Claims for Patent: 11,919,907

Summary for Patent: 11,919,907

Title:	Deuterated JAK inhibitor and uses thereof
Abstract:	Disclosed is a JAK1 and/or JAK2 inhibitor of the following structural formula: or a pharmaceutically acceptable salt thereof. This invention also provides pharmaceutical compositions comprising a compound of Formula (I), optionally including additional therapeutic agents, and use in methods of treatment for hair loss disorders.
Inventor(s):	I. Robert Silverman, Changhua Liu
Assignee:	Sun Pharmaceutical Industries Inc
Application Number:	US17/327,044
Patent Claims:	1. A compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof, wherein Y1 is selected from hydrogen and deuterium; each Y2 is selected from hydrogen and deuterium; and each Y3 is selected from hydrogen and deuterium; provided that at least one of Y1, Y2, and Y3 is deuterium; and wherein each position designated specifically as deuterium has at least 90% deuterium incorporation. 2. The compound of claim 1, selected from: or a pharmaceutically acceptable salt thereof. 3. The compound of claim 2, which is Compound 10: or a pharmaceutically acceptable salt thereof. 4. The compound of claim 1, wherein each position designated specifically as deuterium has at least 95% deuterium incorporation. 5. The compound of claim 1, wherein each position designated specifically as deuterium has at least 97% deuterium incorporation. 6. The compound of claim 1, wherein the pharmaceutically acceptable salt is a phosphate salt. 7. A pharmaceutical composition comprising a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof, wherein Y1 is selected from hydrogen and deuterium; each Y2 is selected from hydrogen and deuterium; each Y3 is selected from hydrogen and deuterium; and wherein each position designated specifically as deuterium has at least 90% deuterium incorporation; and a pharmaceutically acceptable carrier. 8. The pharmaceutical composition of claim 7, further comprising an additional therapeutic agent which is a JAK inhibitor. 9. The pharmaceutical composition of claim 8, wherein the additional therapeutic agent which is a JAK inhibitor is selected from CTP-543, ruxolitinib, tofacitinib, baricitinib, upadacitinib, fedratinib, filgotinib, momelotinib, pacritinib, itacitinib, peficitinib, PF-06651600, PF-06700841 (brepocitinib), and abrocitinib, or a pharmaceutically acceptable salt thereof. 10. The pharmaceutical composition of claim 9, wherein the compound of Formula (I) is or a pharmaceutically acceptable salt thereof, and the JAK inhibitor is CTP-543, or a pharmaceutically acceptable salt thereof. 11. The pharmaceutical composition of claim 7, wherein the pharmaceutical formulation is in tablet form. 12. The pharmaceutical composition of claim 7, wherein the pharmaceutical formulation is in capsule form. 13. A method of inhibiting the activity of one or more of JAK1 or JAK2 in a cell, comprising contacting the cell with a compound of claim 1, or a pharmaceutically acceptable salt thereof. 14. The method of claim 13, further comprising contacting the cell with one or more additional JAK inhibitors selected from CTP-543, ruxolitinib, tofacitinib, baricitinib, upadacitinib, fedratinib, filgotinib, momelotinib, pacritinib, itacitinib, peficitinib, PF-06651600, PF-06700841 (brepocitinib), and abrocitinib; or a pharmaceutically acceptable salt thereof. 15. A method of treating a disease or disorder in a human subject that is beneficially treated by inhibiting the activity of a JAK, the method comprising administering to the subject an effective amount of a pharmaceutical composition comprising a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof, wherein Y1 is selected from hydrogen and deuterium; each Y2 is selected from hydrogen and deuterium; and each Y3 is selected from hydrogen and deuterium wherein each position designated specifically as deuterium has at least 90% deuterium incorporation; and a pharmaceutically acceptable carrier. 16. The method of claim 15, wherein the disease or disorder is a hair loss disorder selected from alopecia areata, alopecia totalis, alopecia universalis, ophiasis, androgenic alopecia, and telogen effluvium. 17. The method of claim 16, wherein the hair loss disorder is alopecia areata. 18. The method of claim 15, wherein the pharmaceutically acceptable salt is a phosphate salt. 19. A method of treating a disease or disorder that is beneficially treated by inhibiting the activity of a JAK in a human subject in need thereof, comprising administering to the human subject an effective amount of a pharmaceutical composition comprising: (i) a first JAK inhibitor which is a compound represented by structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein, Y1 is selected from hydrogen and deuterium; each Y2 is selected from hydrogen and deuterium; and each Y3 is selected from hydrogen and deuterium wherein each position designated specifically as deuterium has at least 90% deuterium incorporation; (ii) a second JAK inhibitor; and (iii) a pharmaceutically acceptable carrier. 20. The method of claim 19, wherein the second JAK inhibitor is selected from CTP-543, ruxolitinib, tofacitinib, baricitinib, upadacitinib, fedratinib, filgotinib, momelotinib, pacritinib, itacitinib, peficitinib, PF-06651600, PF-06700841 (brepocitinib), and abrocitinib, and pharmaceutically acceptable salts thereof. 21. The method of claim 19, wherein the compound of Formula (I) is or a pharmaceutically acceptable salt thereof, and the second JAK inhibitor is CTP-543, or a pharmaceutically acceptable salt thereof. 22. The method of claim 21, wherein the pharmaceutical composition is administered at 16 mg/day or 24 mg/day of the first JAK inhibitor and the second JAK inhibitor together. 23. The compound of claim 3, wherein the pharmaceutically acceptable salt is a phosphate salt. 24. The method of claim 21, wherein the pharmaceutically acceptable salt is a phosphate salt.