IP Library Granted Patent US 9,475,818
Granted Patent B2
US 9,475,818 · App. 14/832,962 · Granted Oct 25, 2016

Selective PI3K delta inhibitors

Inventors: Swaroop Kumar V. S. Vakkalanka (La Chaux-de-Fonds, CH); Meyyappan Muthuppalaniappan (Hyderabad, IN); Dhanapalan Nagarathnam (La Chaux-de-Fonds, CH)
Assignee: RHIZEN PHARMACEUTICALS SA
C07D487/04A61K31/519A61K45/06
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Quick Facts
Patent No.
US 9,475,818
App. No.
14/832,962
Granted
Oct 25, 2016
Kind
B2
Abstract

The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.

Claims (22)

1. A compound selected from

(S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-3-(3-fluorophenyl)-4H-chromen-4-one

and pharmaceutically acceptable salts thereof.

2. A pharmaceutical composition comprising a compound of claim 1 and at least one pharmaceutically acceptable carrier.

3. A method for the treatment of leukemia comprising the step of administering to a subject in need thereof an effective amount of the compound of claim 1 .

4. The method of claim 3 , further comprising the step of administering simultaneously or sequentially to a subject in need thereof at least one other anti-cancer agent.

5. The compound of claim 1 , wherein the compound has an enantiomeric excess of at least 98%.

6. The method of claim 3 , wherein the leukemia is chronic lymphocytic leukemia (CLL).

7. The method of claim 3 , wherein the leukemia is acute lymphocytic leukemia.

8. The method of claim 3 , wherein the leukemia is acute myelocytic leukemia (AML).

9. The method of claim 3 , wherein the leukemia is promyelocytic leukemia.

10. The method of claim 3 , wherein the leukemia is chronic myelogenous leukemia.

11. (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-3-(3-fluorophenyl)-4H-chromen-4-one.

12. The compound of claim 11 , wherein the compound has an enantiomeric excess of at least 98%.

13. A pharmaceutical composition comprising a compound of claim 11 and at least one pharmaceutically acceptable carrier.

14. A method for the treatment of leukemia comprising the step of administering to a subject in need thereof an effective amount of the compound of claim 11 .

15. The method of claim 14 , further comprising the step of administering simultaneously or sequentially to a subject in need thereof at least one other anti-cancer agent.

16. The method of claim 14 , wherein the leukemia is chronic lymphocytic leukemia (CLL).

17. The method of claim 14 , wherein the leukemia is acute lymphocytic leukemia.

18. The method of claim 14 , wherein the leukemia is acute myelocytic leukemia (AML).

19. The method of claim 14 , wherein the leukemia is promyelocytic leukemia.

20. The method of claim 14 , wherein the leukemia is chronic myelogenous leukemia.

Assignments (2)
CHANGE OF ADDRESS Recorded Oct 6, 2021
From: RHIZEN PHARMACEUTICALS AG
To: RHIZEN PHARMACEUTICALS AG
Reel/Frame 057836/0286 →
CHANGE OF ADDRESS Recorded Mar 22, 2021
From: RHIZEN PHARMACEUTICALS SA
To: RHIZEN PHARMACEUTICALS SA
Reel/Frame 056775/0375 →
Priority Claims (2)
IN 2692/CHE/2012 · Jul 4, 2012 · national
IN 2693/CHE/2012 · Jul 4, 2012 · national
Continuity (4)
Continuation 13933856 · Jul 2, 2013
Provisional Application 61691561 · Aug 21, 2012
Provisional Application 61691586 · Aug 21, 2012
Related Publication 20150361083A1 · Dec 17, 2015