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Last Updated: April 25, 2024

Claims for Patent: 10,189,818


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Summary for Patent: 10,189,818
Title:5-(5-(2-(3-aminopropdoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2- -carbonitfile (S)-lactate monohydrate
Abstract: The disclosure herein includes 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2- -carbonitrile (S)-lactate monohydrate that inhibits Chk1/2 and is useful in the treatment of cancer.
Inventor(s): Ennett-Shepard; Alessandra B. (Indianapolis, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:15/513,185
Patent Claims:1. A compound which is 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2- -carbonitrile (S)-lactate monohydrate.

2. The compound according to claim 1 in crystalline form.

3. The compound according to claim 2, wherein the crystalline form is characterized by a X-ray powder diffraction pattern (CuKa radiation, .lamda.=1.54060 .ANG.) comprising a peak at 12.6, and one or more peaks at 24.8, 25.5, 8.1, 6.6, 12.3, and 16.3 (2.theta.+/-0.2.degree.).

4. A pharmaceutical composition comprising 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2- -carbonitrile (S)-lactate monohydrate and one or more pharmaceutically acceptable carriers, diluents, or excipients.

5. The pharmaceutical composition of claim 4, wherein 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2- -carbonitrile (S)-lactate monohydrate is in crystalline form.

6. The pharmaceutical composition of claim 5, wherein the crystalline form is characterized by a X-ray powder diffraction pattern (CuKa radiation, .lamda.=1.54060 .ANG.) comprising a first peak at 12.6, and one or more peaks at 24.8, 25.5, 8.1, 6.6, 12.3, and 16.3 (2.theta.+/-0.2.degree.).

7. A method of treating cancer comprising: administering to a patient in need thereof an effective amount of a compound which is 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2- -carbonitrile (S)-lactate monohydrate.

8. The method of claim 7, wherein the compound is in crystalline form.

9. The method of claim 8, where the crystalline form is characterized by a X-ray powder diffraction pattern (CuKa radiation, .lamda.=1.54060 .ANG.) comprising a peak at 12.6, and one or more peaks at 24.8, 25.5, 8.1, 6.6, 12.3, and 16.3 (2.theta.+/-0.2.degree.).

10. The method according to claim 7, wherein the compound is administered with one or more pharmaceutically acceptable carriers, diluents, or excipients.

11. The method according to claim 7, wherein the method further comprises administering ionizing radiation.

12. The method according to claim 7, wherein the method further comprises administering one or more chemotherapy agents.

13. The method according to claim 7, wherein the method further comprises administering a chemotherapy agent selected from the group consisting of 5-fluorouracil, hydroxyurea, gemcitabine, methotrexate, pemetrexed, doxorubicin, etoposide, cetuximab, cisplatin, taxol, and combinations thereof.

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