You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 28, 2024

Claims for Patent: 9,949,971


✉ Email this page to a colleague

« Back to Dashboard


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.

Details for Patent 9,949,971

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. RITUXAN rituximab Injection 103705 11/26/1997 ⤷  Try a Trial 2034-06-17
Novartis Pharmaceuticals Corporation ARZERRA ofatumumab Injection 125326 10/26/2009 ⤷  Try a Trial 2034-06-17
Novartis Pharmaceuticals Corporation ARZERRA ofatumumab Injection 125326 04/01/2011 ⤷  Try a Trial 2034-06-17
Novartis Pharmaceuticals Corporation KESIMPTA ofatumumab Injection 125326 08/20/2020 ⤷  Try a Trial 2034-06-17
Genentech, Inc. GAZYVA obinutuzumab Injection 125486 11/01/2013 ⤷  Try a Trial 2034-06-17
Genentech, Inc. RITUXAN HYCELA rituximab and hyaluronidase human Injection 761064 06/22/2017 ⤷  Try a Trial 2034-06-17
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.