IP Library Granted Patent US 11,376,238
Granted Patent B2
US 11,376,238 · App. 16/994,921 · Granted Jul 5, 2022

(3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate and methods of treating or preventing neurodegeneration

Inventor: Maria Maccecchini (West Chester, PA)
Assignee: ANNOVIS BIO, INC.
A61K31/407A61K9/0053A61K9/20A61K9/2886A61K9/48A61K9/4825A61P25/28
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Quick Facts
Patent No.
US 11,376,238
App. No.
16/994,921
Granted
Jul 5, 2022
Kind
B2
Abstract

The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.

Claims (19)

1. A method of ameliorating Huntington's disease in a human patient, by administering a pharmaceutical composition consisting of posiphen or a pharmaceutically acceptable salt thereof in an amount from about 0.1 mg/day to about 30 mg/day together with one or more pharmaceutically acceptable excipients, on a once a day basis to a human patient suffering from Huntington's disease.

2. The method of claim 1 , wherein posiphen or a pharmaceutically acceptable salt thereof is administered orally in an amount from about 1 mg to about 30 mg on a once a day basis.

3. The method of claim 1 , wherein posiphen or a pharmaceutically acceptable salt thereof is administered parenterally in an amount from about 0.5 mg to about 30 mg/day.

4. The method of claim 1 , wherein posiphen or a pharmaceutically acceptable salt thereof is administered intravenously in an amount from about 0.1 mg/day to about 25 mg/day.

5. The method of claim 1 , wherein posiphen or a pharmaceutically acceptable salt thereof is administered intramuscularly in an amount from about 0.3 mg/day to about 30 mg/day.

6. The method of claim 1 , wherein the peak plasma circulating level ranges of posiphen are from about 10 ng/mL to about 160 ng/ml in the human patient.

7. The method of claim 1 , wherein the peak plasma circulating level of posiphen is reached within about 6 hours after said administering the pharmaceutical composition.

8. The method of claim 1 , wherein the plasma circulating level of posiphen is equal to or greater than about 20 ng/mL for at least 9 hours after administering the pharmaceutical composition.

9. The method of claim 1 , wherein the administration results in a brain level of posiphen that ranges from about 4 to about 10 times the plasma level of posiphen in the human patient.

10. The method of claim 1 , wherein the half-life of posiphen in cerebrospinal fluid after administering is about 12 hours.

11. The method of claim 1 , wherein the half-life of posiphen in plasma after administering is about 5 hours.

12. The method of claim 1 , wherein the pharmaceutical composition is selected from the group consisting of tablets, capsules, caplets, pills, gel caps, troches, dispersions, suspensions, solutions, syrups, granules, beads, transdermal patches, gels, powders, pellets, magmas, lozenges, creams, pastes, plasters, lotions, discs, suppositories, liquid sprays for nasal or oral administration, dry powder or aerosolized formulations for inhalation, and a composition for intravesical administration.

13. The method of claim 1 , wherein the pharmaceutical composition inhibits the synthesis of HTT.

14. The method of claim 2 , wherein the pharmaceutical composition inhibits the synthesis of HTT.

15. A method of ameliorating Huntington's disease in a human patient by administering a pharmaceutical composition consisting of posiphen or a pharmaceutically acceptable salt thereof in an amount from about 0.1 mg/day to about 30 mg/day together with one or more pharmaceutically acceptable excipients, to a human patient suffering from Huntington's disease.

16. The method of claim 15 , wherein the pharmaceutical composition is administered orally on a once a day basis in an amount from about 1 mg to about 30 mg.

17. The method of claim 15 , wherein posiphen or a pharmaceutically acceptable salt thereof is administered orally in an amount from about 10 mg to about 30 mg on a once a day basis.

18. The method of claim 15 , wherein posiphen or a pharmaceutically acceptable salt thereof is administered parenterally in an amount from about 0.5 mg/day to about 30 mg/day.

19. The method of claim 15 , wherein the pharmaceutical composition inhibits the synthesis of HTT.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 28, 2020
From: MACCECCHINI, MARIA
To: QR PHARMA, INC.
Reel/Frame 053625/0763 →
CHANGE OF NAME Recorded Aug 28, 2020
From: QR PHARMA, INC.
To: ANNOVIS BIO, INC.
Reel/Frame 053636/0865 →
Continuity (4)
Continuation 16504813 · Jul 8, 2019
Continuation 15450937 · Mar 6, 2017
Continuation 13041211 · Mar 4, 2011
Related Publication 20210093610A1 · Apr 1, 2021