RU-2026104385-A - 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea for use in the treatment of diseases associated with the 5-HT serotonin receptor

Inventors

• Бёрстейн Итан С.

Assignees

• АКАДИА ФАРМАСЬЮТИКАЛЗ ИНК.

Dates

Publication Date

20260508

Application Date

20240801

Priority Date

20230802

Claims (20)

1. 1. A pharmaceutical composition containing from about 10 mg to about 90 mg of 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea or an approximately equivalent amount of its pharmaceutically acceptable salt and/or hydrate of a pharmaceutically acceptable salt as an active ingredient and one or more pharmaceutically acceptable excipients.
2. 2. A pharmaceutical composition for the treatment of diseases and conditions associated with the 5-HT serotonin receptor, containing from about 10 mg to about 90 mg of 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea or an approximately equivalent amount of its pharmaceutically acceptable salt and/or hydrate of a pharmaceutically acceptable salt as an active ingredient and one or more pharmaceutically acceptable excipients.
3. 3. A pharmaceutical composition according to claim 1 or 2, characterized in that said composition contains from about 15 mg to about 85 mg of 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea or an approximately equivalent amount of its pharmaceutically acceptable salt and/or a hydrate of a pharmaceutically acceptable salt.
4. 4. A pharmaceutical composition according to any one of claims 1-3, characterized in that said composition contains from about 20 mg to about 80 mg of 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea or an approximately equivalent amount of its pharmaceutically acceptable salt and/or a hydrate of a pharmaceutically acceptable salt.
5. 5. A pharmaceutical composition according to any one of claims 1-4, characterized in that said composition contains from about 25 mg to about 65 mg of 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea or an approximately equivalent amount of its pharmaceutically acceptable salt and/or a hydrate of a pharmaceutically acceptable salt.
6. 6. A pharmaceutical composition according to any one of claims 1-5, characterized in that said composition contains from about 25 mg to about 35 mg of 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea or an approximately equivalent amount of its pharmaceutically acceptable salt and/or a hydrate of a pharmaceutically acceptable salt.
7. 7. A pharmaceutical composition according to any one of claims 1-6, characterized in that said composition contains about 30 mg of 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea or an approximately equivalent amount of its pharmaceutically acceptable salt and/or a hydrate of a pharmaceutically acceptable salt.
8. 8. A pharmaceutical composition according to any one of claims 1-5, characterized in that said composition contains from about 55 mg to about 65 mg of 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea or an approximately equivalent amount of its pharmaceutically acceptable salt and/or a hydrate of a pharmaceutically acceptable salt.
9. 9. A pharmaceutical composition according to any one of claims 1-5, characterized in that said composition contains about 60 mg of 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea or an approximately equivalent amount of its pharmaceutically acceptable salt and/or a hydrate of a pharmaceutically acceptable salt.
10. 10. A pharmaceutical composition according to any one of claims 1-9, characterized in that said active ingredient contains 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea hemitartrate.
11. 11. A pharmaceutical composition according to any one of claims 1-9, characterized in that said active ingredient contains 3-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea hemitartrate monohydrate.
12. 12. A pharmaceutical composition according to any one of paragraphs 1-11, characterized in that said composition is included in a formulation for oral administration.
13. 13. A pharmaceutical composition according to any one of paragraphs 1-12, characterized in that said composition is included in a formulation for administration to humans.
14. 14. A pharmaceutical composition according to any one of paragraphs 1-13, characterized in that said composition is included in a formulation for administration to a human being once a day.
15. 15. A pharmaceutical composition according to any one of paragraphs 1-13, characterized in that said composition is included in a formulation for administration to a human in the form of several doses per day.
16. 16. A pharmaceutical composition according to any one of claims 1-15, characterized in that oral administration to a human provides an average C max,ss in the range from about 20 ng/ml to about 250 ng/ml.
17. 17. A pharmaceutical composition according to any one of claims 1-15, characterized in that oral administration to a human provides an average C max,ss in the range from about 30 ng/ml to about 90 ng/ml.
18. 18. A pharmaceutical composition according to any one of claims 1-15, characterized in that oral administration to a human provides an average C max , ss in the range from about 100 ng/ml to about 180 ng/ml.
19. 19. A pharmaceutical composition according to any one of claims 1-15, characterized in that oral administration to humans provides an average C max,ss of approximately 68 ng/ml.
20. 20. A pharmaceutical composition according to any one of claims 1-15, characterized in that oral administration to humans provides an average C max.ss of approximately 133 ng/ml.