Claims for Patent: 11,814,368

Summary for Patent: 11,814,368

Title:	Triazine derivatives having virus replication inhibitory activity and pharmaceutical composition comprising the same
Abstract:	The present invention provides a compound exhibiting coronavirus 3 CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same. Furthermore, the present invention provides a crystalline form useful as an active pharmaceutical ingredient, and a pharmaceutical composition comprising the same.A compound represented by Formula:or a pharmaceutically acceptable salt thereof.
Inventor(s):	Yuki Tachibana, Shota UEHARA, Yuto Unoh, Kenji Nakahara, Yoshiyuki Taoda, Yukiko YAMATSU, Shigeru Ando, Michihito SASAKI
Assignee:	Hokkaido University NUC , Shionogi and Co Ltd
Application Number:	US17/733,366
Patent Claims:	1. A compound represented by the following Formula: or a pharmaceutically acceptable salt thereof. 2. A pharmaceutical composition comprising the compound according to claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. 3. A coronavirus 3 CL protease inhibitor comprising the compound according to claim 1, or a pharmaceutically acceptable salt thereof. 4. A coronavirus replication inhibitor comprising the compound according to claim 1 , or a pharmaceutically acceptable salt thereof. 5. The coronavirus replication inhibitor according to claim 4, wherein the coronavirus is an alphacoronavirus and/or betacoronavirus. 6. The coronavirus replication inhibitor according to claim 4, wherein the coronavirus is SARS-CoV-2. 7. A method for treating and/or preventing a disease associated with coronavirus 3 CL proteases, comprising administering an effective amount of the compound according to claim 1, or a pharmaceutically acceptable salt thereof, to a patient in need thereof. 8. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, for use in treating and/or preventing a disease associated with coronavirus 3CL proteases. 9. A complex comprising a compound represented by Formula (I-B): and fumaric acid. 10. The complex according to claim 9, wherein the compound represented by Formula (I-B): and fumaric acid are present in a molar ratio of 1:1. 11. The complex according to claim 9, which is a fumaric acid cocrystal Form I. 12. The fumaric acid cocrystal Form I according to claim 11, which exhibits a powder X-ray diffraction pattern having peaks at diffraction angles (2θ): 9.5 ± 0.2°, 10.9 ± 0.2°, 18.6 ± 0.2°, 23.5 ± 0.2° and 24.6 ± 0.2°. 13. The fumaric acid cocrystal Form I according to claim 11, which exhibits a powder X-ray diffraction pattern having peaks at diffraction angles (2θ): 7.8 ± 0.2°, 9.5 ± 0.2°, 10.1 ± 0.2°, 10.9 ± 0.2°, 13.8 ± 0.2°, 14.7 ± 0.2°, 18.6 ± 0.2°, 22.6 ± 0.2°, 23.5 ± 0.2° and 24.6 ± 0.2°. 14. The fumaric acid cocrystal Form I according to claim 11, which exhibits a Raman spectrum having Raman spectral peaks: 676.3 cm-1±2 cm-1, 748.0 cm-1±2 cm-1, 1029.3cm- 1±2 cm-1, 1374.4 cm-1±2 cm-1, 1515.5 cm-1±2 cm-1, 1665.7 cm-1±2 cm-1, 1715.7 cm-1±2 cm-1 and 1739.1 cm-1±2 cm-1. 15. A pharmaceutical composition comprising the fumaric acid cocrystal Form I according to claim 11.