IP Library Granted Patent US 12,144,798
Granted Patent B2
US 12,144,798 · App. 17/834,367 · Granted Nov 19, 2024

(3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8ahexahydropyrrolo[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
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,144,798
App. No.
17/834,367
Granted
Nov 19, 2024
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 (20)

1. A method of ameliorating Alzheimer's Disease in a human patient consisting of 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 Alzheimer's Disease.

2. The method of claim 1 , wherein the pharmaceutical composition 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 the pharmaceutical composition is administered parenterally in an amount from about 0.5 mg to about 30 mg on a once-a-day basis.

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

5. The method of claim 4 , wherein said peak plasma circulating level is reached within about 3 hours after said administering.

6. The method of claim 1 , wherein the administration of said pharmaceutical composition provides a plasma circulating level of posiphen that is equal to or greater than about 20 ng/ml for at least 12 hours after said administering.

7. The method of claim 1 , wherein the administration of said pharmaceutical composition provides a plasma circulating level of posiphen that is equal to or greater than about 20 ng/ml for at least 9 hours after said administering.

8. The method of claim 1 , wherein said administering results in a steady state plasma concentration of posiphen of at least about 100 ng/ml in said subject.

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

10. The method of claim 1 , wherein the pharmaceutical composition is administered intravenously in an amount from about 0.1 mg/day to about 25 mg/day.

11. The method of claim 1 wherein the pharmaceutical composition is administered intramuscularly in an amount from about 0.3 mg/day to about 30 mg/day.

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

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

14. The method of claim 1 , wherein the pharmaceutical composition includes from about 15 mg to less than about 30 mg of posiphen or a pharmaceutically acceptable salt thereof.

15. A method of ameliorating Alzheimer's Disease in a human patient, consisting of administering a pharmaceutical composition consisting of from about 7.5 mg to less than about 20 mg of posiphen or a pharmaceutically acceptable salt thereof together with one or more pharmaceutically acceptable excipients, on a once-a-day basis, such that the production of neurotoxic aggregating protein in the human patient is inhibited.

16. The method of claim 1 , wherein the administration of said pharmaceutical composition provides a peak plasma circulating level ranges from about 10 ng/ml to about 160 ng/ml in the human patient.

17. 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, and dry powder or aerosolized formulations for inhalation.

18. The method of claim 1 , wherein the pharmaceutical composition provides (i) disease modification; (ii) symptomatic improvement; or (iii) both (i) and (ii) to the human patient.

19. The method of claim 1 , whereby administration of the posiphen inhibits synthesis of APP, alpha-synuclein, tau, prions, and combinations of any of the foregoing.

20. The method of claim 1 , wherein posiphen or a pharmaceutically acceptable salt thereof is administered in an amount less than 20 mg/day.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 9, 2022
From: MACCECCHINI, MARIA
To: QR PHARMA, INC.
Reel/Frame 060149/0016 →
CHANGE OF NAME Recorded Jun 9, 2022
From: QR PHARMA, INC.
To: ANNOVIS BIO, INC.
Reel/Frame 060328/0401 →
Continuity (5)
Continuation 16994881 · Aug 17, 2020
Continuation 16504813 · Jul 8, 2019
Continuation 15450937 · Mar 6, 2017
Continuation 13041211 · Mar 4, 2011
Related Publication 20220323413A1 · Oct 13, 2022