IP Library Granted Patent US 10,940,149
Granted Patent B1
US 10,940,149 · App. 17/084,971 · Granted Mar 9, 2021

Kinase inhibitor salts and compositions thereof

Inventors: Fang-Yu Liu (San Jose, CA); K. C. Sung (Tainan, TW); Chin-Yao Yang (Tainan, TW); Chi-Cheng Lin (Tainan, TW); Yi-Hsin Lin (Tainan, TW); Li Qiao (San Jose, CA)
Assignee: HANDA ONCOLOGY, LLC
A61K31/506A61K9/0053A61K9/20A61K9/48A61P35/02
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Quick Facts
Patent No.
US 10,940,149
App. No.
17/084,971
Granted
Mar 9, 2021
Kind
B1
Abstract

The present invention relates to polymorphic forms of nilotinib lauryl sulfate salt.

Claims (16)

1. A crystalline nilotinib lauryl sulfate salt characterized by an x-ray powder diffraction (XRPD) pattern with 2θ peaks at 5.6±0.2, 8.5±0.2 and one or more 2θ peaks selected from the group consisting of 9.4±0.2, 19.1±0.2, 21.5±0.2, and 24.9±0.2.

2. The crystalline nilotinib lauryl sulfate salt of claim 1 further characterized by an XRPD pattern with one or more 2θ peaks selected from the group consisting of 13.1±0.2, 20.2±0.2, 26.5±0.2, 27.7±0.2, and 29.0±0.2.

3. The crystalline nilotinib lauryl sulfate salt of claim 1 characterized by an XRPD pattern with 2θ peaks at 5.6±0.2, 8.5±0.2, 9.4±0.2, 19.1±0.2, 21.5±0.2, and 24.9±0.2.

4. The crystalline nilotinib lauryl sulfate salt of claim 3 further characterized by an XRPD pattern with one or more 2θ peaks selected from the group consisting of 13.1±0.2, 20.2±0.2, 26.5±0.2, 27.7±0.2 and 29.0±0.2.

5. The crystalline nilotinib lauryl sulfate salt of claim 1 characterized by an XRPD pattern with 2θ peaks at 5.6±0.2, 8.5±0.2, 9.4±0.2, 19.1±0.2, 20.2±0.2, 21.5±0.2, 24.9±0.2, 26.5±0.2 and 27.7±0.2 and one or more 2θ peaks selected from the group consisting of 9.2±0.2, 13.1±0.2, 13.7±0.2, 17.1±0.2, 17.8±0.2, 22.0±0.2, 25.8±0.2 and 29.0±0.2.

6. The crystalline nilotinib lauryl sulfate salt of claim 1 characterized by an XRPD pattern with 2θ peaks at 5.6±0.2, 8.5±0.2, 9.4±0.2, 13.1±0.2, 13.7±0.2, 17.1±0.2, 19.1±0.2, 20.2±0.2, 21.5±0.2, 24.9±0.2, 26.5±0.2 and 27.7±0.2.

7. An oral pharmaceutical composition comprising the crystalline nilotinib lauryl sulfate salt of claim 1 and at least one pharmaceutically acceptable excipient.

8. A crystalline nilotinib lauryl sulfate salt characterized by an x-ray powder diffraction (XRPD) pattern with 2θ peaks at 5.6±0.2, 8.5±0.2 and one or more 2θ peaks selected from the group consisting of 17.1±0.2, 20.2±0.2, 22.0±0.2, 22.8±0.2, 25.8±0.2, 26.1±0.2 and 26.6±0.2.

9. The crystalline nilotinib lauryl sulfate salt of claim 8 characterized by an XRPD pattern with 2θ peaks at 5.6±0.2, 8.5±0.2, 26.6±0.2, and one or more 2θ peaks selected from the group consisting of 9.4±0.2, 13.0±0.2, 13.6±0.2, 17.1±0.2, 19.1±0.2, 20.2±0.2, 21.5±0.2, 22.0±0.2, 24.8±0.2, 25.8±0.2, and 26.1±0.2.

10. The crystalline nilotinib lauryl sulfate salt of claim 8 characterized by an XRPD pattern with 2θ peaks at 5.6±0.2, 8.5±0.2, 9.4±0.2, 13.0±0.2, 13.6±0.2, 17.1±0.2, 19.1±0.2, 20.2±0.2, 21.5±0.2, 22.8±0.2, 24.8±0.2 and 26.6±0.2.

11. An oral pharmaceutical composition comprising the crystalline nilotinib lauryl sulfate salt of claim 8 and at least one pharmaceutically acceptable excipient.

12. A crystalline nilotinib lauryl sulfate salt characterized by an x-ray powder diffraction (XRPD) pattern with 2θ peaks at 5.6±0.2, 8.5±0.2 and one or more 2θ peaks selected from the group consisting of 9.1±0.2, 16.7±0.2, 17.9±0.2, 18.4±0.2, 19.6±0.2, 20.9±0.2, 23.0±0.2, 24.1±0.2, 25.8±0.2, 27.7±0.2, and 29.0±0.2.

13. The crystalline nilotinib lauryl sulfate salt of claim 12 further characterized by an XRPD pattern with one or more 2θ peaks selected from the group consisting of 9.6±0.2, 13.1±0.2, 13.9±0.2, 17.2±0.2, 19.1±0.2, 21.3±0.2 and 24.7±0.2.

14. The crystalline nilotinib lauryl sulfate salt of claim 12 characterized by an XRPD pattern with 2θ peaks at 5.6±0.2, 8.5±0.2, 9.6±0.2, 13.1±0.2, 13.9±0.2, 17.2±0.2, 19.1±0.2, 21.3±0.2, 23.0±0.2, 24.7±0.2, 27.7±0.2, and 29.0±0.2.

15. The crystalline nilotinib lauryl sulfate salt of claim 14 further characterized by an XRPD pattern with one or more 2θ peaks at 30.0±0.2, 30.7±0.2, 33.8±0.2, 34.6±0.2 and 38.7±0.2.

16. An oral pharmaceutical composition comprising the crystalline nilotinib lauryl sulfate salt of claim 12 and at least one pharmaceutically acceptable excipient.

Continuity (6)
Continuation 16798935 · Feb 24, 2020
Continuation 16701941 · Dec 3, 2019
Continuation PCTUS2019036947 · Jun 13, 2019
Provisional Application 62685411 · Jun 15, 2018
Provisional Application 62791356 · Jan 11, 2019
Provisional Application 62811368 · Feb 27, 2019
Cited By (5)
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