2033-08-02 RX search
Genentech ACTIVASE alteplase VIAL; SINGLE-USE 103172 002 1987-11-13   Start Trial Syntrix Biosystems, Inc. (Auburn, WA) 2033-08-02 RX search
Genentech CATHFLO ACTIVASE alteplase VIAL 103172 003 1987-11-13   Start Trial Syntrix Biosystems, Inc. (Auburn, WA) 2033-08-02 RX search
Centocor Inc REOPRO abciximab INJECTABLE; INJECTION 103575 001 1994-12-22   Start Trial Syntrix Biosystems, Inc. (Auburn, WA) 2033-08-02 RX search
Centocor Inc REMICADE infliximab VIAL 103772 001 1998-08-24   Start Trial Syntrix Biosystems, Inc. (Auburn, WA) 2033-08-02 RX Orphan search
Genentech TNKASE tenecteplase VIAL 103909 001 2000-06-02   Start Trial Syntrix Biosystems, Inc. (Auburn, WA) 2033-08-02 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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