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Last Updated: March 28, 2024

Details for Patent: 8,980,901


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Title:5-fluoro-3-phenyl-2[1-(9H-purin-6-ylamino)propyl]-3H-quinazolin-4-one and 6-fluoro-3-phenyl-2-[1-(9H-purin-6-ylamino)ethyl]-3H-quinazolin-4-one as inhibitors of human phosphatidylinositol 3-kinase delta
Abstract: Compounds that inhibit PI3K.delta. activity, including compounds that selectively inhibit PI3K.delta. activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K.delta.) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K.delta. plays a role in leukocyte function, using the compounds also are disclosed. Exemplary compounds disclosed in this application are shown below: ##STR00001##
Inventor(s): Fowler; Kerry W. (Seattle, WA), Huang; Danwen (Bellevue, WA), Kesicki; Edward A. (Bothell, WA), Ooi; Hua Chee (Mill Creek, WA), Oliver; Amy (Bothell, WA), Ruan; Fuqiang (Bellevue, WA), Treiberg; Jennifer (Redmond, WA), Puri; Kamal Deep (Lynnwood, WA)
Assignee: Icos Corporation (Foster City, CA)
Filing Date:Oct 08, 2013
Application Number:14/049,163
Claims:1. A method of treating a hematological malignancy in a human, comprising administering to the human a compound selected from the group consisting of ##STR00184## or a pharmaceutically acceptable salt thereof.

2. The method of claim 1, wherein the hematological malignancy is selected from the group consisting of leukemia and lymphoma.

3. The method of claim 1, wherein the hematological malignancy is non-Hodgkin's lymphoma.

4. The method of claim 1, wherein the hematological malignancy is Hodgkin's lymphoma.

5. The method of claim 1, wherein the hematological malignancy is lymphocytic leukemia.

6. The method of claim 1, wherein the hematological malignancy is multiple myeloma.

7. The method of claim 1, wherein the compound or pharmaceutically acceptable salt thereof is the S-enantiomer.

8. The method of claim 1, further comprising administering a pharmaceutical composition comprising a) at least one pharmaceutically acceptable excipient; and b) the compound or a pharmaceutically acceptable salt thereof.

9. The method of claim 8, wherein the compound or pharmaceutically acceptable salt thereof is the S-enantiomer.

10. A method of treating a hematological malignancy in a human comprising administering to the human a compound having the structure: ##STR00185## or a pharmaceutically acceptable salt thereof.

11. The method of claim 10, wherein the hematological malignancy is selected from the group consisting of leukemia and lymphoma.

12. The method of claim 10, wherein the hematological malignancy is non-Hodgkin's lymphoma.

13. The method of claim 10, wherein the hematological malignancy is Hodgkin's lymphoma.

14. The method of claim 10, wherein the hematological malignancy is lymphocytic leukemia.

15. The method of claim 10, wherein the hematological malignancy is multiple myeloma.

16. A method of treating a hematological malignancy in a human comprising administering to the human a compound having the structure: ##STR00186## or a pharmaceutically acceptable salt thereof.

17. The method of claim 16, wherein the hematological malignancy is selected from the group consisting of leukemia and lymphoma.

18. The method of claim 16, wherein the hematological malignancy is non-Hodgkin's lymphoma.

19. The method of claim 16, wherein the hematological malignancy is Hodgkin's lymphoma.

20. The method of claim 16, wherein the hematological malignancy is lymphocytic leukemia.

21. The method of claim 16, wherein the hematological malignancy is multiple myeloma.

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