RU-2026111789-A - IMMEDIATE-RELEASE TYK2 INHIBITOR FORMULATIONS

Inventors

• АЛОНЦО, Давид
• ХАНЬ, Чиэнь-Суань
• Шлезингер, Эрика
• Уолд, Рэнди Дж.

Assignees

• ЭЛЮМИС ИНК.

Dates

Publication Date

20260505

Application Date

20240920

Priority Date

20230920

Claims (20)

1. 1. An immediate release oral tablet composition comprising:
2. about 20 mg, about 40 mg, or about 60 mg of the compound N-(4-((2-methoxy-3-(1-(methyl-d 3 )-1H-1,2,4-triazol-3-yl)phenyl)amino)-5-(propanoIL-3,3,3-d 3 )pyridin-2-yl)cyclopropanecarboxamide, wherein 20 mg, 40 mg, or 60 mg are based on the amount of the free base of the compound; and wherein the compound is present as a salt; and
3. a pharmaceutically acceptable excipient; wherein the composition has greater than 85% dissolution within 20 minutes as measured by the USP Dissolution Apparatus II (paddle) at 75 rpm, 900 ml pH 4.5 (50 mM acetate) with 0.25% sodium lauryl sulfate at 37°C).
4. 2. An immediate release oral tablet composition according to claim 1, comprising:
5. an intragranular component containing about 20 mg, about 40 mg, or about 60 mg of the compound, wherein the 20 mg, 40 mg, or 60 mg is based on the amount of the free base of the compound; and wherein the compound is present as a salt; and one or more pharmaceutically acceptable excipients; and
6. an extragranular component containing one or more pharmaceutically acceptable excipients.
7. 3. An immediate release oral tablet composition according to claim 1 or 2, wherein the compound is present as a hydrochloride.
8. 4. An immediate release oral tablet composition according to any one of claims 1 to 3, comprising:
9. intragranular component containing:
10. about 20 mg, about 40 mg, or about 60 mg of the compound N-(4-((2-methoxy-3-(1-(methyl-d 3 )-1H-1,2,4-triazol-3-yl)phenyl)amino)-5-(propanoIL-3,3,3-d 3 )pyridin-2-yl)cyclopropanecarboxamide hydrochloride, wherein 20 mg, 40 mg, or 60 mg is based on the amount of the free base of the compound;
11. diluent;
12. from about 3 to about 7 weight percent of a leavening agent; and
13. glidant and/or lubricant; and
14. extragranular component containing:
15. about 1 to 3 weight percent baking powder; and
16. glidant and/or lubricants;
17. where each weight percentage is based on the total weight of the intragranular and extragranular components.
18. 5. An immediate release oral tablet composition according to any one of claims 1 to 4, containing 20 mg of the compound.
19. 6. An immediate release oral tablet composition according to any one of claims 1 to 4, containing 40 mg of the compound.
20. 7. An immediate-release oral tablet composition with a fixed dose, comprising: