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Last Updated: October 18, 2019

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Claims for Patent: 9,949,971

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Summary for Patent: 9,949,971
Title:Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor and/or a JAK-2 inhibitor
Abstract: Therapeutic combinations of a Janus kinase-2 (JAK-2) inhibitor, a Bruton\'s tyrosine kinase (BTK) inhibitor, and/or a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the .gamma.- and .delta.-isoforms and selective for both .gamma.- and .delta.-isoforms, are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of (1) a PI3K-.delta. inhibitor and a BTK inhibitor, (2) a JAK-2 inhibitor and a BTK inhibitor, or (3) a JAK-2 inhibitor, PI3K-.delta. inhibitor, and BTK inhibitor, and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.
Inventor(s): Hamdy; Ahmed (Santa Cruz, CA), Rothbaum; Wayne (Delray Beach, FL), Izumi; Raquel (San Carlos, CA), Lannutti; Brian (Solana Beach, CA), Covey; Todd (San Carlos, CA), Ulrich; Roger (Sammamish, WA), Johnson; Dave (Aptos, CA), Barf; Tjeerd (Ravenstein, NL), Kaptein; Allard (Zaltbommel, NL)
Assignee: Acerta Pharma B.V. (Oss, NL)
Application Number:15/319,740
Patent Claims:1. A method of treating a hyperproliferative disease, comprising co-administering, to a mammal in need thereof, therapeutically effective amounts of (1) a Janus kinase-2 (JAK-2) inhibitor, and (2) a Bruton's tyrosine kinase (BTK) inhibitor.

2. The method of claim 1, wherein the BTK inhibitor is selected from the group consisting of: ##STR00212## ##STR00213##

3. The method of claim 1, wherein the BTK inhibitor is selected from the group consisting of: ##STR00214##

4. The method of claim 1, wherein the JAK-2 inhibitor is selected from the group consisting of: ##STR00215##

5. The method of claim 1, further comprising the step of administering a therapeutically effective amount of an anti-CD20 antibody selected from the group consisting of rituximab, obinutuzumab, ofatumumab, veltuzumab, tositumomab, and ibritumomab.

6. The method of claim 1, further comprising the step of administering a phosphoinositide 3-kinase (PI3K) inhibitor.

7. The method of claim 6, wherein the PI3K inhibitor is a PI3K-.delta. inhibitor.

8. The method of claim 6, wherein the PI3K inhibitor is selected from the group consisting of: ##STR00216##

9. The method of claim 1, wherein the hyperproliferative disease is a cancer, and the cancer is a B cell hematological malignancy, and wherein the B cell hematological malignancy is selected from the group consisting of chronic lymphocytic leukemia (CLL), small lymphocytic leukemia (SLL), non-Hodgkin's lymphoma (NHL), diffuse large B cell lymphoma (DLBCL), follicular lymphoma (FL), mantle cell lymphoma (MCL), Hodgkin's lymphoma, B cell acute lymphoblastic leukemia (B-ALL), Burkitt's lymphoma, Waldenstrom's macroglobulinemia (WM), Burkitt's lymphoma, multiple myeloma, and myelofibrosis.

10. The method of claim 1, wherein the hyperproliferative disease is a cancer, and wherein the cancer is a solid tumor cancer, and wherein the solid tumor cancer is selected from the group consisting of bladder cancer, non-small cell lung cancer, cervical cancer, anal cancer, pancreatic cancer, squamous cell carcinoma including head and neck cancer, renal cell carcinoma, melanoma, ovarian cancer, small cell lung cancer, glioblastoma, gastrointestinal stromal tumor, breast cancer, lung cancer, colorectal cancer, thyroid cancer, bone sarcoma, stomach cancer, oral cavity cancer, oropharyngeal cancer, gastric cancer, kidney cancer, liver cancer, prostate cancer, esophageal cancer, testicular cancer, gynecological cancer, colon cancer, and brain cancer.

11. A method of treating a cancer in a human comprising the step of co-administering (1) a therapeutically effective amount of a Janus kinase-2 (JAK-2) inhibitor, and (2) a therapeutically effective amount of a Bruton's tyrosine kinase (BTK) inhibitor, wherein the therapeutically effective amount is effective to inhibit signaling between a tumor cell of the cancer and at least one tumor microenvironment selected from the group consisting of macrophages, monocytes, mast cells, helper T cells, cytotoxic T cells, regulatory T cells, natural killer cells, myeloid-derived suppressor cells, regulatory B cells, neutrophils, dendritic cells, and fibroblasts.

12. The method of claim 11, wherein the cancer is a solid tumor cancer selected from the group consisting of bladder cancer, non-small cell lung cancer, cervical cancer, anal cancer, pancreatic cancer, squamous cell carcinoma including head and neck cancer, renal cell carcinoma, melanoma, ovarian cancer, small cell lung cancer, glioblastoma, gastrointestinal stromal tumor, breast cancer, lung cancer, colorectal cancer, thyroid cancer, bone sarcoma, stomach cancer, oral cavity cancer, oropharyngeal cancer, gastric cancer, kidney cancer, liver cancer, prostate cancer, esophageal cancer, testicular cancer, gynecological cancer, colon cancer, and brain cancer.

13. The method of claim 11, wherein the BTK inhibitor is selected from the group consisting of: ##STR00217## ##STR00218##

14. The method of claim 11, wherein the JAK-2 inhibitor is selected from the group consisting of: ##STR00219##

15. The method of claim 11, further comprising the step of administering a therapeutically effective amount of a phosphoinositide 3-kinase (PI3K) inhibitor.

16. The method of claim 15, wherein the PI3K inhibitor is selected from the group consisting of: ##STR00220##

17. A pharmaceutical composition comprising (1) a Janus kinase-2 (JAK-2) inhibitor; and (2) a Bruton's tyrosine kinase (BTK) inhibitor present in an amount therapeutically effective to treat a hyperproliferative disease.

18. The composition of claim 17, wherein the BTK inhibitor is selected from the group consisting of: ##STR00221## ##STR00222##

19. The composition of claim 17, wherein the BTK inhibitor is selected from the group consisting of: ##STR00223##

20. The composition of claim 17, wherein the JAK-2 inhibitor is selected from the group consisting of: ##STR00224##

21. The composition of claim 17, further comprising a therapeutically effective amount of an anti-CD20 antibody selected from the group consisting of rituximab, obinutuzumab, ofatumumab, veltuzumab, tositumomab, and ibritumomab.

22. The composition of claim 17, further comprising a phosphoinositide 3-kinase (PI3K) inhibitor.

23. The composition of claim 22, wherein the PI3K inhibitor is a PI3K-.delta. inhibitor.

24. The composition of claim 23, wherein the PI3K-.delta. inhibitor is selected from the group consisting of: ##STR00225## ##STR00226##

25. The composition of claim 17, wherein the hyperproliferative disease is a cancer, and the cancer is a B cell hematological malignancy, and wherein the B cell hematological malignancy is selected from the group consisting of chronic lymphocytic leukemia (CLL), small lymphocytic leukemia (SLL), non-Hodgkin's lymphoma (NHL), diffuse large B cell lymphoma (DLBCL), follicular lymphoma (FL), mantle cell lymphoma (MCL), Hodgkin's lymphoma, B cell acute lymphoblastic leukemia (B-ALL), Burkitt's lymphoma, Waldenstrom's macroglobulinemia (WM), Burkitt's lymphoma, multiple myeloma, and myelofibrosis.

26. The composition of claim 17, wherein the hyperproliferative disease is a cancer, and wherein the cancer is a solid tumor cancer, and wherein the solid tumor cancer is selected from the group consisting of bladder cancer, non-small cell lung cancer, cervical cancer, anal cancer, pancreatic cancer, squamous cell carcinoma including head and neck cancer, renal cell carcinoma, melanoma, ovarian cancer, small cell lung cancer, glioblastoma, gastrointestinal stromal tumor, breast cancer, lung cancer, colorectal cancer, thyroid cancer, bone sarcoma, stomach cancer, oral cavity cancer, oropharyngeal cancer, gastric cancer, kidney cancer, liver cancer, prostate cancer, esophageal cancer, testicular cancer, gynecological cancer, colon cancer, and brain cancer.

Summary for Patent:   Start Trial

PCT Information
PCT FiledJune 17, 2015PCT Application Number:PCT/IB2015/001811
PCT Publication Date:December 23, 2015PCT Publication Number:WO2015/193740

Details for Patent 9,949,971

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Genentech RITUXAN rituximab VIAL 103705 001 1997-11-26   Start Trial Acerta Pharma B.V. (Oss, NL) 2034-06-17 RX search
Glaxo Grp Ltd ARZERRA ofatumumab INJECTABLE; INJECTION 125326 001 2009-10-26   Start Trial Acerta Pharma B.V. (Oss, NL) 2034-06-17 RX search
Genentech GAZYVA obinutuzumab INJECTABLE;INJECTION 125486 001 2013-11-01   Start Trial Acerta Pharma B.V. (Oss, NL) 2034-06-17 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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